A Review on 1,2,4-Triazoles as Scaffold for Various Pharmacological Activities

Review Article

Abstract

The 1,2,4-triazole scaffold represents a fundamental heterocyclic system exhibiting broad-spectrum pharmacological activities. The aromatic nature and unique electronic properties of the triazole ring enable formation of stable linkages with diverse bioactive scaffolds, positioning these compounds as central elements in medicinal chemistry. Recent investigations have revealed promising applications of 1,2,4-triazole derivatives, particularly in addressing challenging therapeutic areas including tuberculosis, cancer, and inflammatory conditions. Notably, several studies document potent antitubercular effects of triazole-based hybrids such as triazoloquinazolines, benzothiazole-triazoles, and fused piperidine-triazole systems against both drug-sensitive and MDR strains of Mycobacterium tuberculosis. Structure-activity relationship studies indicate that electron-withdrawing substituents, heteroaromatic fusion, and hydrazone linkers enhance biological efficacy. The integration of Schiff and Mannich base modifications has yielded derivatives with significant antimicrobial and antioxidant properties. Modern approaches combining synthetic strategies with computational analysis and biological evaluations have accelerated the development of optimized triazole-based therapeutic agents. This paper discusses key developments in 1,2,4-triazole chemistry, emphasizing their pharmacological significance and potential for further development as therapeutic agents, with particular focus on antitubercular applications