Synthesis and anti-inflammatory evaluation of new pyrazoles bearing biodynamic thiazole and thiazolidinone scaffolds

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• 作者：Lalit D. Khillare ; Manisha R. Bhosle ; Amarsinh R. Deshmukh…
• 关键词：Pyrazole ; Thiazole ; Thiazolidinone ; Anti ; inflammatory activity
• 刊名：Medicinal Chemistry Research
• 出版年：2015
• 出版时间：April 2015
• 年：2015
• 卷：24
• 期：4
• 页码：1380-1386
• 全文大小：335 KB
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• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

New trisubstituted pyrazoles bearing thiazolyl and thiazolidinonyl moieties have been successfully and conveniently synthesized in three steps using 5-acetyl thiazoles (1a-strong class="a-plus-plus">b) as starting materials. The route includes the synthesis of new intermediates, 4-formyl 5-thiazolyl pyrazoles (4a-strong class="a-plus-plus">b). The formyl pyrazoles on one pot cyclocondensation with anilines and thioglycolic acid have been found to yield the titled compounds (7a-strong class="a-plus-plus">j). The new pyrazoles have been screened to evaluate in vivo anti-inflammatory activity and compounds 7c, 7d, 7f, 7g, 7h, and 7i have better anti-inflammatory activity than reference drug Celecoxib. The synthetic details and results of anti-inflammatory activity are discussed.