Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists
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DOI:
10.1016/s0960-894x(99)00339-x
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发表时间:
1999-07-19
影响因子:
2.7
通讯作者:
Wu, YS
Wu, YS
中科院分区:
医学4区
文献类型:
--
作者:
Ahn, HS;Arik, L;Wu, YS

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已经发现了一系列吡咯并喹唑啉,它们代表凝血酶受体的分子内配体的新型小分子抑制剂。制备类似物以研究在杂环的N1、N3和N7位取代的构效关系。化合物4e和4f已被鉴定为分别具有56和52 nM的IC 50。(C)1999 Elsevier Science Ltd.保留所有权利。
A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively. (C) 1999 Elsevier Science Ltd. All rights reserved.