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本文引用的文献

1
Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.2-(3-氟-4-甲基磺酰胺基苯基)丙酰胺的苄基C区域类似物作为有效的TRPV1拮抗剂的构效关系
Bioorg Med Chem. 2015 Nov 1;23(21):6844-54. doi: 10.1016/j.bmc.2015.10.001. Epub 2015 Oct 9.
2
α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists.α-取代的2-(3-氟-4-甲基磺酰胺基苯基)乙酰胺作为有效的瞬时受体电位香草酸亚型1（TRPV1）拮抗剂。
Bioorg Med Chem Lett. 2015 Jun 1;25(11):2326-30. doi: 10.1016/j.bmcl.2015.04.024. Epub 2015 Apr 12.
3
Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014).瞬时受体电位香草酸亚型1拮抗剂：专利综述（2011 - 2014年）
Expert Opin Ther Pat. 2015 Mar;25(3):291-318. doi: 10.1517/13543776.2015.1008449.
4
Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.2-(3-氟-4-甲基磺酰氨基苯基)丙酰胺的吡啶C-区域类似物作为有效的瞬时受体电位香草酸亚型1（TRPV1）拮抗剂
Eur J Med Chem. 2015 Mar 26;93:101-8. doi: 10.1016/j.ejmech.2015.02.001. Epub 2015 Feb 2.
5
Structural insight into tetrameric hTRPV1 from homology modeling, molecular docking, molecular dynamics simulation, virtual screening, and bioassay validations.通过同源建模、分子对接、分子动力学模拟、虚拟筛选和生物测定验证对四聚体hTRPV1的结构洞察。
J Chem Inf Model. 2015 Mar 23;55(3):572-88. doi: 10.1021/ci5007189. Epub 2015 Feb 18.
6
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.2-(3-氟-4-甲磺酰氨基苯基)丙酰胺的2-芳基取代吡啶C区域类似物作为高效TRPV1拮抗剂。
Bioorg Med Chem Lett. 2014 Aug 15;24(16):4044-7. doi: 10.1016/j.bmcl.2014.05.072. Epub 2014 Jun 2.
7
2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.2-(3-氟-4-甲基磺酰氨基苯基)丙酰胺的2-烷基/烯基取代吡啶C区类似物作为高效TRPV1拮抗剂。
Bioorg Med Chem Lett. 2014 Aug 15;24(16):4039-43. doi: 10.1016/j.bmcl.2014.05.074. Epub 2014 Jun 2.
8
Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions.瞬时受体电位香草酸亚型1（TRPV1）通道的调控：当前临床试验及聚焦于神经系统疾病的近期专利
Recent Pat CNS Drug Discov. 2013 Dec;8(3):180-204. doi: 10.2174/1574889808666131209124012.
9
TRPV1 structures in distinct conformations reveal activation mechanisms.不同构象的 TRPV1 结构揭示了其激活机制。
Nature. 2013 Dec 5;504(7478):113-8. doi: 10.1038/nature12823.
10
Structure of the TRPV1 ion channel determined by electron cryo-microscopy.电子冷冻显微镜解析 TRPV1 离子通道结构。
Nature. 2013 Dec 5;504(7478):107-12. doi: 10.1038/nature12822.

发现N-（3-氟-4-甲基磺酰胺基甲基苯基）脲作为一种有效的TRPV1拮抗剂模板。

Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.

作者信息

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

机构信息

Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.

Shenyang Pharmaceutical University, Shenyang 110016, China.

出版信息

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3603-7. doi: 10.1016/j.bmcl.2016.06.010. Epub 2016 Jun 7.

DOI:10.1016/j.bmcl.2016.06.010
PMID:27317643
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6957248/
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.

摘要

研究了原型拮抗剂1及其脲替代物的一系列同源类似物作为hTRPV1配体。通过在各自药效基团区域进行单碳延长，确定N-(3-氟-4-甲基磺酰胺基甲基苯基)脲为一种新型强效TRPV1拮抗模板。其代表性化合物27显示出与先导化合物1相当的效力。在我们的hTRPV1同源模型中对化合物27进行对接分析表明，其结合模式与1S相似。

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