Design, synthesis and biological evaluation of novel hydrogen sulfide releasing capsaicin derivatives

A series of new hybrids of capsaicin or dihydrocapsaicin bearing various H2S-releasing moieties were prepared and evaluated in an effort to improve the activity of CAP and alleviate its irritating effects. [Display omitted] Capsaicin (CAP), the prototypical TRPV1 agonist, is the major active compone...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2018-05, Vol.26 (9), p.2632-2639
Hauptverfasser:	Gao, Mingxiang, Li, Jinyu, Nie, Cunbin, Song, Beibei, Yan, Lin, Qian, Hai
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesic Analgesics - chemical synthesis Analgesics - chemistry Analgesics - pharmacology Animals Anticancer Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Capsaicin Capsaicin - analogs & derivatives Capsaicin - chemical synthesis Capsaicin - pharmacology Cell Line, Tumor Doxorubicin - pharmacology Drug Design Gastric Mucosa - drug effects Gastric mucosa irritation HEK293 Cells Humans Hydrogen sulfide Hydrogen Sulfide - metabolism Male Mice Rats Structure-Activity Relationship TRPV Cation Channels - agonists TRPV1 agonist
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