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6. Synthesis, characterization and evaluation of antituberculosis activity of some hydrazones

Author

Koçyiğit Kaymakçıoğlu, B. and Rollas, S.

Subjects
*HYDRAZONES, *CHEMICALS, *STRUCTURE-activity relationship in pharmacology, *ANTITUBERCULAR agents, *PHARMACOKINETICS
Abstract

Several new hydrazone derivatives were prepared by the reaction of some active hydrogen compounds with the diazonium salts of 4-amino-3,5-di/1,3,5-trimethylpyrazoles at 0–5 °C. Structures of the new substances were confirmed using UV, IR, 1H NMR, 13C NMR and EI-mass spectral data. In vitro antituberculosis activity of these compounds were tested on Mycobacterium tuberculosis H37Rv at 6.25 μg/ml. Both hydrazone products, ethyl 2-[(3,5-dimethylpyrazole-4-yl)hydrazono]-3-oxobutyrate (3d) and methyl 2-[(3,5-dimethylpyrazole-4-yl)hydrazono]-4-methoxy-3-oxobutyrate (3e) showed 29 and 28% inhibition against M. tuberculosis, respectively. [ABSTRACT FROM AUTHOR]

Published
2002

7. Synthesis and antituberculosis activity of new N-phenyl-N′-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thioureas

Author

Karakuş, S. and Rollas, S.

Subjects
*ANTITUBERCULAR agents, *PHENYL compounds, *STRUCTURE-activity relationship in pharmacology
Abstract

In this study, eight original N-phenyl-N′-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea derivatives were synthesized and tested for antituberculosis activity. Antituberculosis activities of the synthesized compounds were screened in vitro using BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv at 6.25 μg/ml. The highest inhibition observed with the synthesized compounds is 67% for N-phenyl-N′-[4-(5-cyclohexylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea. [ABSTRACT FROM AUTHOR]

Published
2002

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