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环状胍类：4,6,7,8-四氢-1H-咪唑并[1,2-a]吡唑并[3,4-d]嘧啶-7-酮和1,4,6,7,8,9-六氢吡唑并[3',4':4,5]嘧啶并[2,1-c][1,2,4]三嗪-7-酮的合成与抗血小板活性

Cyclic guanidines: synthesis and antiplatelet activity of 4,6,7,8-tetrahydro-1H-imidazo[1,2-a]pyrazolo[3,4-d]pyrimidin-7-ones and 1,4,6,7,8,9-hexahydropyrazolo [3',4':4,5]pyrimido[2,1-c] [1,2,4]triazin-7-ones.

作者信息

Ferroni R, Simoni D, Orlandini P, Bardi A, Franze G P, Guarneri M

机构信息

Dipartimento di Scienze Farmaceutiche dell'Università, Ferrara, Italy.

出版信息

Arzneimittelforschung. 1990 Dec;40(12):1328-31.

PMID:2095128
Abstract

A series of 4,6,7,8-tetrahydro-1H-imidazo[1,2-a]pyrazolo [3,4-d]pyrimidin-7-ones (1b-n) and 1,4,6,7,8,9-hexahydropyrazolo [3',4':4,5]pyrimido [2,1-c][1,2,4]triazin-7-ones (2a-d) has been synthesized. In view of their potential anti-aggregating activity the compounds were tested in vitro for inhibitory activity towards ADP- and collagen-induced aggregation of human platelets. Among the compounds studied, 8-benzyl-1-(2,5-dichlorophenyl)-4,6,7,8-tetrahydro-1H-imidazo [1,2-a]pyrazolo[3,4-d]pyrimidin-7-one (1n) exhibited the most favorable activity. The 2,5-dichlorophenyl side chain is an important lipophilic and/or steric pharmacophore.

摘要

已合成了一系列4,6,7,8-四氢-1H-咪唑并[1,2-a]吡唑并[3,4-d]嘧啶-7-酮（1b-n）和1,4,6,7,8,9-六氢吡唑并[3',4':4,5]嘧啶并[2,1-c][1,2,4]三嗪-7-酮（2a-d）。鉴于它们潜在的抗聚集活性，对这些化合物进行了体外测试，以检测其对ADP和胶原诱导的人血小板聚集的抑制活性。在所研究的化合物中，8-苄基-1-(2,5-二氯苯基)-4,6,7,8-四氢-1H-咪唑并[1,2-a]吡唑并[3,4-d]嘧啶-7-酮（1n）表现出最有利的活性。2,5-二氯苯基侧链是一个重要的亲脂性和/或空间药效基团。

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