TRPV1 modulators: Structure-activity relationships using a rational combinatorial approach (170 visite)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2011 Jun 15; 21(12): 3541-3545.
Tipo di articolo: Journal Article,
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:
Caterina, M.J., Schumacher, M.A., Tominaga, M., Rosen, T.A., Levine, J.D., Julius, D., (1997) Nature, 389, p. 81
Caterina, M.J., Leffler, A., Malmberg, A.B., Martin, W.J., Trafton, J., Petersen-Zeitz, K.R., Koltzenburg, M., Julius, D., (2000) Science, 288, p. 306
Cortright, D.N., Krause, J.E., Broom, D.C., (2007) Biochim. Biophys. Acta, 1772, p. 978
Palazzo, E., Rossi, F., Maione, S., (2008) Mol. Cell. Endocrinol., 286, pp. S79
Willis Jr., W.D., (2009) Exp. Brain Res., 196, p. 5
Cortright, D.N., Szallasi, A., (2009) Curr. Pharm. Des., 15, p. 1736
Tominaga, M., Caterina, M.J., Malmberg, A.B., Rosen, T.A., Gilbert, H., Skinner, K., Raumann, B.E., Julius, D., (1998) Neuron, 21, p. 531
Ross, R.A., (2003) Br. J. Pharmacol., 140, p. 790
Hwang, S.W., Cho, H., Kwak, J., Lee, S.Y., Kang, C.J., Jung, J., Cho, S., Oh, U., (2000) Proc. Natl. Acad. Sci. U.S.A., 97, p. 6155
Huang, J., Zhang, X., McNaughton, P.A., (2006) Curr. Neuropharmacol., 4, p. 197
Silva, C., Silva, J., Castro, H., Reis, F., Dinis, P., Avelino, A., Cruz, F., (2007) BMC Urol., 7, p. 9
Brooks, S.M., (2008) Lung, 186, pp. S88
Holzer, P., (2008) Gut, 57, p. 882
Shimizu, T., (2009) Brain Nerve., 61, p. 949
Bley, K.R., (2004) Expert. Opin. Investig. Drugs, 13, p. 1445
Knotkova, H., Pappagallo, M., Szallasi, A., (2008) Clin. J. Pain, 24, p. 142
Conway, S., (2008) J. Chem. Soc. Rev., 37, p. 1530
Pal, M., Angaru, S., Kodimuthali, A., Dhingra, N., (2009) Curr. Pharm. Des., 15, p. 1008
Broad, L.M., Keding, S.J., Blanco, M., (2008) J. Curr. Top. Med. Chem., 8, p. 1431
Szallasi, A., Cortright, D.N., Blum, C.A., Eid, S.R., (2007) Nat. Rev. Drug Discov., 6, p. 357
Kym, P.R., Kort, M.E., Hutchins, C.W., (2009) Biochem. Pharmacol., 78, p. 211
Szallasi, A., Blumberg, P.M., (1999) Pharmacol. Rev., 51, p. 159
Szallasi, A., Appendino, G., (2004) J. Med. Chem., 47, p. 2717
McLeod, R.L., Correll, C.C., Jia, Y., Anthes, J.C., (2008) Lung, 186, pp. S59
Gunthorpe, M.J., Chizh, B.A., (2009) Drug Discovery Today, 14, p. 56
Wong, G.Y., Gavva, N.R., (2009) Brain Res. Rev., 60, p. 267
Bonache, M.A., Garcia-Martinez, C., De Garcia Diego, L., Carreno, C., Perez De Vega, M.J., Garcia-Lopez, M.T., Ferrer-Montiel, A., Gonzalez-Muniz, R., (2006) ChemMedChem, 1, p. 429
(2008) The Power of Functional Resins in Organic Chemistry, , Tulla-Puche, J., Albericio, F., Eds.
