1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors

被引：17

作者：

Harmat, NJS

Di Bugno, C

Criscuoli, M

Giorgi, R

Lippi, A

Martinelli, A

Monti, S

Subissi, A

机构：

[1] Menarini Ric SpA, Lab Firenze, I-50131 Florence, Italy

[2] Menarini Ric SpA, Lab Pisa, I-56010 Pisa, Italy

[3] Dipartimento Sci Farmaceut, I-56126 Pisa, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(98)00200-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of tripeptide arginine aldehydes was synthesized by replacement of proline with 1,2-disubstituted cyclohexane derivatives in the sequence of D-MePhe-Pro-Arg-H. Based on molecular modeling, further modification of the D-MePhe residue resulted in a potent and selective thrombin inhibitor. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：1249 / 1254

页数：6

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