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吡唑的胍基苯基衍生物:合成及其对丝氨酸蛋白酶、血液凝固和血小板聚集的抑制作用。

Guanidinophenyl derivatives of pyrazole: synthesis and inhibitory effect on serine proteinases, blood coagulation and platelet aggregation.

作者信息

Ferroni R, Menegatti E, Scalia S, Orlandini P, Guarneri M, Taddeo U

出版信息

Farmaco Sci. 1986 Oct;41(10):747-57.

PMID:3539635
Abstract

Guanidinophenyl derivatives of pyrazole have been synthesized. Their inhibitory effects on (i) bovine trypsin, bovine thrombin, porcine pancreatic kallikrein catalyzed hydrolysis of p-nitro anilide of N alpha -benzoyl-arginine and (ii) blood coagulation and platelet aggregation, were investigated. The kinetic behaviour of all compounds conformed to that of a reversible competitive inhibition pattern, and they were also found to act in vitro as inhibitors of platelet aggregation induced by ADP.

摘要

已合成吡唑的胍基苯基衍生物。研究了它们对(i)牛胰蛋白酶、牛凝血酶、猪胰激肽释放酶催化的Nα-苯甲酰精氨酸对硝基苯胺水解反应,以及(ii)血液凝固和血小板聚集的抑制作用。所有化合物的动力学行为均符合可逆竞争性抑制模式,并且还发现它们在体外可作为ADP诱导的血小板聚集的抑制剂。

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