Some novel Schiff bases of [1,2,4]triazole bearing haloarene moiety—synthesis and evaluation of antituberculosis properties and neutrophil function test

A series of novel Schiff bases of [1,2,4]triazole-bearing haloarene moiety ( 5a–l ) were synthesized from 4-amino-3-methyl-5-mercapto-4 H -[1,2,4]triazole ( 3 ) and were confirmed by FT-IR, 1 H-NMR, 13 C-NMR, LC-Mass spectra and elemental analyses and screened for in vitro antituberculosis propertie...

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Veröffentlicht in:Medicinal chemistry research 2016, Vol.25 (1), p.83-93
Hauptverfasser: Castelino, Prakash Anil, Dasappa, Jagadeesh Prasad, Bhat, Kishore G., Joshi, Sumith Ashok, Jalalpure, Sunil
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Sprache:eng
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Zusammenfassung:A series of novel Schiff bases of [1,2,4]triazole-bearing haloarene moiety ( 5a–l ) were synthesized from 4-amino-3-methyl-5-mercapto-4 H -[1,2,4]triazole ( 3 ) and were confirmed by FT-IR, 1 H-NMR, 13 C-NMR, LC-Mass spectra and elemental analyses and screened for in vitro antituberculosis properties and for neutrophil function test, where they exhibited moderate neutrophil functions and antituberculosis properties. Compounds ( 5a ), ( 5c ), ( 5f ), ( 5h ) and ( 5i ) were moderately sensitive to antituberculosis activity, while ( 5a ), ( 5b ), ( 5g ) and ( 5h ) were sensitive for neutrophil functions in the series. The acute oral toxicity studies on the Swiss albino mice according to the OECD/OCDE guidelines 423 confirmed that the compounds were slightly toxic and hence they may be considered as drug candidates for microbial pathogens. The antituberculosis studies by both ZOI and MIC tests confirmed that the novel derivatives are moderately sensitive towards Mycobacterium tuberculosis (H37RV) strain.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-015-1461-2