作为环氧化酶-2（COX-2）抑制剂的N-取代吲哚酯的合成及生物学评价

Synthesis and biological evaluation of N-substituted indole esters as inhibitors of cyclo-oxygenase-2 (COX-2).

作者信息

Olgen Süreyya, Nebioglu Doğu

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Catania, Italy.

出版信息

Farmaco. 2002 Aug;57(8):677-83. doi: 10.1016/s0014-827x(02)01233-8.

DOI:10.1016/s0014-827x(02)01233-8

PMID:12361236

Abstract

A series of novel N-substituted indole carboxylic, acetic and propionic acid esters have been prepared as possible cyclo-oxygenase-2 (COX-2) enzyme inhibitors. Compounds 20, 23 were found slightly active against COX-2. The synthesis of indole carboxylic, acetic and propionic acid esters were furnished by using dicyclohexyl carbodiimide (DCC), dimethylamino pyridine (DMAP) as carboxylate activators. N-substitution of indole esters was verified with several benzyl and benzoyl group in presence of NaH in DMF, respectively.

摘要

已制备了一系列新型的N-取代吲哚羧酸酯、乙酸酯和丙酸酯，作为可能的环氧化酶-2（COX-2）酶抑制剂。发现化合物20、23对COX-2有轻微活性。吲哚羧酸酯、乙酸酯和丙酸酯的合成是通过使用二环己基碳二亚胺（DCC）、二甲基氨基吡啶（DMAP）作为羧酸盐活化剂来完成的。分别在DMF中NaH存在下，用几个苄基和苯甲酰基验证了吲哚酯的N-取代。