Shams Abdel-hafez - Academia.edu (original) (raw)
Papers by Shams Abdel-hafez
Journal of Heterocyclic Chemistry, Nov 21, 2022
Both 2‐(N‐arylcarbamoyl)methylsulfanyl‐3‐cyano‐5‐ethoxycarbonyl‐6‐methyl‐4‐(2′‐thienyl)pyridines ... more Both 2‐(N‐arylcarbamoyl)methylsulfanyl‐3‐cyano‐5‐ethoxycarbonyl‐6‐methyl‐4‐(2′‐thienyl)pyridines 2a‐e and their isomers, 3‐amino‐2‐(N‐arylcarbamoyl)‐5‐ethoxy‐carbonyl‐6‐methyl‐4‐(2′‐thienyl)thieno[2,3‐b]pyridines 3a‐e were synthesized by reaction of ethyl 3‐cyano‐1,2‐dihydro‐6‐methyl‐4‐(2′‐thienyl)‐2‐thioxopyridine‐5‐carboxylate (1) with the respective N‐aryl‐2‐chloroacetamides in the presence of different basic catalysts. Compounds 3a‐e were used as precursors for synthesizing of pyridothienopyrimidinones 4a‐e, pyridothienotriazinones 5a‐e and tetrahydropyridothienopyrimidinones 6a‐c via treatment with triethyl orthoformate, nitrous acid, and/or 4‐chlorobenzaldehyde respectively. The photophysical properties of aminothienylthienopyridines 3a‐e and tetrahydropyridothieno‐pyrimidine‐4(3H)‐ones 6a‐c were studied and the fluorescence data revealed that all selected compounds possess AIE behaviors in solution and in solid state. Most of the prepared compounds were evaluated in vitro for their antibacterial and antifungal activities, and considerable results were obtained. Moreover, the cytotoxic activity of thienopyridines 3a‐d against MCF‐7 and HepG2 cell lines was evaluated and they showed moderate to very strong activity.
Polish Journal of Environmental Studies, Feb 21, 2024
![Research paper thumbnail of Selenium Containing Heterocycles: Synthesis and Pharmacological Activities of Some New Selenolo[2,3-b]quinoline Derivatives and Related Pentacyclic Systems](https://attachments.academia-assets.com/112925452/thumbnails/1.jpg)
](Phosphorus Sulfur and Silicon and The Related Elements, Nov 23, 2010
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Phosphorus Sulfur and Silicon and The Related Elements, Mar 1, 2006
... M. Hassan a , RA Ahmed a , Sh. H. Abdel-Hafez a & MA Abdel-Azim a ... Theoritical Fou... more ... M. Hassan a , RA Ahmed a , Sh. H. Abdel-Hafez a & MA Abdel-Azim a ... Theoritical Foundations of Organic Chemistry [Russian Translation], Mir, Moscous , : 831 [CSA] View all references] This conclusion is in good agreement with the data in the literature, [1216. ...
European journal of medicinal chemistry, Sep 1, 2008
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Russian Journal of Bioorganic Chemistry, Jul 1, 2015
Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl... more Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4-[({[3-Mercapto-5-oxo-6-[2-(2-thienyl)vinyl]-1,2,4-triazin-4(5H)-yl]imino}methyl)amino]-benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4-{[({8-Cyano-4-oxo-3-[2-(2-thienyl)vinyl]-4H,8H-[1,2,4]triazino[3,4-b][1,3,4]thiadiazin7-yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonodinitrile and it was unique among other compounds being unable to increase glutathione S-transferase and reduced glutathione S-transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.
