Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 20, 2003, Pages 3447-3450

  Singh, Chandan ^a   Gupta, Nitin ^a   Puri, Sunil K ^a  

^a CENTRAL DRUG RESEARCH INSTITUTE   (India)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,4 TRIOXANE DERIVATIVE; ACETIC ACID DERIVATIVE; ARTEMISININ; CHLOROQUINE; GERANIOL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; IN VIVO STUDY; MOUSE; MOUSE STRAIN; NONHUMAN; PARASITEMIA; PLASMODIUM YOELII;

PLASMODIUM YOELII;

EID: 0141851824     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00782-0     Document Type: Article

References (23)

1. (a) Klayman D.L. Science. 228:1985;1049.
2. (b) Luo X.D., Shen C.C. Med. Res. Rev. 7:1987;29.
3. (c) Zaman S.S., Sharma R.P. Heterocycles. 32:1991;1593.
4. (d) Cumming J.N., Ploypradith P., Posner G.H. Adv. Pharmacol. 37:1997;253.
5. (e) Zhou W.S., Xu X.X. Acc. Chem. Res. 27:1994;211.
6. (f) Bhattacharya A.K., Sharma R.P. Heterocycles. 51:1999;1681.
7. (a) O'Neill P.M., Pugh M., Davies J., Ward S.A., Park B.K. Tetrahedron Lett. 42:2001;4569.
8. (b) Bloodworth A.J., Johnson K.A. Tetrahedron Lett. 35:1994;8057.
9. (c) Bloodworth A.J., Curtis R.J., Spencer M.D., Tallant M.S. Tetrahedron. 49:1993;2729.
10. (d) Posner G.H., Oh C.H., Tilhous W.K. Tetrahedron Lett. 34:1991;4235.
11. (e) Bunelle W.H., Isbell T.A., Bames C.L., Qualls S. J. Am. Chem. Soc. 113:1991;8168.
12. (f) Avery M.A., Jennings-White C., Chong W.K.M. J. Org. Chem. 54:1989;1792.
13. (g) Singh C. Tetrahedron Lett. 33:1990;6901.
14. (h) Kepler J.A., Philip A., Lee Y.W., Morey M.C., Caroll F.I. J. Med. Chem. 31:1988;713.
15. (i) Jefford C.W., Jaggi D., Boukouvalas J., Burger S. J. Am. Chem. Soc. 105:1983;6497.
16. (b) Singh C., Misra D., Saxena G., Chandra S. Bioorg. Med. Chem. Lett. 5:1995;1913.
17. (a) Singh C., Misra D., Saxena G., Chandra S. Bioorg. Med. Chem. Lett. 2:1992;497.
18. Singh C., Gupta N., Puri S.K. Bioorg. Med. Chem. Lett. 12:2002;1913.
19. Dodd D.S., Oehlschlager A.C., Georgopapadakou N.H., Polok A.-M., Hartman P.G. J. Org. Chem. 57:1992;7226.
20. ++1). Anal. calcd: C 78.00%, H 7.67%; found C 77.69%, H 8.01%.
21. 9 Mice treated with artemisinin and chloroquine served as positive controls.
22. Since artemisinin is active at a dose of 48 mg/kg, we have chosen 96 mg/kg as the highest dose in the primary screening of trioxanes.
23. Puri S.K., Singh N. Expl. Parasit. 94:2000;8.