Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity

European Journal of Medicinal Chemistry

Volumn 45, Issue 12, 2010, Pages 5767-5772

  Álvarez, Guzmán ^a   Aguirre López, Beatriz ^b   Varela, Javier ^a   Cabrera, Mauricio ^a   Merlino, Alicia ^a   López, Gloria V ^a   Lavaggi, María Laura ^a   Porcal, Williams ^a   Di Maio, Rossanna ^a   González, Mercedes ^a   Cerecetto, Hugo ^a   Cabrera, Nallely ^b   Pérez Montfort, Ruy ^b   De Gómez Puyou, Marieta Tuena ^b   Gómez Puyou, Armando ^b  

^a UNIVERSIDAD DE LA REPÚBLICA   (Uruguay)

^b INSTITUTO DE FISIOLOGÍA CELULAR   (Mexico)

Author keywords

Drug discovery; Massive screening; T. cruzi; TIM

Indexed keywords

ANTIPROTOZOAL AGENT; DIHYDROXYACETONE PHOSPHATE; ENZYME INHIBITOR; GLYCERALDEHYDE 3 PHOSPHATE; TRIOSEPHOSPHATE ISOMERASE; TRIOSEPHOSPHATE ISOMERASE INHIBITOR; UNCLASSIFIED DRUG;

ANTIPROTOZOAL ACTIVITY; ARTICLE; DRUG INHIBITION; DRUG SCREENING; DRUG SELECTIVITY; IN VITRO STUDY; NONHUMAN; TRYPANOSOMA CRUZI;

DIMERIZATION; ENZYME INHIBITORS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PARASITIC SENSITIVITY TESTS; SMALL MOLECULE LIBRARIES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRIOSE-PHOSPHATE ISOMERASE; TRYPANOCIDAL AGENTS; TRYPANOSOMA CRUZI;

EID: 78649328166     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2010.09.034     Document Type: Article

References (29)

1. A.C. Moncayo, and M.I. Ortiz Yanine Ann. Trop. Med. Parasitol. 100 2006 663 677
2. C.J. Schofield, J. Jannin, and R. Salvatella Trends Parasitol. 22 2006 583 588
3. A. Gomez-Puyou, E. Saavedra-Lira, I. Becker, R.A. Zubillaga, A. Rojo-Dominguez, and R. Perez-Montfort Chem. Biol. 2 1995 847 855
4. S.S. Velanker, S.S. Ray, R.S. Gokhale, H. Balaram, P. Balaram, and M.R.N. Murthy Structure 5 1997 751 761
5. A.A. Cortés-Figueroa, A. Pérez-Torres, N. Salaiza, N. Cabrera, A. Escalona-Montaño, A. Rondán, M. Aguirre-García, A. Gómez-Puyou, R. Pérez-Montfort, and I. Becker Parasitol. Res. 102 2008 635 643
6. E. Maldonado, M. Soriano-García, A. Moreno, N. Cabrera, G. Garza-Ramos, M. de Gómez-Puyou, A. Gómez-Puyou, and R. Perez-Montfort J. Mol. Biol. 283 1998 193 203
7. S.G. Waley Biochem. J. 135 1973 165 172
8. S. Zabori, R. Rudolph, and R. Jaenicke Z. Naturforsch. 35C 1980 999 1004
9. V. Olivares-Illana, A. Rodríguez-Romero, I. Becker, M. Berzunza, J. García, R. Pérez-Montfort, N. Cabrera, F. López- Calahorra, M. Tuena de Gómez-Puyou, and A. Gómez-Puyou PLoS Neglected Trop. Dis. 1 2007 e01
10. V. Olivares-Illana, R. Pérez-Montfort, F. López-Calahorra, M. Costas, A. Rodríguez-Romero, M. Tuena de Gómez-Puyou, and A. Gómez Puyou Biochemistry 45 2006 2556 2560
11. H. Cerecetto, and M. González Mini Rev. Med. Chem. 8 2008 1355 1383
12. See Supplementary Content section for complete references of the studied compounds.
13. A. Téllez-Valencia, V. Olivares-Illana, A. Hernández- Santoyo, R. Pérez-Montfort, M. Costas, A. Rodríguez-Romero, F. López-Calahorra, M. Tuena de Gómez-Puyou, and A. Gómez-Puyou J. Mol. Biol. 341 2004 1353 1365
14. L.M. Espinoza-Fonseca, and J.G. Trujillo-Ferrara Biochem. Biophys. Res. Comm. 328 2005 922 928
15. J.F. Faucher, T. Baltz, and K.G. Petry Parasitol. Res. 81 1995 441 443
16. M. Almeida-de-Faria, E. Freymuller, W. Colli, and M.J. Alves Exp. Parasitol. 92 1999 263 274
17. B. Zingales, M.E.S. Pereira, K.A. Almeida, E.S. Umezawa, N.S. Nehme, R.P. Oliveira, A. Macedo, and R.P. Souto Mem. Inst. Oswaldo Cruz 92 1997 811 814
18. N. Yoshida Parasitol. Int. 57 2008 105 109
19. L.S. Filardi, and Z. Brener Trans. Royal Soc. Trop. Med. Hyg. 81 1987 755 759
20. J. Molina, Z. Brener, A.J. Romanha, and J.A. Urbina J. Antimicrob. Chem. 46 2000 137 140
21. miLogP was calculated using Molinspiration online property calculation toolkit http://www.molinspiration.com/cgi-bin/properties
22. P. Gaillard, P.A. Carrupt, B. Testa, and A. Boudon J. Comp.-Aided Mol. Des 8 1994 83 96
23. A.J.M. Carpy, and N. Marchand-Geneste SAR QSAR Environ. Res. 14 2003 329 337
24. P. Ostoa-Saloma, G. Garza-Ramos, J. Ramírez, I. Becker, M. Berzunza, A. Landa, A. Gómez-Puyou, M. Tuena de Gómez-Puyou, and R. Perez-Montfort Eur. J. Biochem. 244 1997 700 705
25. S.C, V. Mande, K.H. Mainfroid, K. Kalk, J.A. Goraj, and W.G. MartialHol Protein Sci. 3 1994 810 821
26. C.N. Pace, F. Vajdos, L. Fee, G. Grimsley, and T. Gray Protein Sci. 4 1995 2411 2423
27. J. Rodríguez, A. Gerpe, G. Aguirre, U. Kemmerling, O.E. Piro, V.J. Arán, J.D. Maya, C. Olea-Azar, M. González, and H. Cerecetto Eur. J. Med. Chem. 44 2009 1545 1553
28. M. Boiani, L. Boiani, A. Merlino, P. Hernández, A. Chidichimo, J.J. Cazzulo, H. Cerecetto, and M. González Eur. J. Med. Chem. 44 2009 4426 4433
29. A. Gerpe, L. Boiani, P. Hernández, M. Sortino, S. Zacchino, H. Cerecetto, and M. González Eur. J. Med. Chem. 45 2010 2154 2164