Phosphorus Sulfur and Silicon and The Related Elements, Dec 1, 2003
2-Amino-4-(4′-phenylsulfanyl-phenyl)-thiazole (2) has been obtained from reaction of 4-chloroacet... more 2-Amino-4-(4′-phenylsulfanyl-phenyl)-thiazole (2) has been obtained from reaction of 4-chloroacetyl diphenyl sulfide (1) with thiourea. Compound (2) reacted with active methylene derivatives, e.g., diethylmalonate or ethylcyano acetate to give fused thiazolo-pyrimidines (3–6) under variable conditions. Other substituted thiazolo-pyrimidines (7–9) also have been prepared by the reaction of (2) with some arylidine malonitriles (benzylidinemalononitrile and ethylbenzylidinecyano-acetate). On treatment of schiff's bases (10a–c)
Russian Journal of Organic Chemistry, Mar 1, 2005
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Arabian Journal of Geosciences, May 1, 2022
Phosphorus Sulfur and Silicon and The Related Elements, May 1, 2000
4′-Nitro-4-aminodiphenylselenide (1) reacts with chloroacetyl chloride giving 4′-nitro-4-chloroac... more 4′-Nitro-4-aminodiphenylselenide (1) reacts with chloroacetyl chloride giving 4′-nitro-4-chloroacetylaminodiphenylselenide (2) which undergo facile reaction with certain amines and hydrazine yielding 4′-glycylamino and hydrazinoacetylamino-4′-nitrodiphenylse lenides (3) and (5). Two moles of (2) react with one mole of piperazine and/or hydrazine to give 1,4-bis [p-N-(p′-nitro-diphenylselenido)aminocarbonylmethylene] piperazine (4) and 1,2-bis[p-N-(p′-nitro-diphenylselenido)aminocarbonyl-methylene]hydrazine (6). Condensation of (5) with aromatic aldehydes in the presence of glacial acetic acid
Bioorganicheskaya Khimiya, 2015
New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,... more New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.
Molecules, Jul 31, 2003
Condensation of 4,4'-diacetyldiphenyl sulphide (2) with variable amounts of thiosemicarbazide (3)... more Condensation of 4,4'-diacetyldiphenyl sulphide (2) with variable amounts of thiosemicarbazide (3) in refluxing ethanol and in the presence of catalytic amounts of dry piperidine afforded only 4-acetylthiosemicarbazone-4'-acetyldiphenyl sulphide (5). Condensation of 2 with excess semicarbazide hydrochloride (4) in the presence of fused sodium acetate and/or piperidine yielded 4,4'-diacetylsemicarbazone diphenyl sulphide (6), whereas use of equimolar amounts of 2 and 4 afforded 4-acetyl-semicarbazone-4'acetyldiphenyl sulphide (7). 4-Acetylsemicarbazone-4'-acetylthiosemicarbazone diphenyl sulphide (8) was also obtained via two different routes. The effect of tautomeric structure 5d is discussed. 4-(4"-phenyl-∆ 3-thiazoline-2"-acetylazino)-4'-acetyldiphenyl sulphide (9), 4-(5"-carboxyethyl-4"-thiazolidinone-2"-acetylazino)-4'-acetyldiphenyl sulphide (10), 4-(4"-thiazolidinone-2'-acetylazino)-4'-acetyldiphenyl sulphide (11) and 4-(4"-methyl-∆ 3-thiazoline-2"-acetylazino)-4'-acetyldiphenyl sulphide (12) were prepared by interaction of 5 with phenacylbromide, bromodiethylmalonate, chloro ethylacetate and chloroacetone, respectively. Sulphides 9-12 were easily condensed with 3 to afford the corresponding 4-(heterocyclic moiety-2"-acetylazino)-4'-acetylthiosemicarbazone diphenyl sulphides 23-26. Oxidation of the prepared sulphides 5-7, 9-12, 23 and 25-26 using H 2 O 2 /glacial AcOH mixtures yielded only 4,4'-diacetyldiphenyl sulphone (13) as the main product in every case, besides 3 and 4 in certain cases. Unsymmetrical and symmetrical sulphones 14-22 were obtained starting from 13. The structures of the synthesized compounds are based on IR, 1 H-NMR, 13 C-NMR and mass spectral data. A Molecules 2003, 8 623 theoretical study on some of the prepared compounds using molecular modeling was carried out.
Phosphorus Sulfur and Silicon and The Related Elements, Jul 30, 2010
... H. Abdel-Hafez a & M.-AM Abou-Omar a pages 1708-1725. ... H 2 SO 4 , while compound 10b g... more ... H. Abdel-Hafez a & M.-AM Abou-Omar a pages 1708-1725. ... H 2 SO 4 , while compound 10b gave a blue color, which could be interpreted via inspection of the charged contributing resonance structure of 10b), 23 27. Dudley, KH and Miller, HW 1968. Tetrahedron Lett. ...
