Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370790 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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.
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Authors
Laura Zaccaro, M. Teresa García-López, Rosario González-Muñiz, Carolina García-Martínez, Antonio Ferrer-Montiel, Fernando Albericio, Miriam Royo,