Synthesis and characterization of Novel 2-sulfanyl-N-(1,3,4-thiadiazol-2-yl)acetamide derivatives (original) (raw)
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Objective: The objective of the paper is synthesis and characterization of sulfonamide-thiazole derived acetamide derivatives and evaluated for them for the anticancer potential. Material and methods: The sulfonamide-thiazole derived acetamide derivatives has been prepared by the two step process, in first step, 2-chloro-N-(4-((2,3-dihydro-4H-1,4-oxazin-4-yl)sulfonyl)phenyl) acetamide (Compound 2) was synthesized, and in step 2, N-(4-((2,3-dihydro-4H-1,4-oxazin-4-yl)sulfonyl)phenyl)-2-((4-substitutedthiazol-2yl)amino)acet-amide (Compound 3) was synthesized by the reaction of synthesized compound 2 with different 4substituted thiazol-2-amine to from the final compounds (compound 3). Total eleven compounds have been synthesized and characterized by physicochemical and IR, NMR and MASS spectral analysis. The final compounds (SA-1 to SA-11) have been evaluated for anticancer activity by SRB assay method.
Synthesis and antibacterial activity study of some new 1,3,4-thiadiazolederivatives
2016
Six substituted N-aryl,5-substituted phenyl 1,3,4-thiadiazole(7a-f) were synthesized by the reaction of different substituted benzaldehyde with different substituted 5-phenyl 1,3,4-thiadiazole 2-amino in the presence of sulphuric acid in refluxing methanol. The newly synthesized compounds were characterized by spectroscopic methods. Further, the synthesized compounds were screened for antibacterial and antifungal activity by standard method. Results of the activities reveal that some compounds exhibited moderate to good antimicrobial activity.
SYNTHESIS AND CHARACTERIZATION OF NEW 2, 5-DISUBSTITUTED-1, 3, 4- THIADIAZOLE DERIVATIVES
In this study, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many cyclization reactions. Starting from (2, 5 – dimercapto-1, 3, 4-Thiadiazole) a variety of compounds have been synthesized.Derivative (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide. The derivative (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the derivative (2). The derivative (3) was obtainedfrom the reaction of derivative (2) with hydrazine hydrate. Schiff base (4) was formation by reacting of derivative(3) with p-Hydroxybenzaldehyde. From phenolic Schiff base (4), Methylolicderivative (5)has been prepared. Etheric derivative (6) was synthesized by the reaction ofMethylolicderivative withsaturated alcohol.Derivative (7)was synthesized by the reaction ofEthericderivative (6)withEpichlorohydrine. The last step of this study was the preparation of aderivative (8) by reacting of derivative(7) withmorpholine via ring opening.All these derivatives were verified by using (FT-IR, UV) spectra photometer, 1 H-NMR spectra and elemental analysis (C.H.N.S).
Ulcers are not usually life threatening, however they can cause serious damage which may leads to cancer if untreated. In the present study with the intension of enhancing the array of therapeutic ammonites to treat ulcer a series of thiazolidinone derivatives (4a-4f) were synthesized from substituted Schiff bases with thioglycolic acid in presence of anhydrous zinc chloride. The structures of these synthesized compounds have been characterized on the basis of physical constants, spectral data and evaluated them for their possible antiulcer activity using ethanol induced gastric lesion model. All the compounds studied showed significant antiulcer activity against ethanol induced gastric ulcers. Lansoprazole was used as a standard drug for comparison and the Compound 4f protected animals from ethanol induced ulcers at the dose of 300 mg/kg, which is comparable to that of standard drug lansoprazole (300 mg/kg).
Iranian Journal of Pharmaceutical Research : IJPR, 2013
Cancer is the second leading cause of death in the world. Despite advances in the diagnosis and treatment, overall survival of patients still remains poor. Hence, there is an urgent need for development of new anticancer agents. Considering promising biological activity of 1,3,4-thiadiazole derivatives, in the present study, synthesis and cytotoxicity assessment of new derivatives of this ring was done. All synthesized compounds were characterized by NMR, IR and MS spectroscopic methods. Obtained data from MTT assay showed that all compounds 3a- 3l had better anticancer activity against MDA(breast cancer) compared to PC3(prostate cancer) and U87(Glioblastoma). Compound 3 g with m-OCH3 moiety on the phenyl ring was the most potent one in this series with IC50 = 9 μM against MDA breast cell line in comparison with imatinib (IC50 = 20 μM) as reference drug.
2018
Recently in our laboratory a novel synthesis of 2-Amino-5-Substituted-1,3,4-thiadiazoles synthesis was successfully carried out by condensation of aryl acid with thiosemicarbazide in presence of POCl3 by using 'green chemistry' approach. The reactions are simple one step reactions. The purity of synthesized compound and its derivatives was justified by Thin Layer Chromatography. The conformation of structure was done as usual by chemical characteristics, elemental analysis and spectral studies. IR spectra was recorded on FT-IR SHIMADAZU, and X-ray Diffraction by RIGAKUMINIFLEXII, The synthesized compounds were tested for their antimicrobial activity against three microorganisms namely E-coli, S. Aureus and P.seudomonas, and the minimum inhibitory concentrations (MICs) of the tested compounds were determined by the dilution method using Ampicillin, Chloramphenicol, Tetracycline.