Journal of Medicinal Chemistry p. 353 - 358 (1995)
Update date:2022-08-03
Topics:
Chihiro
Nagamoto
Takemura
Kitano
Komatsu
Sekiguchi
Tabusa
Mori
Tominaga
Yabuuchi
Neutrophils have an important role in the self-defense systems of organisms through the production of superoxide. On the other hand, it has been proposed that abnormal amounts of superoxide produced by neutrophils are a serious factor in tissue injury. A series of novel thiazole derivatives was prepared and evaluated inhibitory effect on superoxide production by human neutrophils in vitro. Among these compounds, 6-[2-(3,4- diethoxyphenyl)thiazol-4-yl]-pyridine-2-carboxylic acid (OPC-6535) was selected as one of the most promising compounds. The synthesis and structure- activity relationships of these compounds are reported herein.
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