SYNTHESIS AND ANTIMICROBIAL EVALUATION OF 2-[(SUBSTITUEDPHENYL)-5-(1-PHENYL-3-(PIPERAZINYL)PYRIDO[3,2-f]QUINAZOLIN-4(1H)-YL]-1,3,4-THIADIAZOLES
Abstract: Several novel
2-[(substitutedphenyl)-5-(1-phenyl-3-(piperazinyl)pyrido[3,2-f]
quinazolin-4(1H)-yl]-1,3,4 thiadiazole derivatives have been designed and
synthesised by incorporating four known moieties such
as 2-methylquinolin-5-ol,
acetophenone, urea and 3-substitutedphenyl-4-amino-5-mercapto triazoles by using
multi-step conventional reaction strategy. The synthesized derivatives were
characterized by IR, 1H-NMR, Mass and elemental analysis (C, H, N). Furthermore
the synthesized
2-[(substitutedphenyl)-5-(1-phenyl-3-(piperazinyl)pyrido[3,2-f]quinazolin-4(1H)-yl]-1,3,4-thiadiazoles
4a-g were screened for antibacterial and antifungal activities. The bacterial
panel consisted of Staphylococcus aureus, Escherichia coli, Klabsiella
pneumoniae, Proteus vulgaris while fungal panel included of Aspergillus
fumigatus (plant isolate), Candida glabrata, Candida albacans, Candida krusei.
Ampicillin trihydrate and fluconazole were used as reference drugs for
antibacterial and antifungal activity respectively. Bacterial and fungal
inhibition determined by disk diffusion and serial plate dilution method
respectively. Pathogenic inhibitions were determined by measuring the diameter
of the inhibition zone in mm. Compound 4c demonstrated significant
antibacterial and antifungal spectrum against all the tested microbes.
Keywords: antibacterial,
antifungal and substituted 1,3,4-thiadiazoles
Author: Tilak Ram, Ranjana
Dubey, Nidhi Chaudhary
Journal Code: jpfarmasigg160043
