ArticleBioorganic & medicinal chemistry letters2016
Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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The trial behind it
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Who cites it
8 citing papers in PubMed.
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Cryo-EM as a powerful tool for drug discovery.Bioorganic & medicinal chemistry letters · 2020Review
- Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.European journal of medicinal chemistry · 2019Article
- TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds' pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development.Acta physiologica (Oxford, England) · 2018Article
- Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).Journal of medicinal chemistry · 2017Article
- Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.Bioorganic & medicinal chemistry letters · 2017Article
- t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.Bioorganic & medicinal chemistry · 2017Article
- TRPV1: A Target for Rational Drug Design.Pharmaceuticals (Basel, Switzerland) · 2016Review
Corrections and comments
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Authors and funding
18 authors.
Funding
Abstract
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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Registered trials
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