作为选择性环氧化酶（COX-2）抑制剂的3-烷基-2-芳基-1,3-噻嗪烷-4-酮衍生物的设计与合成

Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.

作者信息

Zebardast Tannaz, Zarghi Afshin, Daraie Bahram, Hedayati Mehdi, Dadrass Orkideh G

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University (M.C), Tehran, Iran.

出版信息

Bioorg Med Chem Lett. 2009 Jun 15;19(12):3162-5. doi: 10.1016/j.bmcl.2009.04.125. Epub 2009 May 3.

DOI:10.1016/j.bmcl.2009.04.125

PMID:19447036

Abstract

A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-benzyl-2-(4-methylsulfonylphenyl)-1,3-thiazinan-4-one (11a) as a potent (IC(50)=0.06 microM) and selective (selectivity index >285) COX-2 inhibitor.

摘要

合成了一组新的具有甲磺酰基药效团的3-烷基-2-芳基-1,3-噻嗪烷-4-酮，并对其环氧化酶-2（COX-2）抑制活性进行了生物活性评估。体外COX-1/COX-2抑制研究确定3-苄基-2-（4-甲磺酰基苯基）-1,3-噻嗪烷-4-酮（11a）为一种强效（IC(50)=0.06 microM）且选择性（选择性指数>285）的COX-2抑制剂。

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作为选择性环氧化酶（COX-2）抑制剂的3-烷基-2-芳基-1,3-噻嗪烷-4-酮衍生物的设计与合成

Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.

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