Wiley-VCH Verlag GmbH: KGaA, Weinheim (Germany)
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
Vazques, J., Royo, M., Albericio, F., (2004) Lett. Org. Chem., 1, p. 224
Chen, S., Xu, J., (1992) Tetrahedron Lett., 33, p. 647
Farrera-Sinfreu, J., Royo, M., Albericio, F., (2002) Tetrahedron Lett., 43, p. 7813
noteUR - http://www.scopus.com/inward/record.url?eid=2-s2.0-79957876139&partnerID=40&md5=8205ccf9ba4dadcff7dc556527ba886d
Caterina, M. J., Schumacher, M. A., Tominaga, M., Rosen, T. A., Levine, J. D., Julius, D., (1997) Nature, 389, p. 81
Caterina, M. J., Leffler, A., Malmberg, A. B., Martin, W. J., Trafton, J., Petersen-Zeitz, K. R., Koltzenburg, M., Julius, D., (2000) Science, 288, p. 306
Cortright, D. N., Krause, J. E., Broom, D. C., (2007) Biochim. Biophys. Acta, 1772, p. 978
Willis Jr., W. D., (2009) Exp. Brain Res., 196, p. 5
Cortright, D. N., Szallasi, A., (2009) Curr. Pharm. Des., 15, p. 1736
Ross, R. A., (2003) Br. J. Pharmacol., 140, p. 790
Hwang, S. W., Cho, H., Kwak, J., Lee, S. Y., Kang, C. J., Jung, J., Cho, S., Oh, U., (2000) Proc. Natl. Acad. Sci. U. S. A., 97, p. 6155
Brooks, S. M., (2008) Lung, 186, pp. S88
Bley, K. R., (2004) Expert. Opin. Investig. Drugs, 13, p. 1445
Broad, L. M., Keding, S. J., Blanco, M., (2008) J. Curr. Top. Med. Chem., 8, p. 1431
Kym, P. R., Kort, M. E., Hutchins, C. W., (2009) Biochem. Pharmacol., 78, p. 211
McLeod, R. L., Correll, C. C., Jia, Y., Anthes, J. C., (2008) Lung, 186, pp. S59
Gunthorpe, M. J., Chizh, B. A., (2009) Drug Discovery Today, 14, p. 56
Wong, G. Y., Gavva, N. R., (2009) Brain Res. Rev., 60, p. 267
Bonache, M. A., Garcia-Martinez, C., De Garcia Diego, L., Carreno, C., Perez De Vega, M. J., Garcia-Lopez, M. T., Ferrer-Montiel, A., Gonzalez-Muniz, R., (2006) ChemMedChem, 1, p. 429
(2008) The Power of Functional Resins in Organic Chemistry, , Tulla-Puche, J., Albericio, F., Eds.
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
noteUR - http: //www. scopus. com/inward/record. url? eid=2-s2. 0-79957876139&partnerID=40&md5=8205ccf9ba4dadcff7dc556527ba886d
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2011 Jun 15; 21(12): 3541-3545.
