1.
Bioorg Med Chem Lett
; 14(20): 5067-70, 2004 Oct 18.
Article
in English
| MEDLINE
| ID: mdl-15380200
ABSTRACT
5-Carboxamido-1,3,2-dioxaphosphorinanes have been identified as potent inhibitors of microsomal triglyceride-transfer protein. The 1,3,2-dioxaphosphorine functionality acted as a neutral and stable replacement for piperidine and piperidine N-oxide.
Subject(s)
Amides/chemical synthesis , Carrier Proteins/antagonists & inhibitors , Cyclic P-Oxides/chemical synthesis , Amides/chemistry , Amides/pharmacology , Animals , Benzimidazoles/chemistry , Benzimidazoles/pharmacology , Cricetinae , Cyclic P-Oxides/chemistry , Cyclic P-Oxides/pharmacology , Humans , In Vitro Techniques , Male , Stereoisomerism , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 13(7): 1337-40, 2003 Apr 07.
Article
in English
| MEDLINE
| ID: mdl-12657277
ABSTRACT
A series of newly synthesized phosphonate esters were evaluated for their effects on microsomal triglyceride transfer protein activity (MTP). The most potent compounds were evaluated for their ability to inhibit lipoprotein secretion in HepG2 cells and to affect VLDL secretion in rats. These inhibitors were also found to lower serum cholesterol levels in a hamster model upon oral dosing.
