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Research paper thumbnail of Synthesis of Certain 2-AROYLINDOLE Derivatives of Potential Analgesic, Anti-Inflammatory and Antipyretic Activities

Bulletin of Pharmaceutical Sciences. Assiut, 2005

In the present study, a series of 2-aroylindole derivatives were synthesized by phase transfer ca... more In the present study, a series of 2-aroylindole derivatives were synthesized by phase transfer catalysis (PTC) and were characterized by IR, 1 H-NMR, Mass spectral and Elemental analysis. Indole derivatives 6a-g, 7a-f, 8a-f and 9a-13a were tested for analgesic activity using hot-plate test. Compounds 7b and 8b were tested for antipyretic and anti-inflammatory activity using yeast induced hyperthermia and paw edema in rats. Analgesic activity was shown when indole nucleus was substituted at position 2 and 3 by phenyl and (p-halo)benzoyl moieties respectively, where highest activity was recognised in compounds 7b and 8b. Both compounds also exhibited faster, more effective and prolonged reduction in hyperthermia and edema induced in rats compared with indomethacin. Compounds 7b and 8b were also tested for ulcerogenic activity in mice, where a lower ulcerogenic effect was observed compared with indomethacin at all tested dose levels.

Research paper thumbnail of Synthesis and Biological Evaluation of Some BENZIMIDAZO-1,2,4-TRIAZOLE Derivatives as Antimicrobial and Anti-Inflammatory Agents

Bulletin of Pharmaceutical Sciences. Assiut, 2011

Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3a]benzimidazol-2-y... more Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3a]benzimidazol-2-ylsulfanyl) acetohydrazides (4a-k), N`-(α-arylethylidene)-2-(1H-1,2,4triazolo[2,3-a]benzimidazol-2-ylsulfanyl) acetohydrazides (5a-d), and 2-({[5-(alkyl or aralkylsulfanyl)-1,3,4-oxadiazol-2-yl]methyl}sulfanyl)-1H-1,2,4-triazolo[2,3-a]benzimidazoles (7a-e) were synthesized. Reaction of compound (1) with methyl bromoacetate afforded (2), which when refluxed with hydrazine hydrate yielded (3). The latter was condensed with aromatic aldehydes and substituted acetophenones to afford compounds (4a-k) and (5a-d) respectively. Treatment of compound (3) with carbon disulfide in the presence of potassium hydroxide resulted in the formation of (6). The latter was alkylated with the appropriate alkyl or aralkyl halides to afford compounds (7a-e). The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1 HNMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their in-vitro antimicrobial and in-vivo anti-inflammatory activities in comparison with ampicillin, fluconazole, and indomethacin as reference drugs respectively. In addition to molecular docking of compound 5c was performed. * Compound 4a was purified by column chromatography (Silica gel 60, Fluka, Switzerland), using Chloroform : methanol (9.5:0.5) as a mobile phase.

Research paper thumbnail of Synthesis of New 1,2,4-TRI Nalidixic Acid as Potenti and Antifungal Agents

Research paper thumbnail of Design, synthesis and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetohydrazide derivatives with anti-inflammatory-analgesic activities

Archives of Pharmacal Research, 2013

A computationally efficient mode space simulation method for atomistic simulation of a graphene n... more A computationally efficient mode space simulation method for atomistic simulation of a graphene nanoribbon field-effect transistor in the ballistic limits is developed. The proposed simulation scheme, which solves the nonequilibrium Green's function coupled with a three dimensional Poisson equation, is based on the atomistic Hamiltonian in a decoupled mode space. The mode space approach, which only treats a few modes (subbands), significantly reduces the simulation time. Additionally, the edge bond relaxation and the third nearest neighbor effects are also included in the quantum transport solver. Simulation examples show that, mode space approach can significantly decrease the simulation cost by about an order of magnitude, yet the results are still accurate. This article also demonstrates that the effects of edge bond relaxation and third nearest neighbor significantly influence the transistor's performance and are necessary to be included in the modeling.

Research paper thumbnail of Synthesis and biological activities of new substituted thiazoline-quinoline derivatives

Research paper thumbnail of Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

JOURNAL OF ADVANCES IN CHEMISTRY, 2015

The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines... more The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.

Research paper thumbnail of Synthesis of New 1,2,4-TRIAZOLE Derivatives of Nalidixic Acid as Potential Antibacterial and Antifungal Agents

Bulletin of Pharmaceutical Sciences. Assiut

refluxing with hydrazine hydrate. Condensation of the key intermediate 4 with aryl aldehydes affo... more refluxing with hydrazine hydrate. Condensation of the key intermediate 4 with aryl aldehydes afforded Schiff's bases 5a-f, while its reaction with alkyl or aralkyl halides gave compounds 6a-e. Furthermore, compounds 5a,e were reacted with benzyl chloride to afford 7a,b. The chemical structure of the target compounds was confirmed by IR, 1 H-NMR, FAB-MS, EI-MS spectra and elemental analyses. The title compounds and the starting Nalidixic acid; were tested for their in-vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable antibacterial activity with those of Nalidixic acid and higher activity than ampicillin. The tested compounds and Nalidixic acid showed non or moderate antifungal activity in comparison to clotrimazole as a reference drug.

