Design, synthesis, and biological evaluation of phenylpropanamides as novel transient receptor potential valnilloid 1 antagonists

Synthesis and structure-activity relationship of N-benzyl-3-phenylpropanamides as transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of substituents such as halide, ester, nitro, and alkyl groups at 2 or 3-position of 4-(methylsulfonylamino) benzyl unit were examin...

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Bibliographic Details
Published in:Archives of pharmacal research 2009, 32(9), , pp.1201-1210
Main Authors: Li, Fu-Nan, Kim, Nam-Jung, Nam, Yeon-Hee, Kim, Seung-Hee, Seo, Seung-Yong, Jeong, Yeon-Su, Kim, Sun-Young, Park, Young-Ho, Suh, Young-Ger
Format: Article
Language:English
Subjects:
Medicine
Pharmacology/Toxicology
Pharmacy
약학
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Summary:Synthesis and structure-activity relationship of N-benzyl-3-phenylpropanamides as transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of substituents such as halide, ester, nitro, and alkyl groups at 2 or 3-position of 4-(methylsulfonylamino) benzyl unit were examined. These compounds exhibited potent 45 Ca 2+ uptake inhibition in rat DRG neuron via TRPV1 blockade. Especially compound 28c , has been identified as a potent antagonist with IC 50 of 38 nM.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-009-1903-9