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4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands

Title
4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands
Authors
Kim, ChanghoonAnn, JihyaeLee, SunhoKim, EunhyeChoi, SunBlumberg, Peter M.Frank-Foltyn, RobertBahrenberg, GregorStockhause, HanneloreChristoph, ThomasLee, Jeewoo
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2018
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link

1464-3391JCR Link
Citation
BIOORGANIC & MEDICINAL CHEMISTRY vol. 26, no. 15, pp. 4509 - 4517
Keywords
Vanilloid receptor 1TRPV1 antagonistsAnalgesic
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
A series of 2-(3,5-substituted 4-aminophenyl)acetamide and propanamide derivatives were investigated as human TRPV1 antagonists. The analysis of the structure-activity relationship indicated that 2-(3,5-dihalo 4-aminophenyl)acetamide analogues displayed excellent antagonism of hTRPV1 activation by capsaicin and showed improved potency compared to the corresponding propanamides. The most potent antagonist (36) exhibited potent and selective antagonism for hTRPV1 not only to capsaicin but also to NADA and elevated temperature; however, it only displayed weak antagonism to low pH. Further studies indicated that oral administration of antagonist 36 blocked the hypothermic effect of capsaicin in vivo but demonstrated hyperthermia at that dose. A docking study of 36 was performed in our established hTRPV1 homology model to understand its binding interactions with the receptor and to compare with that of previous antagonist 1.
DOI
10.1016/j.bmc.2018.07.040
Appears in Collections:
약학대학 > 약학과 > Journal papers
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