Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X sub(7) antagonists

Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X sub(7) antagonists were identified with simi...

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Published inBioorganic & medicinal chemistry letters Vol. 17; no. 14; pp. 4044 - 4048
Main Authors Carroll, William A, Kalvin, Douglas M, Medrano, Arturo Perez, Florjancic, Alan S, Wang, Ying, Donnelly-Roberts, Diana L, Namovic, Marian T, Grayson, George, Honore, Prisca, Jarvis, Michael F
Format Journal Article
LanguageEnglish
Published 01.07.2007
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Summary:Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X sub(7) antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-1
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.075