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In vivo and in vitro anti-leishmanial activities of 4-nitro-N-pyrimidin- and N-pyrazin-2-ylbenzenesulfonamides, and N2-(4-nitrophenyl)-N1-propylglycinamide.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2009 Nov 01; Vol. 17 (21), pp. 7449-56. Date of Electronic Publication: 2009 Sep 20. - Publication Year :
- 2009
-
Abstract
- A series of compounds containing the nitrobenzene and sulfonamido moieties were synthesized and their leishmanicidal effect was assessed in vitro against Leishmaniainfantum promastigotes. Among the compounds evaluated, the p-nitrobenzenesulfonamides 4Aa and 4Ba, and the p-nitroaniline 5 showed significant activity with a good selectivity index. In a Balb/c mice model of L. Infantum, administration of compounds 4Aa, 4Ba or 5 (5mg/kg/day for 10 days, injected ip route) led to a clear-cut parasite burden reduction (ca. 99%). In an attempt to elucidate their mechanism of action, the DNA interaction of 4Aa and 5 was investigated by means of viscosity studies, thermal denaturation and nuclease activity assay. Both compounds showed nuclease activity in the presence of copper salt. The results suggest that compounds 4Aa, 4Ba and 5 represent possible candidates for drug development in the therapeutic control of leishmaniasis.
- Subjects :
- Aniline Compounds chemical synthesis
Aniline Compounds pharmacology
Animals
Glycine chemical synthesis
Glycine chemistry
Glycine pharmacology
Leishmaniasis drug therapy
Mice
Mice, Inbred BALB C
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Sulfonamides chemical synthesis
Sulfonamides pharmacology
Trypanocidal Agents chemical synthesis
Trypanocidal Agents pharmacology
Benzenesulfonamides
Aniline Compounds chemistry
Glycine analogs & derivatives
Pyrimidines chemistry
Sulfonamides chemistry
Trypanocidal Agents chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 17
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 19811921
- Full Text :
- https://doi.org/10.1016/j.bmc.2009.09.030