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Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.


ABSTRACT: The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b, exhibited potent activity against the chloroquine-resistant K1 strain of Plasmodium falciparum. Furthermore, a notable number from the tetrazole series were significantly more active against M. tuberculosis than kanamycin, a standard TB drug.

SUBMITTER: Tukulula M 

PROVIDER: S-EPMC4027538 | biostudies-other | 2013 Jan

REPOSITORIES: biostudies-other

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Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.

Tukulula Matshawandile M   Sharma Rajni-Kant RK   Meurillon Maïa M   Mahajan Aman A   Naran Krupa K   Warner Digby D   Huang Jianxing J   Mekonnen Belew B   Chibale Kelly K  

ACS medicinal chemistry letters 20121126 1


The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b, exhibited potent activity against the chloroquine-resistant K1 strain of Plasmodium falciparum. Furthermore, a notable number from the tetrazole series were significantly more active against M. tuberculosis than kanamycin, a standard TB drug. ...[more]

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