Literature DB >> 20347296

Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

Mark Hadden1, Allan Goodman, Cheng Guo, Peter R Guzzo, Alan J Henderson, Kevin Pattamana, Megan Ruenz, Bruce J Sargent, Brian Swenson, Larry Yet, Jian Liu, Shuwen He, Iyassu K Sebhat, Linus S Lin, Constantin Tamvakopoulos, Qianping Peng, Yanqing Kan, Oksana Palyha, Theresa M Kelly, Xiao-Ming Guan, Joseph M Metzger, Marc L Reitman, Ravi P Nargund.   

Abstract

SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20347296     DOI： 10.1016/j.bmcl.2010.03.028

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


  5 in total

Review 1.  Bombesin receptor subtype 3 as a potential target for obesity and diabetes.

Authors:  Nieves González; Paola Moreno; Robert T Jensen
Journal:  Expert Opin Ther Targets       Date:  2015-06-12       Impact factor: 6.902

2.  A selective human bombesin receptor subtype-3 peptide agonist mediates CREB phosphorylation and transactivation.

Authors:  Xiaoqun Qin; Xiangping Qu; David Coy; H Christian Weber
Journal:  J Mol Neurosci       Date:  2011-11-30       Impact factor: 3.444

3.  Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.

Authors:  Ping Liu; Thomas J Lanza; Marc Chioda; Carrie Jones; Harry R Chobanian; Yan Guo; Linda Chang; Theresa M Kelly; Yanqing Kan; Oksana Palyha; Xiao-Ming Guan; Donald J Marsh; Joseph M Metzger; Katie Ramsay; Sheng-Ping Wang; Alison M Strack; Randy Miller; Jianmei Pang; Kathy Lyons; Jasminka Dragovic; Jian G Ning; Wes A Schafer; Christopher J Welch; Xiaoyi Gong; Ying-Duo Gao; Viktor Hornak; Richard G Ball; Nancy Tsou; Marc L Reitman; Matthew J Wyvratt; Ravi P Nargund; Linus S Lin
Journal:  ACS Med Chem Lett       Date:  2011-10-03       Impact factor: 4.345

4.  Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.

Authors:  Iyassu K Sebhat; Christopher Franklin; Michael M-C Lo; David Chen; James P Jewell; Randy Miller; Jianmei Pang; Oksana Palyha; Yanqing Kan; Theresa M Kelly; Xiao-Ming Guan; Donald J Marsh; Jennifer A Kosinski; Joseph M Metzger; Kathryn Lyons; Jasminka Dragovic; Peter R Guzzo; Alan J Henderson; Marc L Reitman; Ravi P Nargund; Matthew J Wyvratt; Linus S Lin
Journal:  ACS Med Chem Lett       Date:  2010-10-18       Impact factor: 4.345

5.  Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.

Authors:  Harry R Chobanian; Yan Guo; Ping Liu; Marc Chioda; Thomas J Lanza; Linda Chang; Theresa M Kelly; Yanqing Kan; Oksana Palyha; Xiao-Ming Guan; Donald J Marsh; Joseph M Metzger; Judith N Gorski; Kate Raustad; Sheng-Ping Wang; Alison M Strack; Randy Miller; Jianmei Pang; Maria Madeira; Kathy Lyons; Jasminka Dragovic; Marc L Reitman; Ravi P Nargund; Linus S Lin
Journal:  ACS Med Chem Lett       Date:  2012-01-21       Impact factor: 4.345
  5 in total

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