SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 10, 2011, Pages 2816-2819

  Perales, Joe B ^a   Freeman, Jennifer ^a   Bacchi, Cyrus J ^b   Bowling, Tana ^a   Don, Robert ^c   Gaukel, Eric ^a   Mercer, Luke ^a   Moore III, Joseph A ^a   Nare, Bakela ^a   Nguyen, Tien M ^a   Noe, Robert A ^a   Randolph, Ryan ^a   Rewerts, Cindy ^a   Wring, Stephen A ^a   Yarlett, Nigel ^b   Jacobs, Robert T ^a  

^a SCYNEXIS Inc   (United States)

^b PACE UNIVERSITY   (United States)

^c Drugs for Neglected Diseases Initiative DNDi   (Switzerland)

Author keywords

2,4 Diamino pyrimidines; Human african trypanosomiasis; Trypanosoma brucei

Indexed keywords

2,4 DIAMINOPYRIMIDINE DERIVATIVE; AMINOPYRIMIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

AFRICAN TRYPANOSOMIASIS; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD BRAIN BARRIER; DRUG EFFICACY; DRUG PENETRATION; DRUG STRUCTURE; DRUG SYNTHESIS; IN VIVO STUDY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TRYPANOSOMA BRUCEI; TRYPANOSOMIASIS;

AMINES; ANIMALS; BLOOD-BRAIN BARRIER; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR STRUCTURE; PERMEABILITY; PYRIMIDINES; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI;

TRYPANOSOMA BRUCEI;

EID: 79955552387     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.097     Document Type: Article

References (12)

1. WHO. Weekly Epidemiological Record 2006, 81, 71.
2. R. Brun, R. Schumacher, C. Schmid, C. Kunz, and C. Burri Tropical Med. Int. Health 6 2001 906
3. C. Burri, and J. Keiser Tropical Med. Int. Health 6 2001 412
4. B. Clement, A. Buerenheide, W. Rieckert, and J. Schwarz Chem. Med. Chem. 1 2006 1260
5. D. Legros, G. Ollivier, M. Gastellu-Etchegorry, C. Paquet, C. Burri, J. Jannin, and P. Buscher Lancet Infect. Dis. 2 2002 437
6. J. Pepin, and F. Milord Adv. Parasitol. 33 1994 1
7. M. Koffi, T. De Meeus, B. Bucheton, P. Solano, M. Camara, D. Kaba, G. Cuny, F.J. Ayala, and V. Jamonneau Proc. Natl. Acad. Sci. U.S.A. 106 2009 209
8. A. Cooper, A. Tait, L. Sweeney, A. Tweedie, L. Morrison, C.M.R. Turner, and A. MacLeod Genome Biol. 9 2008 R103
9. L. Mercer, T. Bowling, J.B. Perales, J. Freeman, T.M. Nguyen, R. Don, R.T. Jacobs, and B. Nare PLoS Neglected Trop. Dis. 5 2011 e956
10. K.M.M. Doan, J.E. Humphreys, L.O. Webster, S.A. Wring, L.J. Shampine, C.J. Serabjit-Singh, K.K. Adkison, and J.W. Polli J. Pharmacol. Exp. Ther. 303 2002 1029
11. K.A. Lentz, J.W. Polli, S.A. Wring, J.E. Humphreys, and J.E. Polli Pharm. Res. 17 2000 1456
12. X.J. Chu, W. DePinto, D. Bartkovitz, S.S. So, B.T. Vu, K. Packman, C. Lukacs, Q. Ding, N. Jiang, K. Wang, P. Goelzer, X. Yin, M.A. Smith, B.X. Higgins, Y. Chen, Q. Xiang, J. Moliterni, G. Kaplan, B. Graves, A. Lovey, and N. Fotouhi J. Med. Chem. 49 2006 6549