Recent accomplishments on the synthetic/biological facets of pharmacologically active 1H-1,2,3-triazoles

Design and Synthesis of New 5-aryl-4-Arylethynyl-1H-1,2,3-triazoles with Valuable Photophysical and Biological Properties

“…1,2,3-Triazoles are widely synthetically available compounds due to the development of simple and effective methods of their preparation on the base of “click” reaction of Cu-catalyzed azide–alkyne cycloaddition (CuAAC) [ 6 , 7 , 8 , 9 , 10 ]. Due to the wide range of available derivatives and the accessibility of structural modifications by a variety of pharmacophore fragments 1,2,3-triazoles attract a special interest in the field of drug design [ 11 , 12 , 13 , 14 ]. The biological properties of triazole derivatives are very diverse.…”

“…The biological properties of triazole derivatives are very diverse. Currently, among the most widely studied types of activity are: antibacterial [ 14 , 15 ], antiviral [ 16 ], and anticancer [ 17 , 18 ].…”

Design and synthesis of phenoxymethybenzoimidazole incorporating different aryl thiazole-triazole acetamide derivatives as α-glycosidase inhibitors

“…Considering the important properties of triazoles such as easy synthetic protocol and promising anti-diabetic properties [ 23 ] as well as imidazole and its derivatives as one of the most important nitrogen-containing heterocyclic scaffolds in medicinal chemistry [ 24 , 25 ], the current study is conducted to evaluate anti-α-glycosidase properties of newly designed phenoxymethybenzoimidazole coupled different thiazole-triazole acetamide ( 9a-n ) derivatives. Kinetic studies of the most potent compounds were also performed to evaluate their inhibition pattern against α-glycosidase.…”

A One-Pot Six-Component Reaction for the Synthesis of 1,5-Disubstituted Tetrazol-1,2,3-Triazole Hybrids and Their Cytotoxic Activity against the MCF-7 Cell Line

“…Five-membered aromatic nitrogenous heterocyclic systems are mostly considered privileged structures in medicinal chemistry and are widely used in the development of synthetic strategies to obtain complex and structurally diverse libraries of bioactive compounds [1-5], being a topical challenge for organic chemists [6][7][8]. In recent years, 1,5-disubstituted tetrazoles (1,5-DS-T) and 1,2,3-triazoles have become a starting point in drug discovery projects due to their remarkable biological activities and their presence in marketed drugs, such as cephalosporin-like antibiotics, cilostazol, tazobactam, ticagrelor, and rufinamide [9][10][11][12][13][14]. In parallel, medicinal chemistry has developed molecular hybridization as a promising strategy to achieve highly active compounds with good selectivity and a desirable pharmacokinetic profile.…”

“…The binding of at least two bioactive motifs (pharmacophores) or privileged structures in a single molecule is the essence of molecular hybridization [15][16][17]. Thus, heterocyclic compounds, such as 1,5-DS-T or 1,2,3-triazoles, and molecular hybridization make a powerful combination in the generation of libraries of compounds with potential biological activity [12,[18][19][20][21]. This synergy is even more favored if efficient synthetic strategies such as isocyanide-based multicomponent reactions (I-MCR) are applied [22][23][24].…”