Document Report Card

ID: ALA1141600

Journal: J Med Chem

Title: Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of acyl-CoA:cholesterol acyl transferase inhibitors.

Authors: Gelain A, Barlocco D, Kwon BM, Jeong TS, Im KR, Legnani L, Toma L.

Abstract: A series of alkylamido- ( 1) and alkylaminobiphenyl ( 2) derivatives were synthesized as possible bioisosters of the reported ACAT inhibitors phenylpyridazine analogues ( I). Both 1 and 2 were tested on the human ACAT-1 and ACAT-2 isoforms. The amino derivatives 2 were found to be inactive, contrary to the related pyridazine derivatives. By contrast, the ortho -substituted amides 1a and 1d showed an interesting activity. These results support the essential role of the pyridazine nucleus. Modeling studies were also performed.

CiteXplore: 18284184

DOI: 10.1021/jm701474c