METABOLISM AND STRUCTURE-ACTIVITY DATA-BASED DRUG DESIGN - DISCOVERY OF (-) SCH-53079 AN ANALOG OF THE POTENT CHOLESTEROL ABSORPTION INHIBITOR (-) SCH-48461

Authors
DUGAR S YUMIBE N CLADER JW VIZZIANO M HUIE K VANHEEK M COMPTON DS DAVIS HR
Citation
S. Dugar et al., METABOLISM AND STRUCTURE-ACTIVITY DATA-BASED DRUG DESIGN - DISCOVERY OF (-) SCH-53079 AN ANALOG OF THE POTENT CHOLESTEROL ABSORPTION INHIBITOR (-) SCH-48461, Bioorganic & medicinal chemistry letters, 6(11), 1996, pp. 1271-1274
Citations number
5
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
11
Year of publication
1996
Pages
1271 - 1274
Database
ISI
SICI code
0960-894X(1996)6:11<1271:MASDDD>2.0.ZU;2-H
Abstract
Based on the metabolism of the potent cholesterol absorption inhibitor (-) SCH48461 and structure activity relationship information, we desi gned and evaluated (-)SCH 53079. This compound was found to be equipot ent to (-)SCH 48461 in both the cholesterol-fed hamster and rhesus mon key assays. Importantly, (-)SCH 53079 was metabolically more stable th an (-)SCH 48461 and as desired had very low plasma levels and did not cause hepatic enzyme induction. Copyright (C) 1996 Elsevier Science Lt d