Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 7, 2012, Pages 2579-2581

  Wang, Cuihua ^a   Ashton, Trent D ^b   Gustafson, Alden ^c   Bland, Nicholas D ^c   Ochiana, Stefan O ^a   Campbell, Robert K ^c   Pollastri, Michael P ^a  

^a NORTHEASTERN UNIVERSITY   (United States)

^b BOSTON UNIVERSITY   (United States)

^c MARINE BIOLOGICAL LABORATORY   (United States)

Author keywords

Neglected disease; PDE5; Phosphodiesterase inhibitors; Sildenafil; Target repurposing; TbrPDEB1; Trypanosoma brucei

Indexed keywords

PHOSPHODIESTERASE IV INHIBITOR; PHOSPHODIESTERASE V INHIBITOR; SILDENAFIL; TADALAFIL; VARDENAFIL;

AFRICAN TRYPANOSOMIASIS; ARTICLE; DRUG DEVELOPMENT; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ERECTILE DYSFUNCTION; NONHUMAN;

ANIMALS; BIOLOGICAL ASSAY; HUMANS; PHOSPHODIESTERASE 5 INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; PIPERAZINES; PROTOZOAN PROTEINS; PURINES; SOLUTIONS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI;

TRYPANOSOMA BRUCEI;

EID: 84862832546     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.119     Document Type: Article

References (21)

1. K. Stuart, R. Brun, S. Croft, A. Fairlamb, R.E. Gurtler, J. McKerrow, S. Reed, and R. Tarleton J. Clin. Invest. 118 2008 1301
2. http://www.who.int/healthinfo/global-burden-disease/2004-report-update/ en/index.html, World Health Organization, accessed 23.01.2012.
3. http://www.who.int/healthinfo/global-burden-disease/metrics-daly/en/, World Health Organization, accessed 23.01.2012.
4. M.P. Pollastri, and R.K. Campbell Future Med. Chem. 3 2011 1307
5. F.S. Menniti, T.A. Chappie, J.M. Humphrey, and C.J. Schmidt Curr. Opin. Investig. Drugs 8 2007 54
6. F.S. Menniti, W.S. Faraci, and C.J. Schmidt Nat. Rev. Drug Disc. 5 2006 660
7. C. Lugnier Pharmacol. Ther. 109 2006 366
8. M.K. Gould, and H.P. de Koning FEMS Microbiol. Rev. 2011
9. M. Oberholzer, G. Marti, M. Baresic, S. Kunz, A. Hemphill, and T. Seebeck FASEB J. 21 2007 720
10. Y. Shakur, K.H.P. de, H. Ke, J. Kambayashi, and T. Seebeck Handb. Exp. Pharmacol. 2011 487
11. N.D. Bland, C. Wang, C. Tallman, A.E. Gustafson, Z. Wang, T.D. Ashton, S.O. Ochiana, G. McAllister, K. Cotter, A.P. Fang, L. Gechijian, N. Garceau, R. Gangurde, R. Ortenberg, M.J. Ondrechen, R.K. Campbell, and M.P. Pollastri J. Med. Chem. 54 2011 8188
12. Ochiana, S. O.; Gustafson, A.; Bland, N. D.; Wang, C.; Campbell, R. K.; Pollastri, M. P. Bioorg. Med. Chem. Lett. 2011, in press, doi:10.1016/j.bmcl. 2012.01.118.
13. H. Wang, Z. Yan, J. Geng, S. Kunz, T. Seebeck, and H. Ke Mol. Microbiol. 1029 2007 66
14. I.R. Baxendale, and S.V. Ley Bioorg. Med. Chem. Lett. 2000 1983 10
15. Liu, H.; He, X.; Choi, H.-S.; Yang, K.; Woodmansee, D.; Wang, Z.; Ellis, D. A.; Wu, B.; He, Y.; Nguyen, T. N., 2006; WO2006047516A2.
16. J.C. Antilla, J.M. Baskin, T.E. Barder, and S.L. Buchwald J. Org. Chem. 69 2004 5578
17. H.A. DeWald, N.W. Beeson, F.M. Hershenson, L.D. Wise, D.A. Downs, T.G. Heffner, L.L. Coughenour, and T.A. Pugsley J. Med. Chem. 31 1988 454
18. J. Yuan, M. Gulianello, L.S. De, R. Brodbeck, A. Kieltyka, and K.J. Hodgetts Bioorg. Med. Chem. Lett. 12 2002 2133
19. Fletcher, S. R.; Menet, C. J. M.; Dykes, G. J.; Merayo, M. N.; Schmitt, B. A., 2008; WO2008071650A2.
20. T. Seebeck, G.J. Sterk, and H. Ke Future Med. Chem. 3 2011 1289
21. T.B. Beghyn, J. Charton, F. Leroux, G. Laconde, A. Bourin, P. Cos, L. Maes, and B. Deprez J. Med. Chem. 54 2011 3222