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.
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists. Publishing Authors By Initials
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists. Journal Published:
PUBLICATION TYPE: Journal Article
Journal: Bioorganic & medicinal chemistry letters
VOLUME: 17
Page Numbers: 5825-30
Journal Abbreviation: Bioorg. Med. Chem. Lett.
ISSN: 0960-894X
DAY: 25
MONTH: 08
YEAR: 2007
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists. Information
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LANGUAGE: eng
NlmUniqueID: 9107377
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Grant and Affiliation Information for Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
AFFILIATION: Chemistry Research & Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. vgore@amgen.com
Country: England
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MEDLINETA: Bioorg Med Chem Lett
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