Literature DB >> 16203136

Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

Anil Vasudevan1, Andrew J Souers, Jennifer C Freeman, Mary K Verzal, Ju Gao, Mathew M Mulhern, Derek Wodka, John K Lynch, Kenneth M Engstrom, Seble H Wagaw, Sevan Brodjian, Brian Dayton, Doug H Falls, Eugene Bush, Michael Brune, Robin D Shapiro, Kennan C Marsh, Lisa E Hernandez, Christine A Collins, Philip R Kym.   

Abstract

The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.

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Year:  2005        PMID: 16203136     DOI: 10.1016/j.bmcl.2005.08.049

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.

Authors:  Jozef Stec; Qingqing Huang; Marco Pieroni; Marcel Kaiser; Alina Fomovska; Ernest Mui; William H Witola; Samuel Bettis; Rima McLeod; Reto Brun; Alan P Kozikowski
Journal:  J Med Chem       Date:  2012-03-20       Impact factor: 7.446

2.  Straightforward protocol for the efficient synthesis of varied N(1)-acylated (aza)indole 2-/3-alkanoic acids and esters: optimization and scale-up.

Authors:  Andy J Liedtke; Kwangho Kim; Donald F Stec; Gary A Sulikowski; Lawrence J Marnett
Journal:  Tetrahedron       Date:  2012-12-02       Impact factor: 2.457

3.  The role of melanin-concentrating hormone and its receptors in energy homeostasis.

Authors:  Douglas J Macneil
Journal:  Front Endocrinol (Lausanne)       Date:  2013-04-22       Impact factor: 5.555

  3 in total

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