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Synthesis, characterization and Anticancer Evaluation of thiophene based Triazole linked Hydrazones

. Sarmad Fayyaz, Muhammad Suleman, Freeha Hafeez & Asma Zafar


Abstract

Triazole derivatives exhibit a wide range of biological activities, such as antimicrobial, antifungal, antileishmanial, antiviral, antitubercular, anticancer, antioxidant, anticholinesterase, anti-inflammatory, antidepressant, antianxiety, and anticonvulsant properties. The recent study developed the synthesis of triazole-linked hydrazones, a stepwise reaction was employed. Initially, clopidogrel was treated with hydrazine monohydrate under reflux for 24 hours, producing acetohydrazide. This intermediate was then reacted with carbon disulfide (CS2) in dimethylformamide (DMF) at 75°C for 4 hours, yielding oxadiazole derivatives. These oxadiazoles were further reacted with hydrazine monohydrate in ethanol under reflux for 10 hours to form the desired triazole compounds. Subsequently, these oxadiazole and triazole compounds were treated with various nitro benzaldehyde derivatives to produce triazole and oxadiazole analogues’ NMR spectroscopy and Cytotoxic study also revealed that notably, derivative 4b demonstrated superior anti-cancer activity relative to the reference compound. Future research aims to enhance the synthesis of novel triazole derivatives with improved anti-cancer properties, striving to develop broad-spectrum efficacy, low-toxicity, and pharmacokinetically favorable drugs.

Keywords: CNS, DMF, FT-IR, NMR, Pharmacokinetic

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