Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor
In: Bioorganic & medicinal chemistry letters (Print), Jg. 14 (2004), Heft 17, S. 4417-4423
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Zugriff:
SAR studies on a series of piperazinebenzenes directed toward the human melanocortin-4 receptor resulted in potent MC4R agonists. Replacement of the triazole moiety of an initial lead 4 by a basic nitrogen baring a lipophilic side-chain increased the binding affinities of these compounds. Analogs bearing an additional hetero-atom in the side-chain possessed good agonist potency. Thus, llh had a Ki of 11 nM, and 13g exhibited an EC50 of 3.8nM and a Ki of 6.4 nM.
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Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor
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Autor/in / Beteiligte Person: | PONTILLO, Joseph ; TRAN, Joseph A ; TUCCI, Fabio C ; WANLONG, JIANG ; CHEN, Caroline W ; WHITE, Nicole S ; FOSTER, Alan C ; CHEN, CHEN ; ARELLANO, Melissa ; FLECK, Beth A ; HUNTLEY, Rajesh ; MARINKOVIC, Dragan ; LANIER, Marion ; NELSON, Jodie ; PARKER, Jessica ; SAUNDERS, John |
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Zeitschrift: | Bioorganic & medicinal chemistry letters (Print), Jg. 14 (2004), Heft 17, S. 4417-4423 |
Veröffentlichung: | Oxford: Elsevier, 2004 |
Medientyp: | academicJournal |
Umfang: | print, |
ISSN: | 0960-894X (print) |
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