1,2,4-Triazoles: A Review of Synthetic Approaches and the Biological Activity

C-Glycosyl 1,2,4-triazoles: Synthesis of the 3-β-d-glucopyranosyl-1,5-disubstituted and 5-β-d-glucopyranosyl-1,3-disubstituted variants

“…2,165.9,165.3,165.2 (C=O),158.0,76.7,74.7,74.3,72.1,60.6,50.5 (2 × CH2),11.9 (CH3 ,5.00;N,5.95. Found: C,66.40;H,5.09;N,6.03.…”

“…As a consequence of this broad utility and interest, a large variety of synthetic methods have been elaborated to get this heteroring and its derivatives resulting in miriads of 1,2,4-triazole containing compounds. [1][2][3][4][5][6][7][8] Carbohydrate derivatives of this heterocycle are much less available. Direct conjugation of the 1,2,4-triazole ring with sugars may occur by a C-N or a C-C bond.…”

Synthesis of some novel heterocylic compounds derived from 2-[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetohydrazide and investigation of their lipase andα-glucosidase inhibition

“…For example, in the treatment of diabetes mellitus patients, some a-glucosidase inhibitors, such as acarbose and voglibose, are extensively used but often causes severe gastrointestinal side effects such as flatulence and diarrhea [11][12][13] . Heterocyclic compounds containing 1,2,4-triazole skeleton are known to possess a wide range of pharmacological activities such as antimicrobial, antitubercular, anti-inflammatory, antiviral, antioxidant, antidepressant, anticonvulsant, antimalarial, anti-diabetic, anti-obesity, enzyme inhibitory and anticancer activities [14][15][16][17] . Some present day drugs such as fluconazole, itraconazole, terconazole (antifungal agents), anastrozole, letrozole, vorozole (aromatase inhibitors in the treatment of postmenopausal breast cancer), ribavirin (antiviral agent), etoperidone and nefazodone (antidepressant), rizatriptan (antimigraine agent) and rilmazafon (hypnotic, anxiolytic, used in the case of neurotic insomnia) are examples of potent bioactive molecules possessing 1,2,4-triazole moieties 16,[18][19][20][21] .…”

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“…Over the past few decades, the biological and pharmaceutical applications of 1, 2, 4-triazoles have fashioned substantial interest in their synthesis and characterization. 1, 2, 4-triazoles and their derivatives possess differing activities which range from antiasthmatic 21 , antiviral (ribavirin) 22 , antifungal (fluconazole) 23 , antibacterial 24 , hypnotics 25 (triazolam) to anticancer. In this regard, we come up with the hypothesis that incorporation of 1H-1, 2, 4-triazole into the multi-substituted 2-amino thiophene unit may enhance their biological activity.…”