ACYL-COA-CHOLESTEROL ACYLTRANSFERASE (ACAT) INHIBITORS - HETEROCYCLICBIOISOSTERES FOR THE UREA GROUP IN DUP-128

Authors
WILDE RG KLACZKIEWICZ JD BILLHEIMER JT WEXLER RR GILLIES PJ
Citation
Rg. Wilde et al., ACYL-COA-CHOLESTEROL ACYLTRANSFERASE (ACAT) INHIBITORS - HETEROCYCLICBIOISOSTERES FOR THE UREA GROUP IN DUP-128, Bioorganic & medicinal chemistry letters, 5(2), 1995, pp. 177-180
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
2
Year of publication
1995
Pages
177 - 180
Database
ISI
SICI code
0960-894X(1995)5:2<177:AA(I-H>2.0.ZU;2-C
Abstract
A series of compounds bearing two heterocyclic substituents were evalu ated for inhibition of the ACAT enzyme. One heterocyclic group was cho sen to mimic the urea group in our clinical candidate, DuP 128. Of the several groups examined, aminobenzoxazoles proved to be the most pote nt in terms of inhibition of ACAT in J774 macrophage cells.