Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators

Liangqin Guo; Zhixiong Ye; Feroze Ujjainwalla; Heather L Sings; Iyassu K Sebhat; John Huber; David H Weinberg; Rui Tang; Tanya MacNeil; Constantin Tamvakopoulos; Qianping Peng; Euan MacIntyre; Lex H T van der Ploeg; Mark T Goulet; Matthew J Wyvratt; Ravi P Nargund

doi:10.1016/j.bmcl.2008.04.049

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3242-7. doi: 10.1016/j.bmcl.2008.04.049. Epub 2008 Apr 25.

Authors

Liangqin Guo¹, Zhixiong Ye, Feroze Ujjainwalla, Heather L Sings, Iyassu K Sebhat, John Huber, David H Weinberg, Rui Tang, Tanya MacNeil, Constantin Tamvakopoulos, Qianping Peng, Euan MacIntyre, Lex H T van der Ploeg, Mark T Goulet, Matthew J Wyvratt, Ravi P Nargund

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, 126 E. Lincoln Avenue, PO Box 2000, RY 50G-332, Rahway, NJ 07065, USA. [email protected]

PMID: 18479920
DOI: 10.1016/j.bmcl.2008.04.049

Abstract

Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.

MeSH terms

Administration, Oral
Humans
Molecular Structure
Pyrrolidines / chemical synthesis*
Pyrrolidines / pharmacokinetics*
Receptor, Melanocortin, Type 4 / agonists*
Stereoisomerism
Structure-Activity Relationship
Telomerase

Substances

Pyrrolidines
Receptor, Melanocortin, Type 4
TERT protein, human
Telomerase