Literature DB >> 17544282

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.

Joe A Tran1, Fabio C Tucci, Wanlong Jiang, Dragan Marinkovic, Caroline W Chen, Melissa Arellano, Stacy Markison, Beth A Fleck, Jenny Wen, Nicole S White, Joseph Pontillo, John Saunders, Daniel Marks, Sam R Hoare, Ajay Madan, Alan C Foster, Chen Chen.   

Abstract

A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good oral bioavailabilities. In addition, 12e demonstrated in vivo efficacy in a murine cachexia model.

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Year:  2007        PMID: 17544282     DOI: 10.1016/j.bmc.2007.05.026

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Rank order entropy: why one metric is not enough.

Authors:  Margaret R McLellan; M Dominic Ryan; Curt M Breneman
Journal:  J Chem Inf Model       Date:  2011-08-29       Impact factor: 4.956

Review 2.  The ups and downs of structure-activity landscapes.

Authors:  Rajarshi Guha
Journal:  Methods Mol Biol       Date:  2011

3.  Val103Ile polymorphism of the melanocortin-4 receptor gene (MC4R) in cancer cachexia.

Authors:  Susanne Knoll; Sabiene Zimmer; Anke Hinney; André Scherag; Andreas Neubauer; Johannes Hebebrand
Journal:  BMC Cancer       Date:  2008-03-31       Impact factor: 4.430

  3 in total

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