Research paper thumbnail of المنهج النبوي في تأسيس السلم المدني في الحروب والنزاعات الأهلية

المجلة الأردنية في الدراسات الإسلامية, 2018

ملخَّص الإسلام دين العدل والسَّلام، ودِيْن المحبَّة والبِناء، لا دِيْن التنازع والفَناء، يدعو إلى... more ملخَّص الإسلام دين العدل والسَّلام، ودِيْن المحبَّة والبِناء، لا دِيْن التنازع والفَناء، يدعو إلى نَشْر السَّلام والأمَان للجميع، والسِّلم المدني (ماديَّاً ومعنوياً) من مقاصد الإسلام العليا التي تتظافر وتتمظهر في سُلَّمِ المقاصد والضَّرورات، وإنَّ دراسة الأوامر النبوية في الحروب والنزاعات الأهلية لها أهداف سامية ومهمة تكمن في بيان جوهر وسموِّ الإسلام في حالة الحروب والنزاع (قبل النزاع إلى نهايته وآثاره)، وجاء هذا البحث ليقف على بيان المنهج النبوي وأوامره قبل النزاعات والحروب وخلالها وما بعدها، بحيث أسلِّط الضوء على تلك الأوامر النبوية من خلال المنهج الوصفي التحليلي، مستخلصاً أهمَّ النتائج التي تظهر لنا أنَّ السلم المدني والسلام ضرورة في سُلَّم المقاصد الشرعية التي راعتها الشريعة الإسلامية، حيث كان للنبي  قصب السبق في تقعيد كثير من المواثيق الحقوقية في المنازعات والحروب، كمعاهدات الصلح، وحقوق الإنسان والمدنيين وحق البيئة المستدامة خلال الحروب والنزاعات. كلمات مفتاحية: المنهج النبوي في السلم، السِّلْم المدني في السنة، الإسلام وحماية المدنيين. Abstract Islam is the religion of justice...

Research paper thumbnail of Synthesis of Certain 2-AROYLINDOLE Derivatives of Potential Analgesic, Anti-Inflammatory and Antipyretic Activities

Bulletin of Pharmaceutical Sciences. Assiut, 2005

In the present study, a series of 2-aroylindole derivatives were synthesized by phase transfer ca... more In the present study, a series of 2-aroylindole derivatives were synthesized by phase transfer catalysis (PTC) and were characterized by IR, 1 H-NMR, Mass spectral and Elemental analysis. Indole derivatives 6a-g, 7a-f, 8a-f and 9a-13a were tested for analgesic activity using hot-plate test. Compounds 7b and 8b were tested for antipyretic and anti-inflammatory activity using yeast induced hyperthermia and paw edema in rats. Analgesic activity was shown when indole nucleus was substituted at position 2 and 3 by phenyl and (p-halo)benzoyl moieties respectively, where highest activity was recognised in compounds 7b and 8b. Both compounds also exhibited faster, more effective and prolonged reduction in hyperthermia and edema induced in rats compared with indomethacin. Compounds 7b and 8b were also tested for ulcerogenic activity in mice, where a lower ulcerogenic effect was observed compared with indomethacin at all tested dose levels.

Research paper thumbnail of Synthesis and Biological Evaluation of Some BENZIMIDAZO-1,2,4-TRIAZOLE Derivatives as Antimicrobial and Anti-Inflammatory Agents

Bulletin of Pharmaceutical Sciences. Assiut, 2011

Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3a]benzimidazol-2-y... more Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3a]benzimidazol-2-ylsulfanyl) acetohydrazides (4a-k), N`-(α-arylethylidene)-2-(1H-1,2,4triazolo[2,3-a]benzimidazol-2-ylsulfanyl) acetohydrazides (5a-d), and 2-({[5-(alkyl or aralkylsulfanyl)-1,3,4-oxadiazol-2-yl]methyl}sulfanyl)-1H-1,2,4-triazolo[2,3-a]benzimidazoles (7a-e) were synthesized. Reaction of compound (1) with methyl bromoacetate afforded (2), which when refluxed with hydrazine hydrate yielded (3). The latter was condensed with aromatic aldehydes and substituted acetophenones to afford compounds (4a-k) and (5a-d) respectively. Treatment of compound (3) with carbon disulfide in the presence of potassium hydroxide resulted in the formation of (6). The latter was alkylated with the appropriate alkyl or aralkyl halides to afford compounds (7a-e). The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1 HNMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their in-vitro antimicrobial and in-vivo anti-inflammatory activities in comparison with ampicillin, fluconazole, and indomethacin as reference drugs respectively. In addition to molecular docking of compound 5c was performed. * Compound 4a was purified by column chromatography (Silica gel 60, Fluka, Switzerland), using Chloroform : methanol (9.5:0.5) as a mobile phase.

