Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity

We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (22), p.6524-6532
Hauptverfasser:	He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Bakshi, Raman K., Hong, Qingmei, Dellureficio, James P., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Reibarkh, Mikhail, Holmes, Mark A., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Agonist Animals Biological and medical sciences Chromatography, High Pressure Liquid Disease Models, Animal General and cellular metabolism. Vitamins MC4R Medical sciences Melanocortin subtype-4 receptor Mice Mice, Knockout Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Obesity Obesity - drug therapy Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Privileged structure Rats Receptor, Melanocortin, Type 4 - agonists Receptor, Melanocortin, Type 4 - genetics Spiroindane Structure-Activity Relationship Triazole Triazoles - chemistry Triazoles - pharmacology Triazoles - therapeutic use
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