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

Authors
BAXTER AJG TEAGUE SJ
Citation
Ajg. Baxter et Sj. Teague, A NEW SYNTHESIS OF FPL-64176 AND ANALOGS - THE DISCOVERY OF BENZOYLPYRROLE CALCIUM-CHANNEL ACTIVATORS WITH LOW NANOMOLAR POTENCY, Tetrahedron, 49(40), 1993, pp. 9089-9094
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron → ACNP
ISSN journal
00404020
Volume
49
Issue
40
Year of publication
1993
Pages
9089 - 9094
Database
ISI
SICI code
0040-4020(1993)49:40<9089:ANSOFA>2.0.ZU;2-J
Abstract
Heavy metal assisted halogen displacement on 2-halobenzoylpyrroles (2 and 3) leads to a simple synthesis of FPL 64176 (1) and a variety of a nalogues (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.