Bioorganic and Medicinal Chemistry Letters p. 3603 - 3607 (2016)
Update date:2022-08-03
Topics:
Ann, Jihyae
Sun, Wei
Zhou, Xing
Jung, Aeran
Baek, Jisoo
Lee, Sunho
Kim, Changhoon
Yoon, Suyoung
Hong, Sunhye
Choi, Sun
Turcios, Noe A.
Herold, Brienna K.A.
Esch, Timothy E.
Lewin, Nancy E.
Abramovitz, Adelle
Pearce, Larry V.
Blumberg, Peter M.
Lee, Jeewoo
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.
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Doi:10.1016/S0960-894X(01)00686-2
(2002)Doi:10.1016/S0022-328X(00)00417-4
(2000)Doi:10.1021/jf0007941
(2001)Doi:10.1007/s10593-008-0079-4
(2008)Doi:10.1039/b006757l
(2000)Doi:10.1007/BF00744562
(1971)
