Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1.
作者： Yan Liu , Chen Liao , Jiaqi Zhou , Chunxia Liu , Qifei Li
DOI: 10.1016/J.BMC.2018.08.002
关键词: Pharmacology 、 Propanoic acid 、 In vivo 、 Transient receptor potential channel 、 Chemistry 、 Benzodiazepine 、 Solubility 、 TRPV1 、 Analgesic 、 Capsaicin
摘要: A new series of derivatives 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 investigated TRPV1 antagonistic activity in vitro, sedative vivo 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), a potent with good
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