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    Bioorg Med Chem Lett. 2011 Jun 15;21(12):3541-5. Epub 2011 May 6.

    TRPV1 modulators: structure-activity relationships using a rational combinatorial approach.

    Zaccaro L, García-López MT, González-Muñiz R, García-Martínez C, Ferrer-Montiel A, Albericio F, Royo M.

    Source

    Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona, Spain.

    Abstract

    A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivity towards NMDA is mainly dictated by the side-chain length and the basic nature of α, ω-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one.

    Copyright © 2011 Elsevier Ltd. All rights reserved.

    PMID:
    21612926
    [PubMed - indexed for MEDLINE]

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