Literature DB >> 21439820

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.

Qingmei Hong1, Raman K Bakshi, Brenda L Palucki, Min K Park, Zhixiong Ye, Shuwen He, Patrick G Pollard, Iyassu K Sebhat, Jian Liu, Liangqin Guo, Doreen E Cashen, William J Martin, David H Weinberg, Tanya MacNeil, Rui Tang, Constantin Tamvakopoulos, Qianping Peng, Randy R Miller, Ralph A Stearns, Howard Y Chen, Airu S Chen, Alison M Strack, Tung M Fong, D Euan MacIntyre, Matthew J Wyvratt, Ravi P Nargund.   

Abstract

We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21439820     DOI: 10.1016/j.bmcl.2011.02.090

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


  5 in total

Review 1.  New targets to treat obesity and the metabolic syndrome.

Authors:  Kathleen A Martin; Mitra V Mani; Arya Mani
Journal:  Eur J Pharmacol       Date:  2015-05-19       Impact factor: 4.432

Review 2.  Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.

Authors:  Mark D Ericson; Cody J Lensing; Katlyn A Fleming; Katherine N Schlasner; Skye R Doering; Carrie Haskell-Luevano
Journal:  Biochim Biophys Acta Mol Basis Dis       Date:  2017-03-29       Impact factor: 5.187

3.  Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1.

Authors:  Xiaomin Ni; David Heidenreich; Thomas Christott; James Bennett; Moses Moustakim; Paul E Brennan; Oleg Fedorov; Stefan Knapp; Apirat Chaikuad
Journal:  ACS Med Chem Lett       Date:  2019-11-25       Impact factor: 4.345

Review 4.  The melanocortin-4 receptor as target for obesity treatment: a systematic review of emerging pharmacological therapeutic options.

Authors:  L Fani; S Bak; P Delhanty; E F C van Rossum; E L T van den Akker
Journal:  Int J Obes (Lond)       Date:  2013-06-18       Impact factor: 5.095

5.  Synthesis and Structure-Activity Relationships of Substituted Urea Derivatives on Mouse Melanocortin Receptors.

Authors:  Anamika Singh; Johannes Kast; Marvin L S Dirain; Huisuo Huang; Carrie Haskell-Luevano
Journal:  ACS Chem Neurosci       Date:  2015-12-24       Impact factor: 4.418

  5 in total

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