title: Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of acyl-CoA:cholesterol acyl transferase inhibitors.
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.
authors.affiliation: Istituto di Chimica Farmaceutica e Tossicologica, Universita di Milano, Milano, Italy.
authors.forename: Arianna
authors.initials: A
authors.lastname: Gelain
authors.forename: Daniela
authors.initials: D
authors.lastname: Barlocco
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
authors.forename: Tae-Sook
authors.initials: TS
authors.lastname: Jeong
authors.forename: Kyung-Ran
authors.initials: KR
authors.lastname: Im
authors.forename: Laura
authors.initials: L
authors.lastname: Legnani
authors.forename: Lucio
authors.initials: L
authors.lastname: Toma
mesh_terms: D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D011724:Pyridazines; D002785:Sterol O-Acyltransferase