SYNTHESIS AND EVALUATION OF WATER-SOLUBLE INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS

Authors
SHEPPARD GS DAVIDSEN SK CARRERA GM PIREH D HOLMS JH HEYMAN HR STEINMAN DH CURTIN ML CONWAY RG RHEIN DA ALBERT DH TAPANG P MAGOC TJ SUMMERS JB
Citation
Gs. Sheppard et al., SYNTHESIS AND EVALUATION OF WATER-SOLUBLE INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(23), 1995, pp. 2913-2918
Citations number
7
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
2913 - 2918
Database
ISI
SICI code
0960-894X(1995)5:23<2913:SAEOWI>2.0.ZU;2-X
Abstract
dinyl)-7-(indol-3-ylcarbonyl)-1H-3H-pyrrolo[1,2-c] thiazoles represent a class of potent, orally active PAF antagonists; however, the lead c ompounds in this series suffered from a lack of aqueous solubility. To overcome this limitation, a number of strategies were examined to ach ieve improved solubility, involving the incorporation of polar substit uents and the use of prodrugs.