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

Richard Sulsky; Jeffrey A Robl; Scott A Biller; Thomas W Harrity; John Wetterau; Fergal Connolly; Kern Jolibois; Lori Kunselman

doi:10.1016/j.bmcl.2004.07.069

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

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. doi: 10.1016/j.bmcl.2004.07.069.

Authors

Richard Sulsky¹, Jeffrey A Robl, Scott A Biller, Thomas W Harrity, John Wetterau, Fergal Connolly, Kern Jolibois, Lori Kunselman

Affiliation

¹ Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. [email protected]

PMID: 15380200
DOI: 10.1016/j.bmcl.2004.07.069

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.

Publication types

Comparative Study

MeSH terms

Amides / chemical synthesis*
Amides / chemistry
Amides / pharmacology
Animals
Benzimidazoles / chemistry
Benzimidazoles / pharmacology
Carrier Proteins / antagonists & inhibitors*
Cricetinae
Cyclic P-Oxides / chemical synthesis*
Cyclic P-Oxides / chemistry
Cyclic P-Oxides / pharmacology
Humans
In Vitro Techniques
Male
Stereoisomerism
Structure-Activity Relationship

Substances

Amides
BMS201038
Benzimidazoles
Carrier Proteins
Cyclic P-Oxides
microsomal triglyceride transfer protein