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Discovery of indane propanamides as potent and selective TRPV1 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Feb 01; Vol. 30 (3), pp. 126838. Date of Electronic Publication: 2019 Dec 03. - Publication Year :
- 2020
-
Abstract
- A series of indane-type acetamide and propanamide analogues were investigated as TRPV1 antagonists. The analysis of structure-activity relationship indicated that indane A-region analogues exhibited better antagonism than did the corresponding 2,3-dihydrobenzofuran and 1,3-benzodioxole surrogates. Among them, antagonist 36 exhibited potent and selective antagonism toward capsaicin for hTRPV1 and mTRPV1. Further, in vivo studies indicated that antagonist 36 showed excellent analgesic activity in both phases of the formalin mouse pain model and inhibited the pain behavior completely at a dose of 1 mg/kg in the 2nd phase.<br /> (Copyright © 2019. Published by Elsevier Ltd.)
- Subjects :
- Acetamides chemistry
Acetamides metabolism
Acetamides therapeutic use
Amides metabolism
Amides therapeutic use
Analgesics chemistry
Analgesics therapeutic use
Animals
Capsaicin chemistry
Capsaicin metabolism
Drug Design
Drug Evaluation, Preclinical
Humans
Mice
Pain chemically induced
Pain drug therapy
Pyridines chemistry
Structure-Activity Relationship
TRPV Cation Channels metabolism
Amides chemistry
Indans chemistry
TRPV Cation Channels antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 30
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 31864799
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.126838