跳转至内容
Merck
  • Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.

Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.

Bioorganic & medicinal chemistry letters (2012-01-20)
Enrico Morera, Luciano De Petrocellis, Ludovica Morera, Aniello Schiano Moriello, Marianna Nalli, Vincenzo Di Marzo, Giorgio Ortar
摘要

In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, a series of nineteen analogues (1b-5) of racemic [6]-gingerol (1a) was synthesized and tested on TRPV1 and TRPA1 channels. The exploration of the structure-activity relationships, by modulating the three pharmacophoric regions of [6]-gingerol, led to the identification of some selective TRPV1 agonists/desensitizers of TRPV1 channels (3a, 3f, and 4) and of some full TRPA1 antagonists (2c, 2d, 3b, and 3d).

材料
货号
品牌
产品描述

Sigma-Aldrich
辣椒素, ≥95%, from Capsicum sp.
Sigma-Aldrich
异硫氰酸烯丙酯, 95%
Sigma-Aldrich
辣椒素, natural
Sigma-Aldrich
辣椒素, from Capsicum sp., ≥50% (HPLC)
Sigma-Aldrich
异硫氰酸烯丙酯, ≥95%, FCC
Supelco
异硫氰酸烯丙酯, PESTANAL®, analytical standard