SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL EVALUATION OF SOME 1, 2, 4-TRIAZOLE DERIVATIVES
Keywords:
Antibacterial activity, Antifungal activity, 1, 2, 4-TriazoleAbstract
Objectives: To synthesize, characterize and evaluate antimicrobial properties of some 1, 2, 4-triazole derivatives.
Methods: A novel series of 1, 2, 4-Triazole derivatives (D-1-D-8) had been synthesized. Ethyl esters of benzoic and 4-substituted benzoic acids were synthesized using ethanol and conc. sulphuric acid. In the second step, hydrazides of these esters were prepared. This hydrazide was converted into potassium salt of dithiocarbazinate using carbon disulfide and potassium hydroxide which on cyclization formed compounds (D-1-D-2). Compound D-3 was formed by reacting D-1 with 4-methylbenzenesulfonyl chloride in dry pyridine. Compounds (D-4-D-8) were synthesized by mixing aqueous solution of 10% NaOH in different primary amines and then heating it with potassium salt of dithiocarbazinate. The structures of newly synthesized compounds were established on the basis of 1H NMR and Mass spectroscopic techniques. The newly synthesized compounds were screened for their in vitro antibacterial and antifungal activity. In vitro antibacterial and antifungal activity was evaluated by Disc Diffusion method. Ofloxacin and Clotrimazole were used as standard drug respectively.
Results: The results revealed that compounds D-3 and D-4 exhibited good antibacterial activity and D-1 and D-2 had moderate antibacterial activity as compared with standard drug Ofloxacin, while compounds (D-5-D-8) exhibited moderate antifungal activity as compared to standard drug Clotrimazole.
Conclusion: A novel series of 1, 2, 4-Triazole derivatives were synthesized and were obtained in good yields. Newly synthesized compounds were isolated and purified by thin layer chromatography and column chromatography respectively.
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