Literature DB >> 20598533

Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.

Qingmei Hong1, Raman K Bakshi, James Dellureficio, Shuwen He, Zhixiong Ye, Peter H Dobbelaar, Iyassu K Sebhat, Liangqin Guo, Jian Liu, Tianying Jian, Rui Tang, Rubana N Kalyani, Tanya Macneil, Aurawan Vongs, Charles I Rosenblum, David H Weinberg, Qingping Peng, Constantin Tamvakopoulos, Randy R Miller, Ralph A Stearns, Doreen Cashen, Willian J Martin, Airu S Chen, Joseph M Metzger, Howard Y Chen, Allison M Strack, Tung M Fong, Euan Maclntyre, Lex H T Van der Ploeg, Matthew J Wyvratt, Ravi P Nargund.   

Abstract

Design, syntheses and structure-activity relationships of N-acetylated piperazine privileged structures containing MC4R agonist compounds were described. The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20598533     DOI: 10.1016/j.bmcl.2010.06.038

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


  3 in total

1.  Conformational study on cyclic melanocortin ligands and new insight into their binding mode at the MC4 receptor.

Authors:  Paolo Grieco; Diego Brancaccio; Ettore Novellino; Victor J Hruby; Alfonso Carotenuto
Journal:  Eur J Med Chem       Date:  2011-05-23       Impact factor: 6.514

2.  Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.

Authors:  Katlyn A Fleming; Katie T Freeman; Mike D Powers; Radleigh G Santos; Ginamarie Debevec; Marc A Giulianotti; Richard A Houghten; Skye R Doering; Clemencia Pinilla; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2019-02-28       Impact factor: 7.446

Review 3.  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 in total

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