Impact factor: 2.554, Impact factor a 5 anni: 2.539
Url: Non disponibile.
Parole chiave: Combinatorial Library, Dipeptides, Hydantoins, Sar Studies, Trpv1, Lysine, Molecular Scaffold, N Methyl Dextro Aspartic Acid Receptor, N Methyl Dextro Aspartic Acid Receptor Blocking Agent, Pyridine, Tryptophan, Vanilloid Receptor 1, Vanilloid Receptor 1 Antagonist, Amino Terminal Sequence, Carboxy Terminal Sequence, Drug Potency, Drug Selectivity, Drug Synthesis, Structure Activity Relation, Anti-Inflammatory Agents, Combinatorial Chemistry Techniques, Humans, Indoles, Molecular Structure, Small Molecule Libraries, Structure-Activity Relationship, Trpv Cation Channels,
Affiliazioni:
*** IBB - CNR *** Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain Istituto di Biostrutture e Bioimmagini CNR, Napoli 80134, Italy Instituto de Química Medica CSIC, Madrid 28006, Spain Centro de Biología Molecular Y Celular, Universidad Miguel Hernandez, Elche, Alicante 03202, Spain Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain Instituto de Qu mica Medica CSIC, Madrid 28006, Spain Centro de Biolog a Molecular Y Celular, Universidad Miguel Hernandez, Elche, Alicante 03202, Spain
Riferimenti:
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Wiley-VCH Verlag GmbH: KGaA, Weinheim (Germany)
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Caterina, M. J., Schumacher, M. A., Tominaga, M., Rosen, T. A., Levine, J. D., Julius, D., (1997) Nature, 389, p. 81
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Nandy, J. P., Prakesch, M., Khadem, S., Reddy, P. T., Sharma, U., Arya, P., (2009) Chem. Rev., 109, p. 1999
Kates, S. A., Albericio, F., (2000) Solid-Phase Synthesis. A Practical Guide, , Marcel Dekker: New York (NY, USA)
Carpino, L. A., Han, G. Y., (1972) J. Org. Chem., 37, p. 3404
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 alpha, omega-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one. (C) 2011 Elsevier Ltd. All rights reserved.
27 Records (27 escludendo Abstract e Conferenze). Impact factor totale: 116.841 (116.841 escludendo Abstract e Conferenze). Impact factor a 5 anni totale: 122.283 (122.283 escludendo Abstract e Conferenze).
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