Phosphorus Sulfur and Silicon and The Related Elements, Nov 2, 2015
GRAPHICAL ABSTRACT Abstract 4,4′-Dimonochloroacetyl diphenylselenide (2) was prepared as a new pr... more GRAPHICAL ABSTRACT Abstract 4,4′-Dimonochloroacetyl diphenylselenide (2) was prepared as a new precursor for the title studies by chloroacetylation of diphenylselenide (1). 2 interacts with thiourea to afford 4,4′-di(2″-aminothiazol-4″-yl)diphenylselenide (3). Condensation of 3 with aromatic aldehydes in the presence of a catalytic amount of dry piperidine furnished aldimines (4). Interaction of 4 with mercaptoacetic acid afforded 4,4′-di(2″-(2‴-substituted phenyl-3‴-thiazolo-4‴-thiazolidinon)-3‴-yl)diphenylselenides (6). Schiff bases 4 interact with mono chloroacetyl chloride in dry dioxane and triethylamine produced 4,4′-di(2″-(4‴-substituted phenyl-3‴-chloro-2‴-azetidinon-1‴-thiazolo)-1‴-yl)diphenylselenides (8). 1,3-Dipolar cyclonucleophilic addition of diazomethane to certain of 4 gave 4,4′-di(2″-(5‴-substituted phenyl-Δ2-1‴,2‴,3‴-triazoline thiazolo)-1‴-yl)diphenylselenides (10). 2 interacts with secondary heteroalicyclic amines to afford 4,4′-diglycyl diphenylselenides (11). The structures of the synthesized compounds are based on correct physical data, IR, 1H NMR, 13C NMR, and by chemical means. Some of the synthesized compounds were biologically tested.
![Research paper thumbnail of Synthesis and reactions of some new selenolo[2,3-c]pyridazines](https://attachments.academia-assets.com/110002234/thumbnails/1.jpg)
](Chemistry of Heterocyclic Compounds, Jun 1, 2011
Bioorganicheskaya Khimiya, 2015
ABSTRACT Thienyl−triazine−sulphonamide conjugates were prepared from their precursor amines using... more ABSTRACT Thienyl−triazine−sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4�[({[3�Mercapto�5�oxo�6�[2�(2�thienyl)vinyl]�1,2,4�triazin� 4(5H)�yl]imino}methyl)amino]�benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4�{[({8�Cyano�4�oxo�3�[2�(2�thienyl)vinyl]� 4H,8H�[1,2,4]triazino[3,4�b][1,3,4]thiadiazin�7�yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonod� initrile and it was unique among other compounds being unable to increase glutathione S�transferase and reduced glutathione S�transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.
A novel folate conjugated to α-tocopherol (VAF) via peptide bond was Successfully synthesized by ... more A novel folate conjugated to α-tocopherol (VAF) via peptide bond was Successfully synthesized by using three components vitamin e (α-tocopherol), chloro acetamide and folic acid under mild and simple conditions. The new synthesized compound was characterized by proton nuclear magnetic resonance 1H NMR, 13H NMR and Fourier transform infrared (FT-IR) analysis. A molecular docking study for targeted compound (VAF ) was performed and showed growth-inhibitory activity towards the human folate receptor alpha (FRα) that may affectively the folate uptake by cancer cells. Further, The predicted pharmacokinetic properties and toxicity of the compound (VAF) and folic acid (F) were determined using a statistical analysis (ADMET). It was suggested that pharmacokinetic properties of compound (VAF) represents a promising drug and used as anticancer agents.
Drought stress is among the major constraints that threat agricultural productivity within the ar... more Drought stress is among the major constraints that threat agricultural productivity within the arid and semi-arid regions, worldwide. In this study, wheat (a strategic crop) was selected to test its growth under drought stress and the mechanisms beyond this adaptation while considering two factors, i.e., (1) deficit irrigation at 35% of the water holding capacity (WHC) versus 75% of WHC (Factor A) and (2) the following safe treatments: the control treatment (C), amending soil with biochar (BC) at a rate of 2%, foliar application of 24-epibrassinolide at two different levels (1 (BR1) or 3 (BR2) μmol) and the combination between BC and BR treatments. The obtained results were statistically analyzed, and the heat-map conceits between measured variables were also calculated by using the Python software. This investigation took place under the greenhouse conditions for 35 days following a complete randomized design and all treatments were replicated trice. Results obtained herein reveale...
Биоорганическая химия, 2015
New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,... more New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.
