DISCOVERY AND OPTIMIZATION OF INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS

Authors
HOLMS JH DAVIDSEN SK SHEPPARD GS CARRERA GM CURTIN ML HEYMAN HR PIREH D STEINMAN DH ALBERT DH CONWAY RG LUO GJ MAGOC TJ TAPANG P RHEIN DA SUMMERS JB
Citation
Jh. Holms et al., DISCOVERY AND OPTIMIZATION OF INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(23), 1995, pp. 2903-2908
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
23
Year of publication
1995
Pages
2903 - 2908
Database
ISI
SICI code
0960-894X(1995)5:23<2903:DAOOIP>2.0.ZU;2-Y
Abstract
(indol-3-ylcarbonyl)-1H-3H-pyrrolo[1,2-c]thiazoles represent a new cla ss of platelet activating factor antagonists. This series was discover ed by combining the indole portion of a previous thiazolidine series w ith the known 3-pyridinyl-pyrrolothiazole pharmacophore. Optimization of the indole substituents resulted in the identification of 8i as one of the most potent PAF antagonists yet described.