新型 1,3-苯并二氮杂环庚烷-4-酮衍生物的设计与合成作为选择性环氧化酶（COX-2）抑制剂。
Design and synthesis of new 1,3-benzdiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
机构信息
Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
出版信息
Arch Pharm (Weinheim). 2012 Apr;345(4):257-64. doi: 10.1002/ardp.201100138. Epub 2011 Nov 11.
A new group of regioisomeric 2,3-diaryl-1,3-benzdiazinan-4-ones, possessing a methyl sulfonyl pharmacophore, were synthesized and their biological activities were tested for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-(p-fluorophenyl)-2-(4-methylsulfonylphenyl)-1,3-benzdiazinane-4-one (2b) as a potent and highly selective (IC(50) = 0.07 µM; selectivity index = 572.8) COX-2 inhibitor.
一组新的 2,3-二芳基-1,3-苯并二氮杂环庚烷-4-酮区域异构体被合成，这些化合物具有一个甲磺酰基药效团，它们的生物活性被测试为环氧化酶-2（COX-2）抑制活性。体外 COX-1/COX-2 抑制研究表明，3-(对氟苯基)-2-(4-甲磺酰基苯基)-1,3-苯并二氮杂环庚烷-4-酮（2b）是一种有效的、高度选择性的（IC50 = 0.07 µM；选择性指数 = 572.8）COX-2 抑制剂。
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