- Synthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents
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To search for potent antimycobacterial lead compounds, a new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one (5a-t) derivatives have been synthesized by the condensation of 2-substituted phenyl thiazole-4-carbaldehy
- Abhale, Yogita K.,Shinde, Abhijit,Shelke, Monika,Nawale, Laxman,Sarkar, Dhiman,Mhaske, Pravin C.
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- PROCESS FOR PREPARING A POTENT THIAZOLE COMPOUND, PHARMACEUTICAL FORMULATION AND USES THEREOF
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The present invention relates to a process for preparing N-[2-[2-(4-chlorophenyl)-4- thiazolyl] ethyl]-butanamide. The present invention further relates to a pharmaceutical formulation and the use of said pharmaceutical formulation consisting of N-[2-[2-(
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Page/Page column 14
(2019/11/12)
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- Synthesis, Characterization, and Antimicrobial Screening of 4″-methyl-2,2″-diaryl-4,2′:4′,5″-terthiazole Derivatives
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A series of novel 4″-methyl-2,2″-diaryl-4,2′:4′,5″-terthiazole (8a-p) derivatives has been synthesized and screened for antibacterial activity against four pathogenic bacteria, Escherichia coli, Pseudomonas flurescence, Staphylococcus aureus, and Bacillus subtilis. Among them, compounds 8a and 8j exhibited excellent antibacterial activity with minimum inhibitory concentration range of 1.0 to 5.3?μg/mL and compounds 8m and 8p exhibited moderate to good antibacterial activity with minimum inhibitory concentration range of 16.9 to 29.7?μg/mL against all tested strains. All the synthesized compounds were screened for their in vitro antifungal activity against Cocinida candida. Most of the compounds reported moderate antifungal activity. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimicrobial agent.
- Nalawade, Jitendra,Mhaske, Pravin C.,Shinde, Abhijit,Patil, Sachin V.,Choudhari, Prafulla B.,Bobade, Vivek D.
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p. 1366 - 1374
(2018/04/25)
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- Heterocycles 44. Synthesis, characterization and anticancer activity of new thiazole ortho-hydroxychalcones
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A novel series of substituted thiazole ortho-hydroxychalcones was synthesized to be physico-chemically characterized and evaluated for the anticancer activity. The chalcones were synthesized with 28–68% yields, via Claisen–Schmidt condensation in an ethanolic solution. All the synthesized compounds were purified and characterized by MS, 1H NMR, 13C NMR, IR, and melting points. The cytotoxicity of thiazole ortho-hydroxychalcones 3a–3o as well as doxorubicin was determined in a panel of 9 cancer cell lines including sensitive and drug resistant phenotypes. Compounds 3a, 3b, 3c, 3j, as well as doxorubicin displayed cytotoxic effects in all the 9 tested cancer cell lines with IC50 values below 75 μM. The best samples showed IC50 values below 10 μM against 5/9 cancer cell lines for 3a, 3h, and 3o, against 7/9 cancer cell lines for 3c and 3f, and against 8/9 cancer cell lines for 3j. Hypersensitivity of all resistant cells towards 3b, 3g, 3j, 3m, and 3o was also obtained, suggesting that these compounds are appropriate molecules that could be used to combat drug resistance of cancer cells.
- Coman, Fana-Maria,Mbaveng, Armelle T.,Leonte, Denisa,Bencze, László Csaba,Vlase, Laurian,Imre, Silvia,Kuete, Victor,Efferth, Thomas,Zaharia, Valentin
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p. 1396 - 1407
(2018/03/06)
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- Synthesis, antitubercular and antimicrobial potential of some new thiazole substituted thiosemicarbazide derivatives
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The increase in antibiotic resistance due to multiple factors has warranted the need for search of new compounds which are active against multidrug resistant pathogens. In this context a small focused library of thiosemicarbazide derivatives of 2-arylthiazole-4-carbaldehyde, 4-methyl-2-arylthiazole-5-carbaldehyde and 1-(4-methyl-2-arylthiazol-5-yl) ethanone, (5a–l) has been synthesized. The title compounds were screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis Bacille Calmette Guerin (ATCC 35743) strains. The synthesized compounds, 5a–l were further assayed for their cytotoxic activity against the two human cancer cell lines, HeLa and human colon carcinoma 116 cell lines and showed no significant cytotoxic activity against these two cell lines at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activity against Gram-negative bacteria, Escherichia coli, Pseudomonas flurescence and Gram-positive bacteria, Staphylococcus aureus, Bacillus subtilis. Most of the synthesized compounds showed moderate activity against fungal strain Candida albicans. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimycobacterial agent.
- Abhale, Yogita K.,Shinde, Abhijit,Deshmukh, Keshav K.,Nawale, Laxman,Sarkar, Dhiman,Mhaske, Pravin C.
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p. 2557 - 2567
(2017/10/06)
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- Synthesis and in-vitro cytotoxicity of poly-functionalized 4-(2-arylthiazol-4-yl)-4H-chromenes
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A new series of 4-aryl-4H-chromenes bearing a 2-arylthiazol-4-yl moiety at the 4-position were prepared as potential cytotoxic agents. The in-vitro cytotoxic activity of the synthesized 4-aryl-4H-chromenes was investigated in comparison with etoposide, a well-known anticancer drug, using MTT colorimetric assay. Among them, the 2-(2-chlorophenyl)thiazol-4-yl analog 4b showed the most potent activity against nasopharyngeal epidermoid carcinoma KB, medulloblastoma DAOY, and astrocytoma 1321N1, and compound 4d bearing a 2-(4-chlorophenyl) thiazol-4-yl moiety at the 4-position of the chromene ring exhibited the best inhibitory activity against breast cancer cells MCF-7, lung cancer cells A549, and colon adenocarcinoma cells SW480 with IC50 values less than 5 μM. The ability of compound 4b to induce apoptosis was confirmed in a nuclear morphological assay by DAPI staining in the KB and MCF-7 cells.
- Mahmoodi, Majid,Aliabadi, Alireza,Emami, Saeed,Safavi, Maliheh,Rajabalian, Saeed,Mohagheghi, Mohammad-Ali,Khoshzaban, Ahad,Samzadeh-Kermani, Alireza,Lamei, Navid,Shafiee, Abbas,Foroumadi, Alireza
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p. 411 - 416
(2011/08/05)
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