The discovery and optimization of pyrimidinone-containing MCH R1 antagonists
- PMID: 16870432
- DOI: 10.1016/j.bmcl.2006.07.008
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists
Abstract
Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented.
Similar articles
-
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.Bioorg Med Chem Lett. 2005 May 16;15(10):2565-9. doi: 10.1016/j.bmcl.2005.03.052. Bioorg Med Chem Lett. 2005. PMID: 15863317
-
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.Bioorg Med Chem Lett. 2006 Jul 15;16(14):3674-8. doi: 10.1016/j.bmcl.2006.04.062. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16690315
-
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16814542
-
Identification of melanin-concentrating hormone receptor and its impact on drug discovery.J Exp Zool A Comp Exp Biol. 2006 Sep 1;305(9):761-8. doi: 10.1002/jez.a.311. J Exp Zool A Comp Exp Biol. 2006. PMID: 16902961 Review.
-
Recent advances in the discovery of melanin-concentrating hormone receptor antagonists.Curr Opin Drug Discov Devel. 2006 Jul;9(4):496-508. Curr Opin Drug Discov Devel. 2006. PMID: 16889232 Review.
Cited by
-
The role of melanin-concentrating hormone and its receptors in energy homeostasis.Front Endocrinol (Lausanne). 2013 Apr 22;4:49. doi: 10.3389/fendo.2013.00049. eCollection 2013. Front Endocrinol (Lausanne). 2013. PMID: 23626585 Free PMC article.
-
Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats.Psychopharmacology (Berl). 2010 Sep;211(4):367-75. doi: 10.1007/s00213-010-1891-y. Epub 2010 Jul 14. Psychopharmacology (Berl). 2010. PMID: 20628734
-
Systematic Data Mining Reveals Synergistic H3R/MCHR1 Ligands.ACS Med Chem Lett. 2017 May 4;8(6):648-653. doi: 10.1021/acsmedchemlett.7b00118. eCollection 2017 Jun 8. ACS Med Chem Lett. 2017. PMID: 28626527 Free PMC article.
-
Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: conformationally restricted 17b-hydroxysteroid dehydrogenase type 2 (17b-HSD2) inhibitors.Molecules. 2013 Apr 16;18(4):4487-509. doi: 10.3390/molecules18044487. Molecules. 2013. PMID: 23591928 Free PMC article.
-
The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.Br J Pharmacol. 2013 Dec;170(8):1459-581. doi: 10.1111/bph.12445. Br J Pharmacol. 2013. PMID: 24517644 Free PMC article.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Chemical Information
Molecular Biology Databases