Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
- 주제(키워드) Analgesic , TRPV1 antagonists , Vanilloid receptor 1
- 등재 SCIE, SCOPUS
- 발행기관 Elsevier Ltd
- 발행년도 2016
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000132372
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.bmcl.2016.06.010
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as hTRPV1 ligands. Through one-carbon elongation in the respective pharmacophoric regions, N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea was identified as a novel and potent TRPV1 antagonistic template. Its representative compound 27 showed a potency comparable to that of lead compound 1. Docking analysis of compound 27 in our hTRPV1 homology model indicated that its binding mode was similar with that of 1S. © 2016 Elsevier Ltd
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