Synthesis and anti-trypanosomal activity of novel 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives
Several novel semicarbazones derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde, and tested in vitro as potential anti-trypanosomal agents. The compounds were prepared in good to excellent yields in 2-3 steps from readily available starting materials. Some derivatives were found to be active against Trypanosoma cruzi with an activity similar to that of Nifurtimox.
Studies in Potential Filaricides: Part 19 - Synthesis of 1-Methyl-4-substituted Carbonylpiperazines as Diethylcarbamazine Analogs
The synthesis and antifilarial activity of a series of 1-methyl-4-substituted carbamoyl- and carbonylpiperazines (6 - 42) against Litomosoides carinii in cotton rats and Dipetalonema viteae in Mastomys natalensis are described.The most potent compound of this series, 1-methyl-4-(pyrrolidin-1-yl)carbonylpiperazine (7) causes 95 - 98 percent reduction of blood microfilarial count in cotton rats infected with L. carinii at an intraperitoneal or oral dose of 1.5 (base) or 3 (citrate) mg/kg given for 6 days.A number of other compounds also exhibit marked microfilaricidal efffect in the dose range of 6 - 30 mg/kg.
Sharma, Satyavan,Agarwal, V. K.,Dubey, S. K.,Iyer, R. N.,Anand, Nitya,et al.
p. 748 - 751
(2007/10/02)
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