Research paper thumbnail of Synthesis of New 1,2,4-TRI Nalidixic Acid as Potenti and Antifungal Agents

Research paper thumbnail of Design, synthesis and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetohydrazide derivatives with anti-inflammatory-analgesic activities

Archives of Pharmacal Research, 2013

A computationally efficient mode space simulation method for atomistic simulation of a graphene n... more A computationally efficient mode space simulation method for atomistic simulation of a graphene nanoribbon field-effect transistor in the ballistic limits is developed. The proposed simulation scheme, which solves the nonequilibrium Green's function coupled with a three dimensional Poisson equation, is based on the atomistic Hamiltonian in a decoupled mode space. The mode space approach, which only treats a few modes (subbands), significantly reduces the simulation time. Additionally, the edge bond relaxation and the third nearest neighbor effects are also included in the quantum transport solver. Simulation examples show that, mode space approach can significantly decrease the simulation cost by about an order of magnitude, yet the results are still accurate. This article also demonstrates that the effects of edge bond relaxation and third nearest neighbor significantly influence the transistor's performance and are necessary to be included in the modeling.

Research paper thumbnail of Synthesis and biological activities of new substituted thiazoline-quinoline derivatives

Research paper thumbnail of Synthesis, anti-inflammatory and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetone thiosemicarbazone cyclized derivatives as PLA-2 inhibitors

JOURNAL OF ADVANCES IN CHEMISTRY, 2015

The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines... more The present work is carried out for the synthesis and evaluation of some new 1,3,4-thiadiazolines, 1,3-thiazolines and 1,3-thiazolidin-4-ones linked to 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflammatory agents. Structure elucidation of these compounds was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All new compounds were tested for their anti-inflammatory activity in comparison to indomethacin (INM) where some of them showed promising results comparable to INM at 4 hours interval. The most active anti-inflammatory compounds (4b, 8c and 9a) were examined on gastric mucosa and didn’t show any gastric ulcerogenic effect compared with the reference INM. Moreover, LD50 of compounds (4b and 9a) were determined in mice; they were found non toxic up to 400 mg Kg–1 (i.p.). Also, docking simulation of some compounds into PLA2 active sites was studied.

Research paper thumbnail of Synthesis of New 1,2,4-TRIAZOLE Derivatives of Nalidixic Acid as Potential Antibacterial and Antifungal Agents

Bulletin of Pharmaceutical Sciences. Assiut

refluxing with hydrazine hydrate. Condensation of the key intermediate 4 with aryl aldehydes affo... more refluxing with hydrazine hydrate. Condensation of the key intermediate 4 with aryl aldehydes afforded Schiff's bases 5a-f, while its reaction with alkyl or aralkyl halides gave compounds 6a-e. Furthermore, compounds 5a,e were reacted with benzyl chloride to afford 7a,b. The chemical structure of the target compounds was confirmed by IR, 1 H-NMR, FAB-MS, EI-MS spectra and elemental analyses. The title compounds and the starting Nalidixic acid; were tested for their in-vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable antibacterial activity with those of Nalidixic acid and higher activity than ampicillin. The tested compounds and Nalidixic acid showed non or moderate antifungal activity in comparison to clotrimazole as a reference drug.

Research paper thumbnail of المنهج النبوي في تأسيس السلم المدني في الحروب والنزاعات الأهلية

المجلة الأردنية في الدراسات الإسلامية, 2018

ملخَّص الإسلام دين العدل والسَّلام، ودِيْن المحبَّة والبِناء، لا دِيْن التنازع والفَناء، يدعو إلى... more ملخَّص الإسلام دين العدل والسَّلام، ودِيْن المحبَّة والبِناء، لا دِيْن التنازع والفَناء، يدعو إلى نَشْر السَّلام والأمَان للجميع، والسِّلم المدني (ماديَّاً ومعنوياً) من مقاصد الإسلام العليا التي تتظافر وتتمظهر في سُلَّمِ المقاصد والضَّرورات، وإنَّ دراسة الأوامر النبوية في الحروب والنزاعات الأهلية لها أهداف سامية ومهمة تكمن في بيان جوهر وسموِّ الإسلام في حالة الحروب والنزاع (قبل النزاع إلى نهايته وآثاره)، وجاء هذا البحث ليقف على بيان المنهج النبوي وأوامره قبل النزاعات والحروب وخلالها وما بعدها، بحيث أسلِّط الضوء على تلك الأوامر النبوية من خلال المنهج الوصفي التحليلي، مستخلصاً أهمَّ النتائج التي تظهر لنا أنَّ السلم المدني والسلام ضرورة في سُلَّم المقاصد الشرعية التي راعتها الشريعة الإسلامية، حيث كان للنبي  قصب السبق في تقعيد كثير من المواثيق الحقوقية في المنازعات والحروب، كمعاهدات الصلح، وحقوق الإنسان والمدنيين وحق البيئة المستدامة خلال الحروب والنزاعات. كلمات مفتاحية: المنهج النبوي في السلم، السِّلْم المدني في السنة، الإسلام وحماية المدنيين. Abstract Islam is the religion of justice...