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약학대학
약학과
Journal papers
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2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists
Title
2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists
Authors
Kang J.M.
;
Kwon S.O.
;
Ann J.
;
Lee S.
;
Kim C.
;
Do N.
;
Jeong J.J.
;
Blumberg P.M.
;
Ha H.
;
Vu T.N.L.
;
Yoon S.
;
Choi S.
;
Frank-Foltyn R.
;
Lesch B.
;
Bahrenberg G.
;
Stockhausen H.
;
Christoph T.
;
Lee J.
Ewha Authors
최선
SCOPUS Author ID
최선
Issue Date
2021
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
Citation
Bioorganic and Medicinal Chemistry Letters vol. 48
Keywords
Analgesic
;
TRPV1 Antagonist
;
Vanilloid Receptor 1
Publisher
Elsevier Ltd
Indexed
SCIE; SCOPUS
Document Type
Article
Abstract
A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor. © 2021 Elsevier Ltd
DOI
10.1016/j.bmcl.2021.128266
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