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Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.32 no.9, 2009년, pp.1201 - 1210   SCOPUS
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Design, Synthesis, and Biological Evaluation of Phenylpropanamides as Novel Transient Receptor Potential Valnilloid 1 Antagonists

Li, Fu-Nan    (College of Pharmacy, Seoul National University   ); Kim, Nam-Jung    (College of Pharmacy, Seoul National University   ); Nam, Yeon-Hee    (College of Pharmacy, Seoul National University   ); Kim, Seung-Hee    (College of Pharmacy, Seoul National University   ); Seo, Seung-Yong    (College of Pharmacy, Woosuk University   ); Jeong, Yeon-Su    (Amorepacific R&D Center   ); Kim, Sun-Young    (Amorepacific R&D Center   ); Park, Young-Ho    (Amorepacific R&D Center   ); Suh, Young-Ger    (College of Pharmacy, Seoul National University  );
  • 초록

    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.


  • 주제어

    Synthesis .   Amide .   Analogues .   TRPV1 .   Antagonists.  

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