Abstract

DESIGN, DOCKING, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF BENZOTRIAZOLE FUSED WITH OXADIAZOLE DERIVATIVE

Jayaseelan K.*, Senthilkumar S.K., Arunagiri M., Bhavadharani S., Deepalakshmi G. and Surya V.

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Abstract

1, 3, 4-Oxadiazole derivatives exhibited significant anti-tuberculosis activity. They also showed antimicrobial, anti-inflammatory, analgesic, antifungal, antipyretic, antidepressant, anti - convulsant, anticholinesterase, antihypertensive, antidiabetic, antitumor/anticancer, anti-HIV, antioxidant, etc. Benzotriazole is a nitrogen-containing heterocyclic compound characterized by the presence of three nitrogen atoms at the 1st, 2nd, and 3rd positions of its five-membered ring. Benzotriazole derivatives that exhibit antimicrobial, antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory, anticonvulsant, analgesic, and antioxidant activities. The basis nucleus of the research work is oxadiazole. A series of novel benzotriazole fused with oxadiazole derivative were designed, Synthesized, and biologically evaluated. The synthesized compounds were characterized using various spectroscopic techniques. Molecular docking studies were performed to predict the binding affinity and mode of interaction with target proteins. The anti-tubercular activity of these compounds was evaluated using the Microplate Alamar Blue Assay (MABA). The results revealed promising anti-tubercular activity against Mycobacterium tuberculosis.

Keywords: Anti-tuberculosis, Anti-cancer, Anti-microbial, Anti-pyretic, Anti-oxidant, Oxadiazole and Benzotriazole.