Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands

Raman K Bakshi; Qingmei Hong; Rui Tang; Rubana N Kalyani; Tanya Macneil; David H Weinberg; Lex H T Van der Ploeg; Arthur A Patchett; Ravi P Nargund

doi:10.1016/j.bmcl.2005.11.095

Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1130-3. doi: 10.1016/j.bmcl.2005.11.095. Epub 2005 Dec 20.

Authors

Raman K Bakshi¹, Qingmei Hong, Rui Tang, Rubana N Kalyani, Tanya Macneil, David H Weinberg, Lex H T Van der Ploeg, Arthur A Patchett, Ravi P Nargund

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. [email protected]

PMID: 16364639
DOI: 10.1016/j.bmcl.2005.11.095

Abstract

Design and synthesis of potent MC4 selective agonists based on cyclohexylpiperidine derived cyclic urea, oxazolidinones, and sulfonamide based privileged structures are disclosed.

MeSH terms

Drug Design*
Humans
Ligands
Molecular Structure
Receptor, Melanocortin, Type 4 / agonists*
Receptor, Melanocortin, Type 4 / metabolism*
Sensitivity and Specificity
Structure-Activity Relationship
Substrate Specificity

Substances

Ligands
MC4R protein, human
Receptor, Melanocortin, Type 4