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Synthesis of Some Novel 2-[2-(aroyl-aroxy)-methyl]-4-phenyl-1,3-thiazoles as Potent Anti-Inflammatory Agents |
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| Authors: | Neithnadka Premsai Rai T. D. Venu B. K. Manuprasad Sheena Shashikanth P. N. Arunachalam Aiysha Firdouse |
| Affiliation: | 1. Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, India Syngene Intl Ltd Plot no 2&3, Bommasandra-jigani link road, Bangalore 576099, India;2. Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, India;3. Syngene Intl Ltd Plot no 2&3, Bommasandra-jigani link road, Bangalore 576099, India;4. Department of Biochemisty, Yuvaraja College, University of Mysore, Mysore 570006, India |
| Abstract: | A series of 2-[2-(aroyl-aroxy)-methyl]-4-phenyl-1,3-thiazoles 4a–j were obtained via multiple step synthesis sequence beginning with the hydroxybenzophenones (1a–g). Hydroxybenzophenones on reaction with chloroacetonitrile affords [(2-benzoyl) phenoxy] acetonitrile (2a–g), which reacts with H2S/NH4OH and yields [(2-benzoyl) phenoxy] acetothiamide (3a–g), which on treatment with phenacylbromides affords 2-[2-(aroyl-aroxy)-methyl]-4-phenyl-1,3-thiazoles (4a–j). All the newly synthesized compounds were evaluated for their anti-inflammatory activity and were compared with standard drugs. Of the compounds studied, (4g), compounds with chloro substituents showed more potent activity than the standard drug phenyl butazone at all doses tested. |
| Keywords: | anti-inflammatory activity benzophenones 1,3-thiazoles |