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Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Feb 01; Vol. 17 (3), pp. 593-6. Date of Electronic Publication: 2006 Nov 10. - Publication Year :
- 2007
-
Abstract
- Amidoxime and O-substituted derivatives of the bis-alkylamidine 1,12-bis(N,N'-acetamidinyl)dodecane were synthesized and evaluated as in vitro and in vivo antimalarial prodrugs. The bis-O-methylsulfonylamidoxime 8 and the bis-oxadiazolone 9 derivatives show relatively potent antimalarial activity after oral administration.
- Subjects :
- Administration, Oral
Animals
Female
Humans
Hydroxylation
Indicators and Reagents
Injections, Intraperitoneal
Malaria drug therapy
Malaria parasitology
Malaria, Falciparum drug therapy
Malaria, Falciparum parasitology
Mice
Plasmodium cynomolgi drug effects
Plasmodium falciparum drug effects
Alkanes chemical synthesis
Alkanes pharmacology
Amidines chemical synthesis
Amidines pharmacology
Antimalarials chemical synthesis
Antimalarials pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17123818
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.11.013