Tipo di articolo: Journal Article,
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:
Caterina, M.J., Schumacher, M.A., Tominaga, M., Rosen, T.A., Levine, J.D., Julius, D., (1997) Nature, 389, p. 81
Caterina, M.J., Leffler, A., Malmberg, A.B., Martin, W.J., Trafton, J., Petersen-Zeitz, K.R., Koltzenburg, M., Julius, D., (2000) Science, 288, p. 306
Cortright, D.N., Krause, J.E., Broom, D.C., (2007) Biochim. Biophys. Acta, 1772, p. 978
Palazzo, E., Rossi, F., Maione, S., (2008) Mol. Cell. Endocrinol., 286, pp. S79
Willis Jr., W.D., (2009) Exp. Brain Res., 196, p. 5
Cortright, D.N., Szallasi, A., (2009) Curr. Pharm. Des., 15, p. 1736
Tominaga, M., Caterina, M.J., Malmberg, A.B., Rosen, T.A., Gilbert, H., Skinner, K., Raumann, B.E., Julius, D., (1998) Neuron, 21, p. 531
Ross, R.A., (2003) Br. J. Pharmacol., 140, p. 790
Hwang, S.W., Cho, H., Kwak, J., Lee, S.Y., Kang, C.J., Jung, J., Cho, S., Oh, U., (2000) Proc. Natl. Acad. Sci. U.S.A., 97, p. 6155
Huang, J., Zhang, X., McNaughton, P.A., (2006) Curr. Neuropharmacol., 4, p. 197
Silva, C., Silva, J., Castro, H., Reis, F., Dinis, P., Avelino, A., Cruz, F., (2007) BMC Urol., 7, p. 9
Brooks, S.M., (2008) Lung, 186, pp. S88
Holzer, P., (2008) Gut, 57, p. 882
Shimizu, T., (2009) Brain Nerve., 61, p. 949
Bley, K.R., (2004) Expert. Opin. Investig. Drugs, 13, p. 1445
Knotkova, H., Pappagallo, M., Szallasi, A., (2008) Clin. J. Pain, 24, p. 142
Conway, S., (2008) J. Chem. Soc. Rev., 37, p. 1530
Pal, M., Angaru, S., Kodimuthali, A., Dhingra, N., (2009) Curr. Pharm. Des., 15, p. 1008
Broad, L.M., Keding, S.J., Blanco, M., (2008) J. Curr. Top. Med. Chem., 8, p. 1431
Szallasi, A., Cortright, D.N., Blum, C.A., Eid, S.R., (2007) Nat. Rev. Drug Discov., 6, p. 357
Kym, P.R., Kort, M.E., Hutchins, C.W., (2009) Biochem. Pharmacol., 78, p. 211
Szallasi, A., Blumberg, P.M., (1999) Pharmacol. Rev., 51, p. 159
Szallasi, A., Appendino, G., (2004) J. Med. Chem., 47, p. 2717
McLeod, R.L., Correll, C.C., Jia, Y., Anthes, J.C., (2008) Lung, 186, pp. S59
Gunthorpe, M.J., Chizh, B.A., (2009) Drug Discovery Today, 14, p. 56
Wong, G.Y., Gavva, N.R., (2009) Brain Res. Rev., 60, p. 267
Bonache, M.A., Garcia-Martinez, C., De Garcia Diego, L., Carreno, C., Perez De Vega, M.J., Garcia-Lopez, M.T., Ferrer-Montiel, A., Gonzalez-Muniz, R., (2006) ChemMedChem, 1, p. 429
(2008) The Power of Functional Resins in Organic Chemistry, , Tulla-Puche, J., Albericio, F., Eds.
Wiley-VCH Verlag GmbH: KGaA, Weinheim (Germany)
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
Vazques, J., Royo, M., Albericio, F., (2004) Lett. Org. Chem., 1, p. 224
Chen, S., Xu, J., (1992) Tetrahedron Lett., 33, p. 647
Farrera-Sinfreu, J., Royo, M., Albericio, F., (2002) Tetrahedron Lett., 43, p. 7813
noteUR - http://www.scopus.com/inward/record.url?eid=2-s2.0-79957876139&partnerID=40&md5=8205ccf9ba4dadcff7dc556527ba886d
Caterina, M. J., Schumacher, M. A., Tominaga, M., Rosen, T. A., Levine, J. D., Julius, D., (1997) Nature, 389, p. 81
Caterina, M. J., Leffler, A., Malmberg, A. B., Martin, W. J., Trafton, J., Petersen-Zeitz, K. R., Koltzenburg, M., Julius, D., (2000) Science, 288, p. 306
Cortright, D. N., Krause, J. E., Broom, D. C., (2007) Biochim. Biophys. Acta, 1772, p. 978
Willis Jr., W. D., (2009) Exp. Brain Res., 196, p. 5
Cortright, D. N., Szallasi, A., (2009) Curr. Pharm. Des., 15, p. 1736
Ross, R. A., (2003) Br. J. Pharmacol., 140, p. 790
