Review of Synthetic Accessibility And Pharmacological Activity of 1,2,4-Triazole and 2-Methylbenzimidazole Derivatives

PHARMACEUTICAL CHEMISTRY JOURNAL(2022)

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Abstract
The main focus of synthetic chemistry is to develop safe and therapeutically active compounds by employing green synthetic reaction conditions. The azole nuclei have been the center of attention for decades owing to their diverse pharmacological activities. Various synthetic routes have been identified for the synthesis of pharmacologically active derivatives of azoles. Coupling reactions have gained much importance in synthetic chemistry the most basic type of joining two chemical species. The coupling reactions of azoles include alkylation and arylation of the nitrogen atom which yields many compounds possessing significant therapeutical potential, only having limitations related to expensive catalyst systems, bulky ligands, time constraints etc. These limitations can be overcome by employing safe and economical catalyst systems involving nanoparticles. These nanosystems are easy to formulate and offer the advantage of catalyzing the reaction more rapidly with significantly improved yield. In this review, two of the most important azole nuclei—triazole and benzimidazole—are discussed on the basis of their diverse pharmacological properties making them effective drug candidates for further development to overcome emerging diseases. In particular, 1,2,4-triazole and 2-methlybenzimidazole have wide range of therapeutic activities such as anti-inflammatory, antioxidant, antimicrobial, antidiabetic, anthelmintic, analgesic, antihypertensive, anticonvulsant, anticancer, antiulcer, antiprotozoal, antimycobacterial, anti-HIV and antipsychotic.
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Key words
1, 2, 4-triazole, 2-methylbenzimidazole, nanoparticle catalyst, coupling reaction, N-arylation reaction, antimicrobial, antioxidant
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