Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models. We report the discovery of piperazine urea based...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (8), p.2330-2334
Hauptverfasser:	Hong, Qingmei, Bakshi, Raman K., Palucki, Brenda L., Park, Min K., Ye, Zhixiong, He, Shuwen, Pollard, Patrick G., Sebhat, Iyassu K., Liu, Jian, Guo, Liangqin, Cashen, Doreen E., Martin, William J., 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., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral agonists animal models Animals Biological and medical sciences Biological Availability chemistry Disease Models, Animal Dogs Drug Evaluation, Preclinical Eating - drug effects Erectile dysfunction General and cellular metabolism. Vitamins Haplorhini MC4R Medical sciences Melanocortin subtype-4 receptor Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Obesity Obesity - drug therapy Partial agonist Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments piperazine Piperazines - chemistry Piperazines - pharmacokinetics Piperazines - therapeutic use Rats Rats, Sprague-Dawley Receptor, Melanocortin, Type 4 - agonists Receptor, Melanocortin, Type 4 - genetics Receptor, Melanocortin, Type 4 - metabolism Structure-Activity Relationship urea Urea - analogs & derivatives Urea - chemistry Urea - pharmacokinetics Urea - therapeutic use Urea piperazine
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Zusammenfassung:	We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models. We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.02.090