Literature DB >> 18818070

Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.

David L Carlton1, Lissa J Collin-Smith, Alejandro J Daniels, David N Deaton, Aaron S Goetz, Christopher P Laudeman, Thomas R Littleton, David L Musso, Ronda J Ott Morgan, Jerzy R Szewczyk, Cunyu Zhang.   

Abstract

Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists.

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Year:  2008        PMID： 18818070     DOI： 10.1016/j.bmcl.2008.09.033

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


  4 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.  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

3.  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

4.  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
  4 in total

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