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 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
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 |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-014-1059-0 |