Appendino Giovanni, Ech-Chahad Abdellah, Minassi Alberto, Bacchiega Sara, De Petrocellis Luciano, Di Marzo Vincenzo
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università del Piemonte Orientale, Viale Ferrucci 33, 28100 Novara, Italy.
Bioorg Med Chem Lett. 2007 Jan 1;17(1):132-5. doi: 10.1016/j.bmcl.2006.09.077. Epub 2006 Sep 29.
Starting from ROPA (2), analogues of RTX (1a) modified on the acyl side chain were prepared and evaluated for vanilloid activity in HEK-293 cells over-expressing the human recombinant TRPV1. The ROPA motif provided an enhancement of potency sufficient to expand the range of vanillyl surrogates to structural elements (e.g., an unsubstituted phenyl ring) that afford inactive analogues in compounds from the capsaicin series.
从ROPA(2)开始，制备了在酰基侧链上修饰的RTX(1a)类似物，并在过表达人重组TRPV1的HEK-293细胞中评估其香草酸活性。ROPA基序提供了足够的活性增强，足以将香草基替代物的范围扩展到在辣椒素系列化合物中产生无活性类似物的结构元件(例如未取代的苯环)。
