Novel piperazine urea derivatives as highly potent transient receptor potential vanilloid 1 (TRPV1) antagonists

In order to find new TRPV1 antagonists without obvious side effects, three series of piperazine urea derivatives were designed, synthesized and evaluated using classical TRPV1 ligands BCTC and GRT12360 as leading compounds. [Display omitted] •Three series of new piperazine urea TRPV1 antagonists wer...

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Veröffentlicht in:	Bioorganic chemistry 2021-10, Vol.115, p.105229-105229, Article 105229
Hauptverfasser:	Hu, Jing, Gao, Mengkang, Zhang, Yang, Wang, Yusui, Qiao, Zhenrui, Zhang, Weiya, Wang, Qiang, Yan, Lin, Qian, Hai
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesic Analgesics - chemical synthesis Analgesics - chemistry Analgesics - pharmacology Animals Capsaicin Dose-Response Relationship, Drug Humans Male Molecular Structure Pain - chemically induced Pain - drug therapy Piperazine - chemical synthesis Piperazine - chemistry Piperazine - pharmacology Piperazine urea Rats Rats, Sprague-Dawley Side effect Structure-Activity Relationship Transient receptor potential vanilloid type 1 TRPV Cation Channels - antagonists & inhibitors TRPV Cation Channels - metabolism Urea - analogs & derivatives Urea - chemistry Urea - pharmacology
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