SYNTHESIS, X-RAY CRYSTAL-STRUCTURE, AND BIOLOGICAL-ACTIVITY OF FR186054, A NOVEL, POTENT, ORALLY-ACTIVE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT) BEARING A PYRAZOLE RING

Authors
TANAKA A TERASAWA T HAGIHARA H KINOSHITA T SAKUMA Y ISHIBE N SAWADA M TAKASUGI H TANAKA H
Citation
A. Tanaka et al., SYNTHESIS, X-RAY CRYSTAL-STRUCTURE, AND BIOLOGICAL-ACTIVITY OF FR186054, A NOVEL, POTENT, ORALLY-ACTIVE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT) BEARING A PYRAZOLE RING, Bioorganic & medicinal chemistry letters, 8(1), 1998, pp. 81-86
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
1
Year of publication
1998
Pages
81 - 86
Database
ISI
SICI code
0960-894X(1998)8:1<81:SXCABO>2.0.ZU;2-T
Abstract
The synthesis, single crystal X-ray structural analysis, and biologica l activity of FR186054 (2c), a new, potent, orally efficacious inhibit or of acyl-CoA:cholesterol O-acyltransferase (ACAT), containing a pyra zole ring are described. This compound displayed excellent in vivo eff icacy, irrespective of dosing method, indicating superior characterist ics compared to other ACAT inhibitors. (C) 1997 Elsevier Science Ltd. All rights reserved.