title: TRPV1 modulators: structure-activity relationships using a rational combinatorial approach.
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.
authors: Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona, Spain.
authors: Laura
authors: L
authors: Zaccaro
authors: M Teresa
authors: MT
authors: García-López
authors: Rosario
authors: R
authors: González-Muñiz
authors: Carolina
authors: C
authors: García-Martínez
authors: Antonio
authors: A
authors: Ferrer-Montiel
authors: Fernando
authors: F
authors: Albericio
authors: Miriam
authors: M
authors: Royo