Advances in the Application of 1,2,4-Triazole-Containing Hybrids as Anti-Tuberculosis Agents

Abstract

Tuberculosis is a deadly communicable disease caused by the bacillus Mycobacterium tuberculosis (MTB), and pulmonary tuberculosis accounts for over 80% of the total cases. The 1,2,4-triazole is a privileged structure in the discovery of new drugs, and its derivatives act on various targets in MTB. In particular, 1,2,4-triazole hybrids can not only exert dual or multiple antitubercular mechanisms of action but also have the potential to enhance efficacy and reduce side effects. The present work aims to summarize the current status of 1,2,4-triazole hybrids as potential antitubercular agents, covering articles published between 2010 and 2020, to aid the further rational design of novel potential drug candidates endowed with higher efficacy, better compliance and fewer side effects.

Toxicity parameters of a new 1,2,4-triazole derivative when subcutaneously injected to guinea pigs

“…Over the past years, a whole series of new drugs and fertilizers have been registered in Ukraine, the active substances of which are derivatives of 1,2,4-triazole. All this in the complex indicates that further studies of new substituted 1,2,4-triazole are promising both theoretically and practically (Küçükgüzel & Çıkla-Süzgün, 2015;Cao & Lu, 2017;Li & Zhang, 2022;Nasri et al, 2022).…”

Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery

“…23,24 1,2,3-Triazole rings formed from azides and terminal acetylenes via the Cu(I)-catalyzed cycloaddition reaction are often found to have a variety of biological properties, including anti-HIV, 25 antiallergic, 26 antifungal, 27 anticancer, 28 and antibiotic activity. 29 Different types of copper catalysts have been reported for the preparation of 1,2,3-triazoles under flow conditions. 30 Since the work reported by Bogdan and Sach, 31 tubular copper reactors have commonly been used for the continuous-flow synthesis of 1,2,3-disubstituted triazoles.…”

“…The 1,3-dipolar copper-catalyzed azide-alkyne cycloaddition (CuAAC, Huisgen reaction) was selected as a model to evaluate the potential of this platform. This transformation represents a convenient protocol for the synthesis of functional 1,2,3-triazoles, which are well-known scaffolds with widespread occurrence in medicinal compounds. , 1,2,3-Triazole rings formed from azides and terminal acetylenes via the Cu­(I)-catalyzed cycloaddition reaction are often found to have a variety of biological properties, including anti-HIV, antiallergic, antifungal, anticancer, and antibiotic activity …”

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

“…Literature data concluded that, fused heteroaromatic system exhibited excellent biological activity like N-alkyl-6-nitro-3,5-dihydro [1,2,4]triazolo [1,5-a]pyrimidin-7-amine, [1,2,4]triazolo [1,5-c]pyrimidines exhibited anticonvulsant and antiparasitic activity, respectively, as shown in Figure 1. [1] Among the heterocyclic systems, 1,2,4-triazole and its derivatives attracted synthetic and medicinal chemist due to various pharmacological potential like anxiolytic, [2][3][4][5] antibacterial, [6][7][8][9] anti-parasitic, [10] antiviral, [11] anti-oxidant, [12] fungicide, [13][14][15] antituberculosis, [16] antiepileptic, [17] antitumor. [18 -20] 1,2,4triazoles are derived from pyrazole via substituting doi.org/10.1002/cbdv.202200679 carbon by nitrogen atom at position 4, it acts as isosteres of ester, amide and carboxylic acid.…”

“…Among the heterocyclic systems, 1,2,4‐triazole and its derivatives attracted synthetic and medicinal chemist due to various pharmacological potential like anxiolytic, [2–5] antibacterial, [6–9] anti‐parasitic, [10] antiviral, [11] anti‐oxidant, [12] fungicide, [13–15] anti‐tuberculosis, [16] antiepileptic, [17] antitumor [18–20] . 1,2,4‐triazoles are derived from pyrazole via substituting carbon by nitrogen atom at position 4, it acts as isosteres of ester, amide and carboxylic acid.…”