Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists

Anil Vasudevan; Matthew J LaMarche; Christopher Blackburn; Jennifer Lee Che; Courtney A Luchaco-Cullis; Sujen Lai; Thomas H Marsilje; Michael A Patane; Andrew J Souers; Derek Wodka; Bradley Geddes; Sumiao Chen; Seven Brodjian; Doug H Falls; Brian D Dayton; Eugene Bush; Michael Brune; Robin D Shapiro; Kennan C Marsh; Lisa E Hernandez; Hing L Sham; Christine A Collins; Philip R Kym

doi:10.1016/j.bmcl.2005.06.089

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4174-9. doi: 10.1016/j.bmcl.2005.06.089.

Affiliation

¹ Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. [email protected]

PMID: 16085414
DOI: 10.1016/j.bmcl.2005.06.089

Abstract

Several potent and efficacious MCHr1 antagonists containing an ortho-amino benzamide or nicotinamide chemotype have been identified, exemplified by 28 and 50.

MeSH terms

Animals
Benzamides / chemical synthesis
Benzamides / pharmacokinetics
Benzamides / pharmacology
Inhibitory Concentration 50
Mice
Mice, Inbred Strains
Niacinamide / analogs & derivatives*
Niacinamide / pharmacokinetics
Niacinamide / pharmacology
Pharmacokinetics
Receptors, Somatostatin / agonists
Receptors, Somatostatin / antagonists & inhibitors*
Structure-Activity Relationship
Tissue Distribution
ortho-Aminobenzoates / chemical synthesis*
ortho-Aminobenzoates / pharmacokinetics
ortho-Aminobenzoates / pharmacology

Substances

Benzamides
Mchr1 protein, mouse
Receptors, Somatostatin
ortho-Aminobenzoates
Niacinamide