JOURNAL 1419
Bioorganic and Medicinal Chemistry Reports
Year: 2019 Issue: 1-2 (January-December)
p.32 - 37
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GRAPHICAL ABSTRACT
ABSTRACT
Bacterial and fungal resistance to almost all antimicrobial agents have been observed in disease causing bacteria and fungi. A series of 3-({4-[substitutedbenzylideneamino]-1-(morpholin-4-ylmethyl)-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl}methyl)-2(3H)-benzothiazolone (6a-6g) were prepared by the reaction of morpholine in the presence of formaldehyde using microwave irradiation with the yield ranging from 50% to 98%. The newly synthesized compounds were characterized on the basis of elemental analysis, IR and 1H-NMR. All the synthesized compounds were tested for their antibacterial activities against Gram + and Gram – bacteria, their clinical isolates and antifungal activities against Candida species in vitro. Many of these compounds exhibited potent antifungal activity, while compound 6g (MIC:32 µg/mL) had comparable activity with ampicillin and gentamycin (MIC: 4 µg/mL) against E.faecalis isolate.
KEYWORDS- 5-Substituted-4-amino-3-mercapto-1,2,4-triazoles
- 2(3H)-benzothiazolone
- Mannich base
- antibacterial
- antifungal
- MIC
