5-羟基邻氨基苯甲酸衍生物作为有效的5-脂氧合酶抑制剂

5-Hydroxyanthranilic acid derivatives as potent 5-lipoxygenase inhibitors.

作者信息

Ohkuma H, Tomita K, Hoshino Y, Suzuki K, Hasegawa M, Sawada Y, Konishi M, Hook D J, Oki T

机构信息

Bristol-Myers Squibb Research Institute, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 1993 May;46(5):705-11. doi: 10.7164/antibiotics.46.705.

DOI:10.7164/antibiotics.46.705

PMID:8514624

Abstract

Three new 5-lipoxygenase inhibitors, designated as BU-4601 A, B and C, were found in the fermentation broth of Streptomyces sp. strain No. AA2807. Their structures were identified as isodecyl, isoundecyl and isolauryl esters of 5-hydroxyanthranilic acid, respectively. Based on their structures, five related esters were synthesized and evaluated for biological activity as inhibitors of 5-lipoxygenase. Both naturally-occurring and chemically-synthesized compounds exhibited almost equal levels of 5-lipoxygenase inhibitory activities in vitro.

摘要

在链霉菌属菌株AA2807的发酵液中发现了三种新型5-脂氧合酶抑制剂，分别命名为BU-4601 A、B和C。它们的结构分别被鉴定为5-羟基邻氨基苯甲酸的异癸酯、异十一烷基酯和异月桂酯。基于它们的结构，合成了五种相关酯，并对其作为5-脂氧合酶抑制剂的生物活性进行了评估。天然存在的化合物和化学合成的化合物在体外均表现出几乎相同水平的5-脂氧合酶抑制活性。