| Literature DB >> 17046253 |
Giovanni Appendino1, Abdellah Ech-Chahad, Alberto Minassi, Sara Bacchiega, Luciano De Petrocellis, Vincenzo Di Marzo.
Abstract
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.Entities:
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Year: 2006 PMID： 17046253 DOI： 10.1016/j.bmcl.2006.09.077
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823