Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists

Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of clinical candidate AMG 517. Clinical candidate AMG 517 ( 1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-09, Vol.18 (18), p.5118-5122
Hauptverfasser:	Stec, Markian M., Bo, Yunxin, Chakrabarti, Partha P., Liao, Lillian, Ncube, Mqhele, Tamayo, Nuria, Tamir, Rami, Gavva, Narender R., Treanor, James J.S., Norman, Mark H.
Format:	Artikel
Sprache:	eng
Schlagworte:	AMG 517 Analgesics Animals Benzothiazoles - pharmacokinetics Benzothiazoles - pharmacology Biological and medical sciences Combinatorial Chemistry Techniques Ion channel Medical sciences Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Rats Rats, Sprague-Dawley Structure-Activity Relationship Transient receptor potential TRPV Cation Channels - antagonists & inhibitors TRPV1 Vanilloid receptor VR1
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