Triazoles are nitrogen-bearing heterocycles. In the last few decades, researchers have focused on fused heterocycles, as they have better pharmacological effect compared to triazoles alone. Among the two isomers of triazole, this article aims to explore the work carried out on 1,2,4-triazole and N-bridged heterocycles derived from 1,2,4-triazole in last 18 years, highlight different synthetic pathways, and present a brief summary of the different biological activities possessed by 1,2,4-triazole derivatives. The information collected in this article is expected to help researchers to discover novel therapeutic agents for better applications in the field of pharmaceutical science. K E Y W O R D Sbio-organic chemistry, medicinal chemistry, organic chemistry

As part of our effort to identify potent α-amylase inhibitors, in the present study, a novel series of fluorinated thiazolidinone-pyrazole hybrid molecules were prepared by the condensation of 3-(aryl/benzyloxyaryl)-pyrazole-4-carbaldehydes with fluorinated 2,3disubstituted thiazolidin-4-ones. The structures of the newly synthesized compounds were confirmed by infrared, 1 H nuclear magnetic resonance (NMR), 13 C NMR, and liquid chromatography-mass spectrometry data. All the compounds were screened for their αamylase inhibitory and free radical scavenging activities by DPPH (1,1-diphenyl-2picrylhydrazyl) and ABTS methods. Among the tested compounds, compound 8g emerged as a promising α-amylase inhibitor with IC 50 = 0.76 ± 1.23 µM, and it was found to be more potent than the standard drug acarbose (IC 50 = 0.86 ± 0.81 μM). Compounds 8b and 8g showed strong free radical scavenging activity compared to the standard butylated hydroxyl anisole. The kinetic study of compound 8g revealed the reversible, classical competitive inhibition mode on the α-amylase enzyme. Molecular docking and dynamic simulations studies were performed for the most potent compound 8g, which displayed remarkable hydrogen bonding with the α-amylase protein (PDB ID: 1DHK).

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Fourteen novel [1,2,4]triazolo[3,4‐b][1,3,4]thiadiazine derivatives bearing benzimidazole moiety (7a‐n) have been synthesized using the one‐pot nitro reductive cyclization method. All the synthesized compounds were confirmed by 1H nuclear magnetic resonance (1H NMR), 13C NMR, fourier‐transform infrared (FT‐IR), mass spectrum, and elemental analyses. All the title compounds were subjected to in vitro antioxidant activity. The free radical scavenging activity of the compounds was examined using DPPH, nitric oxide, and superoxide radical scavenging methods. The results demonstrated that compound 3‐(2‐(3,4‐dimethoxyphenyl)‐1‐propyl‐1H‐benzo[d]imidazol‐5‐yl)‐6‐4‐tolyl‐7H‐[1,2,4]triazolo[3,4‐b][1,3,4]thiadiazine (7c) was potent in scavenging both DPPH and nitric oxide radical with IC50 values of 13.57 and 18.55 μg/ml when compared to the standard with IC50 values of 23.75 and 23.14 μg/ml, respectively, which was due to the presence of electron‐donating groups. The activity was found to decline when electron‐donating groups were replaced by electron‐withdrawing groups. Moderate scavenging activity was observed for the superoxide radical. Structure activity relationship and physiochemical properties were studied for all the derivatives.