Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere

Recent preclinical studies demonstrate a role for the prostaglandin E2 (PGE2) subtype 1 (EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and diabetes mellitus. A series of amide and N-acylsulfonamide analogs of a previously described picolinic acid-based human EP1 r...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (1), p.37-41
Hauptverfasser:	Downey, Jason D., Saleh, Sam A., Bridges, Thomas M., Morrison, Ryan D., Scott Daniels, J., Lindsley, Craig W., Breyer, Richard M.
Format:	Artikel
Sprache:	eng
Schlagworte:	agonists Animals Antagonist antagonists chemistry diabetes mellitus Diabetes Mellitus - drug therapy EP1 EP3 Half-Life Humans hypertension Hypertension - drug therapy Mice Microsomes, Liver - metabolism pathophysiology Prostaglandin E2 prostaglandins Pyridines - chemistry Pyridines - pharmacokinetics Pyridines - therapeutic use Receptors, Prostaglandin E, EP1 Subtype - antagonists & inhibitors Receptors, Prostaglandin E, EP1 Subtype - metabolism Receptors, Prostaglandin E, EP3 Subtype - antagonists & inhibitors Receptors, Prostaglandin E, EP3 Subtype - metabolism Receptors, Thromboxane - antagonists & inhibitors Receptors, Thromboxane - metabolism Structure-Activity Relationship Sulfonamides - chemistry Sulfonamides - pharmacokinetics Sulfonamides - therapeutic use
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