α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists

A series of α-substituted acetamide derivatives of previously reported 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide leads (1, 2) were investigated for antagonism of hTRPV1 activation by capsaicin. Compound 34, which possesses an α-m-tolyl substituent, showed highly potent and selective antagoni...

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Publicat a:Bioorg Med Chem Lett
Autors principals: Tran, Phuong-Thao, Kim, Ho Shin, Ann, Jihyae, Kim, Sung-Eun, Kim, Changhoon, Hong, Mannkyu, Hoang, Van-Hai, Ngo, Van T. H., Hong, Sunhye, Cui, Minghua, Choi, Sun, Blumberg, Peter M., Frank-Foltyn, Robert, Bahrenberg, Gregor, Stockhausen, Hannelore, Christoph, Thomas, Lee, Jeewoo
Format: Artigo
Idioma:Inglês
Publicat: 2015
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Article
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC6957262/
https://ncbi.nlm.nih.gov/pubmed/25937016
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.04.024
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