5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP

[Display omitted] 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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-10, Vol.14 (20), p.5067-5070
Main Authors: Sulsky, Richard, Robl, Jeffrey A., Biller, Scott A., Harrity, Thomas W., Wetterau, John, Connolly, Fergal, Jolibois, Kern, Kunselman, Lori
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Animals
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Carrier Proteins - antagonists & inhibitors
Cricetinae
Cyclic P-Oxides - chemical synthesis
Cyclic P-Oxides - chemistry
Cyclic P-Oxides - pharmacology
Cyclophosphonates
General and cellular metabolism. Vitamins
Humans
In Vitro Techniques
Male
Medical sciences
MTP inhibitors
Pharmacology. Drug treatments
Stereoisomerism
Structure-Activity Relationship
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Description
Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.07.069