Fleischmann K, Scheunemann K H, Schorlemmer H U, Dickneite G, Blumbach J, Fischer G, Dürckheimer W, Sedlacek H H
Research Laboratories of Pharma Research, Frankfurt Main, Fed. Rep. of Germany.
Arzneimittelforschung. 1989 Jul;39(7):743-6.
A series of carboxyalkylthio-substituted thiazole-carboxylic acids was synthesized and examined for macrophage activation and stimulation of the DTH (delayed type of hypersensitivity)-reaction. The structure-activity relationship in this series of new immunomodulators is discussed. Broadest immunological activity was seen for [2-(3-carboxy-1-propylthio)-4-methyl-1,3-thiazole]acetic acid (tiprotimod, HBW 538) which was selected for further studies.
合成了一系列羧烷基硫代取代的噻唑羧酸,并检测了它们对巨噬细胞的激活作用以及对迟发型超敏反应(DTH)的刺激作用。讨论了这一系列新型免疫调节剂的构效关系。[2-(3-羧基-1-丙硫基)-4-甲基-1,3-噻唑]乙酸(替普罗米德,HBW 538)表现出最广泛的免疫活性,因此被选作进一步研究。