1.
Bioorg Med Chem Lett
; 15(2): 251-4, 2005 Jan 17.
Article
in English
| MEDLINE
| ID: mdl-15603933
ABSTRACT
The discovery of a novel, potent and selective beta(3)-adrenergic receptor (AR) agonist is described. SAR studies demonstrated the structural requirements for activity and selectivity. Compound 1c, which showed good beta(3)-AR activity and selectivity, was identified and pharmacokinetics were investigated.
Subject(s)
Adrenergic beta-3 Receptor Agonists , Adrenergic beta-Agonists/chemical synthesis , Adrenergic beta-Agonists/pharmacology , Animals , CHO Cells , Cricetinae , Humans , Models, Chemical , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 14(3): 633-7, 2004 Feb 09.
Article
in English
| MEDLINE
| ID: mdl-14741258
ABSTRACT
The synthesis and biological properties of a novel squalene epoxidase inhibitor, FR194738, are described. This compound displayed potent in vitro inhibitory activities against squalene epoxidase and cholesterol synthesis, and lowered plasma cholesterol and triglyceride levels in dogs.