Phosphorus, Sulfur, and Silicon and the Related Elements, 2006
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Journal of Heterocyclic Chemistry, Nov 21, 2022
Both 2‐(N‐arylcarbamoyl)methylsulfanyl‐3‐cyano‐5‐ethoxycarbonyl‐6‐methyl‐4‐(2′‐thienyl)pyridines ... more Both 2‐(N‐arylcarbamoyl)methylsulfanyl‐3‐cyano‐5‐ethoxycarbonyl‐6‐methyl‐4‐(2′‐thienyl)pyridines 2a‐e and their isomers, 3‐amino‐2‐(N‐arylcarbamoyl)‐5‐ethoxy‐carbonyl‐6‐methyl‐4‐(2′‐thienyl)thieno[2,3‐b]pyridines 3a‐e were synthesized by reaction of ethyl 3‐cyano‐1,2‐dihydro‐6‐methyl‐4‐(2′‐thienyl)‐2‐thioxopyridine‐5‐carboxylate (1) with the respective N‐aryl‐2‐chloroacetamides in the presence of different basic catalysts. Compounds 3a‐e were used as precursors for synthesizing of pyridothienopyrimidinones 4a‐e, pyridothienotriazinones 5a‐e and tetrahydropyridothienopyrimidinones 6a‐c via treatment with triethyl orthoformate, nitrous acid, and/or 4‐chlorobenzaldehyde respectively. The photophysical properties of aminothienylthienopyridines 3a‐e and tetrahydropyridothieno‐pyrimidine‐4(3H)‐ones 6a‐c were studied and the fluorescence data revealed that all selected compounds possess AIE behaviors in solution and in solid state. Most of the prepared compounds were evaluated in vitro for their antibacterial and antifungal activities, and considerable results were obtained. Moreover, the cytotoxic activity of thienopyridines 3a‐d against MCF‐7 and HepG2 cell lines was evaluated and they showed moderate to very strong activity.
Polish Journal of Environmental Studies, Feb 21, 2024
Phosphorus Sulfur and Silicon and The Related Elements, Nov 23, 2010
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Phosphorus Sulfur and Silicon and The Related Elements, Mar 1, 2006
... M. Hassan a , RA Ahmed a , Sh. H. Abdel-Hafez a & MA Abdel-Azim a ... Theoritical Fou... more ... M. Hassan a , RA Ahmed a , Sh. H. Abdel-Hafez a & MA Abdel-Azim a ... Theoritical Foundations of Organic Chemistry [Russian Translation], Mir, Moscous , : 831 [CSA] View all references] This conclusion is in good agreement with the data in the literature, [1216. ...
European journal of medicinal chemistry, Sep 1, 2008
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Russian Journal of Bioorganic Chemistry, Jul 1, 2015
Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl... more Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4-[({[3-Mercapto-5-oxo-6-[2-(2-thienyl)vinyl]-1,2,4-triazin-4(5H)-yl]imino}methyl)amino]-benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4-{[({8-Cyano-4-oxo-3-[2-(2-thienyl)vinyl]-4H,8H-[1,2,4]triazino[3,4-b][1,3,4]thiadiazin7-yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonodinitrile and it was unique among other compounds being unable to increase glutathione S-transferase and reduced glutathione S-transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.
Phosphorus Sulfur and Silicon and The Related Elements, Dec 1, 2003
2-Amino-4-(4′-phenylsulfanyl-phenyl)-thiazole (2) has been obtained from reaction of 4-chloroacet... more 2-Amino-4-(4′-phenylsulfanyl-phenyl)-thiazole (2) has been obtained from reaction of 4-chloroacetyl diphenyl sulfide (1) with thiourea. Compound (2) reacted with active methylene derivatives, e.g., diethylmalonate or ethylcyano acetate to give fused thiazolo-pyrimidines (3–6) under variable conditions. Other substituted thiazolo-pyrimidines (7–9) also have been prepared by the reaction of (2) with some arylidine malonitriles (benzylidinemalononitrile and ethylbenzylidinecyano-acetate). On treatment of schiff's bases (10a–c)
Russian Journal of Organic Chemistry, Mar 1, 2005
Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared ... more Several selenolo[2,3-b]quinolines and pyrimido[49,59:4,5]selenolo[2,3-b]quinolines were prepared by annulations via reaction of NaSeH with 2-chloro-3-cyano-4-methylquinoline 1 followed by reactions with aromatic aldehydes, cycloalkanones, and acetic anhydride. Spectroscopic (IR, 1 H-NMR, and MS) properties of the synthesized compounds are reported. Some selected compounds 5a, 7b, 7c, 8b-d, 9a, 11b, and 11d were investigated for their anti-inflammatory and analgesic activities; in addition, the most active compounds were tested for their ulcerogenicity and acute toxicity. Moreover, some of the test compounds 7c, 9a, 11b, and 11d were screened for their antibacterial and antifungal activities.
