A NEW SYNTHESIS OF FPL-64176 AND ANALOGS - THE DISCOVERY OF BENZOYLPYRROLE CALCIUM-CHANNEL ACTIVATORS WITH LOW NANOMOLAR POTENCY

被引：10

作者：

BAXTER, AJG

TEAGUE, SJ

机构：

[1] Department of Medicinal Chemistry, Fisons plc, Pharmaceutical Division, Loughborough, Leicestershire LE11 ORH, Bakewell Road

来源：

TETRAHEDRON | 1993年 / 49卷 / 40期

关键词：

D O I：

10.1016/S0040-4020(01)91225-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Heavy metal assisted halogen displacement on 2-halobenzoylpyrroles (2 and 3) leads to a simple synthesis of FPL 64176 (1) and a variety of analogues (4-10). The difluoro derivative (4), EC50 1nM, and the amino linked analogue (7), EC50 2.7nM, are presently the most potent calcium channel activators known.

引用

页码：9089 / 9094

页数：6

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