Synthesis of Analogues of  BCTC  Incorporating a Pyrrolidinyl Linker and Biological Evaluation as Transient Receptor Potential Vanilloid 1 Antagonists | Zendy

Yan Lin | Zendy; Wang Jingjie | Zendy; Pan Miaobo | Zendy; Qiu Qianqian | Zendy; Huang Wenlong | Zendy; Qian Hai | Zendy

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Synthesis of Analogues of BCTC Incorporating a Pyrrolidinyl Linker and Biological Evaluation as Transient Receptor Potential Vanilloid 1 Antagonists

Author(s) -

Yan Lin,

Wang Jingjie,

Pan Miaobo,

Qiu Qianqian,

Huang Wenlong,

Qian Hai

Publication year - 2016

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.12661

Subject(s) - antagonism , trpv1 , antagonist , linker , chemistry , capsaicin , in vivo , analgesic , transient receptor potential channel , pharmacology , in vitro , receptor , biochemistry , biology , microbiology and biotechnology , computer science , operating system

A series of novel pyrrolidinyl linker TRPV 1 antagonists were prepared in an effort to lower the hyperthermic side‐effects of first‐generation antagonist BCTC . These compounds were investigated for antagonism of h TRPV 1 activation by capsaicin and acid in vitro . Preliminary results suggested the compounds 10a , 10b , 10c and 10j had favorable TRPV 1 antagonism activity. In further studies in vivo , 10b , comparable to BCTC , showed potent analgesic activity in capsaicin‐induced and heat‐induced pain models. In addition, 10b indicated a reduced risk of body temperature elevation. All of these demonstrated that 10b can be considered as a safe candidate for the further development of analgesic drugs.

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