Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors

Acta Chimica Sinica ›› 2006, Vol. 64 ›› Issue (15): 1559-1564. Previous Articles Next Articles

Original Articles

萘普生噻唑衍生物的设计和合成及其环氧合酶-2抑制活性的体外评价

郭长彬, 郭彦伸, 郭宗儒*, 肖景发, 褚凤鸣, 程桂芳

(中国医学科学院中国协和医科大学药物研究所北京 100050)

投稿日期:2005-10-24 修回日期:2006-01-06 发布日期:2006-08-14
通讯作者: 郭宗儒

Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors

GUO Chang-Bin, GUO Yan-Shen, GUO Zong-Ru*, XIAO Jing-Fa
CHU Feng-Ming, CHENG Gui-Fang

(Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050)

Received:2005-10-24 Revised:2006-01-06 Published:2006-08-14
Contact: GUO Zong-Ru

Abstract

Based on the differences between cyclooxygenase-2 (COX-2) and COX-1, a series of derivatives of naproxen in which the carboxyl group was replaced with a variety of substituted thiazolyls were designed. Seven target compounds were synthesized in four steps with naproxen as a starting material and structurally confirmed by ¹H NMR, MS and elemental analysis or HRMS. The biological tests showed that some of them have inhibitory activity against COX-2 in vitro.

Key words: naproxen, cyclooxygenase-2, inhibitor, thiazole derivative

Cite this article

GUO Chang-Bin, GUO Yan-Shen, GUO Zong-Ru*, XIAO Jing-Fa
CHU Feng-Ming, CHENG Gui-Fang. Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors[J]. Acta Chimica Sinica, 2006, 64(15): 1559-1564.

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萘普生噻唑衍生物的设计和合成及其环氧合酶-2抑制活性的体外评价

Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors

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