Synthesis of novel and potent vorapaxar analogues

被引：6

作者：

Knight, Emily ^{[1
]}

Robinson, Eifion ^{[1
]}

Smoktunowicz, Natalia ^{[2
]}

Chambers, Rachel C. ^{[2
]}

Aliev, Abil E. ^{[1
]}

Inglis, Graham G. ^{[3
]}

Chudasama, Vijay ^{[1
]}

Caddick, Stephen ^{[1
]}

机构：

[1] UCL, Dept Chem, 20 Gordon St, London WC1H 0AJ, England

[2] Ctr Inflammat & Tissue Repair, 5 Univ St, London WC1E 6JJ, England

[3] GSK, Gunnels Wood Rd, Stevenage SG1 2NY, Herts, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2016年 / 14卷 / 12期

基金：

英国工程与自然科学研究理事会;

关键词：

THROMBIN RECEPTOR ANTAGONIST; PAR-1; ANTAGONISTS; DISCOVERY; RING;

D O I：

10.1039/c5ob02541a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Vorapaxar is a first-in-class PAR-1 antagonistic drug based on the ent-himbacine scaffold. Detailed in this article are enantioselective and racemic routes to various novel vorapaxar analogues. Biological testing revealed these compounds to have moderate to excellent potencies against PAR-1 with the most potent analogue demonstrating an IC50 of 27 nM.

引用

页码：3264 / 3274

页数：11

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