Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2302-5. doi: 10.1016/j.bmcl.2006.01.016. Epub 2006 Feb 3.

Authors

Tricia J Vos¹, Suresh Balani, Christopher Blackburn, Ryan W Chau, M Diana Danca, Stacey V Drabic, Cheryl A Farrer, Michael A Patane, Stephen G Stroud, David L Yowe, Christopher F Claiborne

Affiliation

¹ Millennium Pharmaceuticals, Inc. 40 Landsdowne St. Cambridge, MA 02139, USA. tricia.vos@mpi.com

PMID: 16458508
DOI: 10.1016/j.bmcl.2006.01.016

Abstract

The identification and optimization of a series of acylguanidine-based melanocortin-4 receptor antagonists is discussed.

MeSH terms

Animals
Binding Sites
Brain / metabolism
Guanidine / analogs & derivatives
Guanidine / chemistry*
Guanidine / pharmacology
Inhibitory Concentration 50
Mice
Plasma / metabolism
Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
Structure-Activity Relationship
Sulfhydryl Compounds / chemistry*
Sulfhydryl Compounds / pharmacology
Time Factors

Substances

Receptor, Melanocortin, Type 4
Sulfhydryl Compounds
Guanidine