Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors
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DOI：
10.1016/s0960-894x(00)00631-4
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发表时间：
2001-01-22
影响因子：
2.7
通讯作者：
Wildgoose, P
中科院分区：
文献类型：
--
作者：
Heinelt, U;Herok, S;Wildgoose, P
从非手性和有效的Xa因子抑制剂1开始，描述了一种新的灵活的固相优化策略，以减少其阳离子特性。通过用亲脂性取代基取代一个带正电荷的侧链，发现了一系列新型的高效和选择性的非手性Xa因子抑制剂。在S4口袋中鉴定的亲脂性替代物可能对fXa抑制剂的其他方法有价值。(C)2001爱思唯尔科技有限公司版权所有。
Starting from the achiral and potent factor Xa inhibitor 1, a new and flexible solid-phase optimisation strategy is described to reduce its cationic character. By replacing one positively charged side chain by a lipophilic substituent, a novel series of highly potent and selective achiral factor Xa inhibitors was discovered. The identified lipophilic replacements in the S4 pocket might be valuable for other approaches towards fXa inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.