Synthesis of 3-chloro-4-fluorophenyl-3,4-dichlorophenyl substituted thiocarbamide derivatives as potential antitubercular agents

A series of dihalosubstituted thiocarbamide derivatives ( 5a – e , 6a – e , 7a – e , and 8a – e ) were synthesized as antitubercular agents. The structures of dihalosubstituted thiocarbamide derivatives were established on the basis of IR, 1 H, 13 C NMR, and mass spectral data. All the compounds wer...

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Veröffentlicht in:Medicinal chemistry research 2015, Vol.24 (1), p.334-343
Hauptverfasser: Faiz Arshad, M., Kumar, Suresh, Al Rohaimi, Abdulmohsen H., Hassan, Allam A., Elkerdasy, Ahmed, Upmanyu, Neeraj
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Sprache:eng
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Zusammenfassung:A series of dihalosubstituted thiocarbamide derivatives ( 5a – e , 6a – e , 7a – e , and 8a – e ) were synthesized as antitubercular agents. The structures of dihalosubstituted thiocarbamide derivatives were established on the basis of IR, 1 H, 13 C NMR, and mass spectral data. All the compounds were tested in vitro for antimycobacterial activity against Mycobacterium tuberculosis (ATCC-25177) by well-diffusion method and MIC by serial dilution method. Results of the antitubercular screening revealed that some of the compounds showed moderate to good antitubercular activity. Of all the compounds tested, two derivatives viz., 8d and 8e expressed MIC of 25 μg/ml, and one compound 7e showed MIC of 12.5 μg/ml against M. tuberculosis (ATCC-25177). Graphical Abstract
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-014-1059-0