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Your search keyword '"Treanor, James J.S."' showing total 2 results
Start Over Author "Treanor, James J.S." Topic pharmaceutical chemistry
2 results on '"Treanor, James J.S."'

1. Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists

Author

Stec, Markian M., Bo, Yunxin, Chakrabarti, Partha P., Liao, Lillian, Ncube, Mqhele, Tamayo, Nuria, Tamir, Rami, Gavva, Narender R., Treanor, James J.S., and Norman, Mark H.

Subjects
*PYRIMIDINES, *DRUG solubility, *PHARMACOKINETICS, *ORGANIC compounds, *PHARMACEUTICAL chemistry, *BIOORGANIC chemistry
Abstract

Abstract: Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of 1. Compounds were identified that maintained potency, had good pharmacokinetic properties, and improved solubility relative to 1. [Copyright &y& Elsevier]

Published
2008
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2. Structure–activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists

Author

Gore, Vijay K., Ma, Vu V., Tamir, Rami, Gavva, Narender R., Treanor, James J.S., and Norman, Mark H.

Subjects
*IMIDAZOLES, *BENZIMIDAZOLES, *CAPSAICIN, *PHARMACEUTICAL chemistry
Abstract

Abstract: A novel series of 4,5-biarylimidazoles as TRPV1 antagonists were designed based on the previously reported 4,6-disubstituted benzimidazole series. The analogs were evaluated for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. These studies led to the identification of a highly potent and orally bioavailable TRPV1 antagonist, imidazole 33. [Copyright &y& Elsevier]

Published
2007
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