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Bioorg Med Chem. 2018 Aug 15;26(15):4567-4573. doi: 10.1016/j.bmc.2018.08.002. Epub 2018 Aug 1.

Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1.

Author information

1
School of Pharmacy, Chongqing Medical University, 1 Yixueyuan Road, Chongqing 400016, PR China. Electronic address: y.liu@cqmu.edu.cn.
2
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
3
School of Pharmacy, Chongqing Medical University, 1 Yixueyuan Road, Chongqing 400016, PR China.
4
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China. Electronic address: qianhai24@cpu.edu.cn.

Abstract

A new series of derivatives of 3-(7-chloro-5-(2-fluorophenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)propanoic acid were designed and synthesized as analgesic modulating for Transient receptor potential vanilloid 1. They were investigated for TRPV1 antagonistic activity in vitro, analgesic activity and sedative activity in vivo and aqueous solubility. Preliminary studies identified 3-(7-chloro-5-(2-fluorophenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-N,N-dimethylpropanamide(Compound 11), as a potent analgesic modulating for TRPV1 with potent activity and good aqueous solubility.

KEYWORDS:

Analgesic; Benzodiazepine; Sedation; Transient receptor potential vanilloid 1

PMID:
30093345
DOI:
10.1016/j.bmc.2018.08.002
[Indexed for MEDLINE]

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