1021938-86-2Relevant academic research and scientific papers
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
Liu, Jian,He, Shuwen,Jian, Tianying,Dobbelaar, Peter H.,Sebhat, Iyassu K.,Lin, Linus S.,Goodman, Allan,Guo, Cheng,Guzzo, Peter R.,Hadden, Mark,Henderson, Alan J.,Pattamana, Kevin,Ruenz, Megan,Sargent, Bruce J,Swenson, Brian,Yet, Larry,Tamvakopoulos, Constantin,Peng, Qianping,Pan, Jie,Kan, Yanqing,Palyha, Oksana,Kelly, Theresa M.,Guan, Xiao-Ming,Howard, Andrew D.,Marsh, Donald J.,Metzger, Joseph M.,Reitman, Marc L.,Wyvratt, Matthew J.,Nargund, Ravi P.
scheme or table, p. 2074 - 2077 (2010/07/03)
This Letter describes a series of potent and selective BRS-3 agonists containing a biarylethylimidazole pharmacophore. Extensive SAR studies were carried out with different aryl substitutions. This work led to the identification of a compound 2-{2-[4-(pyridin-2-yl)phenyl]ethyl}-5-(2,2-dimethylbutyl)-1H-imidazole 9 with excellent binding affinity (IC50 = 18 nM, hBRS-3) and functional agonist activity (EC50 = 47 nM, 99% activation). After oral administration, compound 9 had sufficient exposure in diet induced obese mice to demonstrate efficacy in lowering food intake and body weight via BRS-3 activation.
SUBSTITUTED IMIDAZOLES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS
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Page/Page column 73, (2008/12/05)
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
