Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core

Iyassu K Sebhat; Yingjie Lai; Khaled Barakat; Zhixiong Ye; Rui Tang; Rubana N Kalyani; Aurawan Vongs; Tanya Macneil; David H Weinberg; M Angeles Cabello; Marta Maroto; Ana Teran; Tung M Fong; Lex H T Van der Ploeg; Arthur A Patchett; Ravi P Nargund

doi:10.1016/j.bmcl.2006.11.084

Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5720-3. doi: 10.1016/j.bmcl.2006.11.084. Epub 2006 Dec 3.

Authors

Iyassu K Sebhat¹, Yingjie Lai, Khaled Barakat, Zhixiong Ye, Rui Tang, Rubana N Kalyani, Aurawan Vongs, Tanya Macneil, David H Weinberg, M Angeles Cabello, Marta Maroto, Ana Teran, Tung M Fong, Lex H T Van der Ploeg, Arthur A Patchett, Ravi P Nargund

Affiliation

¹ Department of Medicinal Chemistry, Merck & Co., Inc, PO Box, 2000, Rahway, NJ 07065, USA. [email protected]

PMID: 17768046
DOI: 10.1016/j.bmcl.2006.11.084

Abstract

SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.

MeSH terms

Alkanes / chemical synthesis
Alkanes / chemistry
Alkanes / pharmacology*
Amides / chemistry
Humans
Molecular Structure
Nitriles / chemistry
Piperidines / chemical synthesis
Piperidines / chemistry*
Piperidines / pharmacology*
Receptor, Melanocortin, Type 4 / agonists*
Receptor, Melanocortin, Type 4 / metabolism*
Structure-Activity Relationship
Tetrazoles / chemistry

Substances

Alkanes
Amides
Nitriles
Piperidines
Receptor, Melanocortin, Type 4
Tetrazoles
1H-tetrazole
piperidine