Arabian Journal of Geosciences, May 1, 2022
Phosphorus Sulfur and Silicon and The Related Elements, May 1, 2000
4′-Nitro-4-aminodiphenylselenide (1) reacts with chloroacetyl chloride giving 4′-nitro-4-chloroac... more 4′-Nitro-4-aminodiphenylselenide (1) reacts with chloroacetyl chloride giving 4′-nitro-4-chloroacetylaminodiphenylselenide (2) which undergo facile reaction with certain amines and hydrazine yielding 4′-glycylamino and hydrazinoacetylamino-4′-nitrodiphenylse lenides (3) and (5). Two moles of (2) react with one mole of piperazine and/or hydrazine to give 1,4-bis [p-N-(p′-nitro-diphenylselenido)aminocarbonylmethylene] piperazine (4) and 1,2-bis[p-N-(p′-nitro-diphenylselenido)aminocarbonyl-methylene]hydrazine (6). Condensation of (5) with aromatic aldehydes in the presence of glacial acetic acid
Bioorganicheskaya Khimiya, 2015
New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,... more New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.
Molecules, Jul 31, 2003
Condensation of 4,4'-diacetyldiphenyl sulphide (2) with variable amounts of thiosemicarbazide (3)... more Condensation of 4,4'-diacetyldiphenyl sulphide (2) with variable amounts of thiosemicarbazide (3) in refluxing ethanol and in the presence of catalytic amounts of dry piperidine afforded only 4-acetylthiosemicarbazone-4'-acetyldiphenyl sulphide (5). Condensation of 2 with excess semicarbazide hydrochloride (4) in the presence of fused sodium acetate and/or piperidine yielded 4,4'-diacetylsemicarbazone diphenyl sulphide (6), whereas use of equimolar amounts of 2 and 4 afforded 4-acetyl-semicarbazone-4'acetyldiphenyl sulphide (7). 4-Acetylsemicarbazone-4'-acetylthiosemicarbazone diphenyl sulphide (8) was also obtained via two different routes. The effect of tautomeric structure 5d is discussed. 4-(4"-phenyl-∆ 3-thiazoline-2"-acetylazino)-4'-acetyldiphenyl sulphide (9), 4-(5"-carboxyethyl-4"-thiazolidinone-2"-acetylazino)-4'-acetyldiphenyl sulphide (10), 4-(4"-thiazolidinone-2'-acetylazino)-4'-acetyldiphenyl sulphide (11) and 4-(4"-methyl-∆ 3-thiazoline-2"-acetylazino)-4'-acetyldiphenyl sulphide (12) were prepared by interaction of 5 with phenacylbromide, bromodiethylmalonate, chloro ethylacetate and chloroacetone, respectively. Sulphides 9-12 were easily condensed with 3 to afford the corresponding 4-(heterocyclic moiety-2"-acetylazino)-4'-acetylthiosemicarbazone diphenyl sulphides 23-26. Oxidation of the prepared sulphides 5-7, 9-12, 23 and 25-26 using H 2 O 2 /glacial AcOH mixtures yielded only 4,4'-diacetyldiphenyl sulphone (13) as the main product in every case, besides 3 and 4 in certain cases. Unsymmetrical and symmetrical sulphones 14-22 were obtained starting from 13. The structures of the synthesized compounds are based on IR, 1 H-NMR, 13 C-NMR and mass spectral data. A Molecules 2003, 8 623 theoretical study on some of the prepared compounds using molecular modeling was carried out.
Phosphorus Sulfur and Silicon and The Related Elements, Jul 30, 2010
... H. Abdel-Hafez a & M.-AM Abou-Omar a pages 1708-1725. ... H 2 SO 4 , while compound 10b g... more ... H. Abdel-Hafez a & M.-AM Abou-Omar a pages 1708-1725. ... H 2 SO 4 , while compound 10b gave a blue color, which could be interpreted via inspection of the charged contributing resonance structure of 10b), 23 27. Dudley, KH and Miller, HW 1968. Tetrahedron Lett. ...
