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TRPV1 modulators: structure-activity relationships using a rational combinatorial approach |
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| Authors: | Zaccaro Laura García-López M Teresa González-Muñiz Rosario García-Martínez Carolina Ferrer-Montiel Antonio Albericio Fernando Royo Miriam |
| Affiliation: | a Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain b Istituto di Biostrutture e Bioimmagini CNR, Napoli 80134, Italy c Instituto de Química Medica CSIC, Madrid 28006, Spain d Centro de Biología Molecular y Celular, Universidad Miguel Hernandez, Elche, Alicante 03202, Spain e Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain f CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain g Department of Organic Chemistry, University of Barcelona, Barcelona 08028, 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. |
| Keywords: | Hydantoins Dipeptides Combinatorial library TRPV1 SAR studies |
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