Discovery and optimization of novel 4-[(aminocarbonyl)amino]- N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

Discovery and optimization of novel 4-[(aminocarbonyl)amino]- N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit. This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (21), p.6237-6240
Hauptverfasser: Pasternak, Alexander, Goble, Stephen D., deJesus, Reynalda K., Hreniuk, Donna L., Chung, Christine C., Tota, Michael R., Mazur, Paul, Feighner, Scott D., Howard, Andrew D., Mills, Sander G., Yang, Lihu
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antagonist
Anti-Obesity Agents - chemical synthesis
Anti-Obesity Agents - chemistry
Anti-Obesity Agents - pharmacology
Benzenesulfonamides
Biological and medical sciences
Cell Line
Drug Design
Drug Inverse Agonism
Ghrelin
Hormones. Endocrine system
Humans
Inverse agonist
Male
Medical sciences
Obesity
Obesity - drug therapy
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Receptors, Ghrelin - antagonists & inhibitors
Receptors, Ghrelin - metabolism
Structure-Activity Relationship
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Beschreibung
Zusammenfassung:This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit. This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.08.076