Hwang, S. W., Cho, H., Kwak, J., Lee, S. Y., Kang, C. J., Jung, J., Cho, S., Oh, U., (2000) Proc. Natl. Acad. Sci. U. S. A., 97, p. 6155
Brooks, S. M., (2008) Lung, 186, pp. S88
Bley, K. R., (2004) Expert. Opin. Investig. Drugs, 13, p. 1445
Broad, L. M., Keding, S. J., Blanco, M., (2008) J. Curr. Top. Med. Chem., 8, p. 1431
Kym, P. R., Kort, M. E., Hutchins, C. W., (2009) Biochem. Pharmacol., 78, p. 211
McLeod, R. L., Correll, C. C., Jia, Y., Anthes, J. C., (2008) Lung, 186, pp. S59
Gunthorpe, M. J., Chizh, B. A., (2009) Drug Discovery Today, 14, p. 56
Wong, G. Y., Gavva, N. R., (2009) Brain Res. Rev., 60, p. 267
Bonache, M. A., Garcia-Martinez, C., De Garcia Diego, L., Carreno, C., Perez De Vega, M. J., Garcia-Lopez, M. T., Ferrer-Montiel, A., Gonzalez-Muniz, R., (2006) ChemMedChem, 1, p. 429
(2008) The Power of Functional Resins in Organic Chemistry, , Tulla-Puche, J., Albericio, F., Eds.
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
noteUR - http: //www. scopus. com/inward/record. url? eid=2-s2. 0-79957876139&partnerID=40&md5=8205ccf9ba4dadcff7dc556527ba886d
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.
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Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995 Oct; 36(4): 401-408.
Impact Factor: 2.425
Dettagli Esporta in BibTeX Esporta in EndNote
Costanzo LL, De Guidi G, Giuffrida S, Rizzarelli E, Vecchio G
Determination of superoxide dismutase-like activity of copper(II) complexes. Relevance of the speciation for the correct interpretation of in vitro O2 - scavenger activity (196 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 1993 Jun; 50(4): 273-281.
Impact Factor: 1.342
Dettagli Esporta in BibTeX Esporta in EndNote
Di Blasio B, Pavone V, Nastri F, Isernia C, Saviano M, Pedone C, Cucinotta V, Impellizzeri G, Rizzarelli E, Vecchio G
Conformation for a β-cyclodextrin monosubstituted with a cyclic dipeptide (180 visite)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 1992 Sep 1; 89(15): 7218-7221.
Impact Factor: 9.04
Dettagli Esporta in BibTeX Esporta in EndNote
Alberghina M, Lupo G, La Spina G, Mangiameli A, Gulisano M, Sciotto D, Rizzarelli E
Cytoprotective effect of copper(II) complexes against ethanol-induced damage to rat gastric mucosa (184 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 1992 Mar; 45(4): 245-259.
Impact Factor: 1.342
Dettagli Esporta in BibTeX Esporta in EndNote
Arena G, Impellizzeri G, Maccarrone G, Pappalardo G, Sciotto D, Rizzarelli E
Thermodynamic and 1H-NMR Study of Proton Complex Formation of Histidine-Containing Cyclodipeptides in Aqueous Solution (203 visite)
J Chem Soc, 1992; N/D: 371-376.
Impact Factor: 0
Dettagli Esporta in BibTeX Esporta in EndNote
Marletta F, Rizzarelli E, Mangiameli A, Brogna A, Sammartano S, Monaco S, Blasi A
Effects of graded doses of copper complexes of L-aminoacids on gastric acid secretion in rats (170 visite)
Boll Soc Ital Biol Sper (ISSN: 0037-8771), 1979 Apr 30; 55(8): 769-775.
Impact Factor: 0
Dettagli Esporta in BibTeX Esporta in EndNote
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).
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).
Esporta in BibTeX Esporta in EndNote
Ultima modifica di Marco Comerci in data Thursday 19 March 2015, 16:43:14
170 visite. Ultima visita in data Sunday 08 December 2019, 3:44:47
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