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新型噻唑基、噻唑啉基和苯并噻唑基席夫碱作为潜在的脂氧合酶抑制剂和抗炎剂。

Novel thiazolyl, thiazolinyl and benzothiazolyl Schiff bases as possible lipoxygenase's inhibitors and anti-inflammatory agents.

作者信息

Geronikaki Athina, Hadjipavlou-Litina Dimitra, Amourgianou Maria

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.

出版信息

Farmaco. 2003 Jul;58(7):489-95. doi: 10.1016/S0014-827X(03)00065-X.

Abstract

In continuation of our previous research, several new thiazolyl/thiazolinyl/benzothiazolyl Schiff bases have been designed, synthesized and identified. The referred compounds are reported to act as lipoxygenase inhibitors affecting inflammation and/or psoriasis. The compounds were screened for their reducing activity (with the stable free radical 1,1-diphenyl-2-picryl-hydrazyl, DPPH) and for inhibition of soybean lipoxygenase (LOX). Anti-inflammatory activity was examined in vivo using the carrageenin induced mice paw edema (32.6-75%). The results are discussed in terms of structural and physicochemical characteristics of the compounds. Compound 2d possessed the highest inhibition 75%.

摘要

作为我们先前研究的延续,我们设计、合成并鉴定了几种新的噻唑基/噻唑啉基/苯并噻唑基席夫碱。据报道,这些化合物可作为脂氧合酶抑制剂,影响炎症和/或牛皮癣。对这些化合物进行了还原活性(使用稳定自由基1,1-二苯基-2-苦基肼,DPPH)和大豆脂氧合酶(LOX)抑制作用的筛选。使用角叉菜胶诱导的小鼠爪肿胀模型在体内检测抗炎活性(32.6-75%)。根据化合物的结构和物理化学特性对结果进行了讨论。化合物2d具有最高的抑制率,为75%。

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