Phosphorus Sulfur and Silicon and The Related Elements, Nov 2, 2015
GRAPHICAL ABSTRACT Abstract 4,4′-Dimonochloroacetyl diphenylselenide (2) was prepared as a new pr... more GRAPHICAL ABSTRACT Abstract 4,4′-Dimonochloroacetyl diphenylselenide (2) was prepared as a new precursor for the title studies by chloroacetylation of diphenylselenide (1). 2 interacts with thiourea to afford 4,4′-di(2″-aminothiazol-4″-yl)diphenylselenide (3). Condensation of 3 with aromatic aldehydes in the presence of a catalytic amount of dry piperidine furnished aldimines (4). Interaction of 4 with mercaptoacetic acid afforded 4,4′-di(2″-(2‴-substituted phenyl-3‴-thiazolo-4‴-thiazolidinon)-3‴-yl)diphenylselenides (6). Schiff bases 4 interact with mono chloroacetyl chloride in dry dioxane and triethylamine produced 4,4′-di(2″-(4‴-substituted phenyl-3‴-chloro-2‴-azetidinon-1‴-thiazolo)-1‴-yl)diphenylselenides (8). 1,3-Dipolar cyclonucleophilic addition of diazomethane to certain of 4 gave 4,4′-di(2″-(5‴-substituted phenyl-Δ2-1‴,2‴,3‴-triazoline thiazolo)-1‴-yl)diphenylselenides (10). 2 interacts with secondary heteroalicyclic amines to afford 4,4′-diglycyl diphenylselenides (11). The structures of the synthesized compounds are based on correct physical data, IR, 1H NMR, 13C NMR, and by chemical means. Some of the synthesized compounds were biologically tested.
Chemistry of Heterocyclic Compounds, Jun 1, 2011
Bioorganicheskaya Khimiya, 2015
ABSTRACT Thienyl−triazine−sulphonamide conjugates were prepared from their precursor amines using... more ABSTRACT Thienyl−triazine−sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4�[({[3�Mercapto�5�oxo�6�[2�(2�thienyl)vinyl]�1,2,4�triazin� 4(5H)�yl]imino}methyl)amino]�benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4�{[({8�Cyano�4�oxo�3�[2�(2�thienyl)vinyl]� 4H,8H�[1,2,4]triazino[3,4�b][1,3,4]thiadiazin�7�yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonod� initrile and it was unique among other compounds being unable to increase glutathione S�transferase and reduced glutathione S�transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.
A novel folate conjugated to α-tocopherol (VAF) via peptide bond was Successfully synthesized by ... more A novel folate conjugated to α-tocopherol (VAF) via peptide bond was Successfully synthesized by using three components vitamin e (α-tocopherol), chloro acetamide and folic acid under mild and simple conditions. The new synthesized compound was characterized by proton nuclear magnetic resonance 1H NMR, 13H NMR and Fourier transform infrared (FT-IR) analysis. A molecular docking study for targeted compound (VAF ) was performed and showed growth-inhibitory activity towards the human folate receptor alpha (FRα) that may affectively the folate uptake by cancer cells. Further, The predicted pharmacokinetic properties and toxicity of the compound (VAF) and folic acid (F) were determined using a statistical analysis (ADMET). It was suggested that pharmacokinetic properties of compound (VAF) represents a promising drug and used as anticancer agents.
Drought stress is among the major constraints that threat agricultural productivity within the ar... more Drought stress is among the major constraints that threat agricultural productivity within the arid and semi-arid regions, worldwide. In this study, wheat (a strategic crop) was selected to test its growth under drought stress and the mechanisms beyond this adaptation while considering two factors, i.e., (1) deficit irrigation at 35% of the water holding capacity (WHC) versus 75% of WHC (Factor A) and (2) the following safe treatments: the control treatment (C), amending soil with biochar (BC) at a rate of 2%, foliar application of 24-epibrassinolide at two different levels (1 (BR1) or 3 (BR2) μmol) and the combination between BC and BR treatments. The obtained results were statistically analyzed, and the heat-map conceits between measured variables were also calculated by using the Python software. This investigation took place under the greenhouse conditions for 35 days following a complete randomized design and all treatments were replicated trice. Results obtained herein reveale...
Биоорганическая химия, 2015
New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,... more New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.
Phosphorus, Sulfur, and Silicon and the Related Elements, 2006
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.