A novel series of piperazine‐1,2,3‐triazole bearing dimethyl(((2‐(4‐((1H‐1,2,3‐triazole‐4‐yl)methyl)piperazin‐1‐yl)ethylamino)(2‐hydroxyaryl)methyl)phosphonate derivatives have been prepared via copper‐catalyzed azide‐alkyne 1,3‐dipolar cycloaddition (CuAAC) (Click Reaction) and Schiff base reactions. The synthesized compounds were confirmed by spectral characterization (1H, 13C and 31P NMR, and mass). The title compounds were evaluated for in vitro alpha glucosidase enzyme inhibition and in vitro antioxidant activity using DPPH and H2O2 methods.
A series of new α‐aminophosphonates containing 1,3,4‐thiadiazole moiety (4a–l) were synthesized via a simple, efficient, and one‐pot three‐component Kabachnik–Fields reaction of 2‐amino‐5‐ethyl‐1,3,4‐thiadiazole with various aryl/heteroaryl aldehydes and diethylphosphite under solvent‐free microwave irradiation conditions using phosphosulfonic acid, as a reusable and heterogeneous solid acid catalyst. All the title compounds were screened for radical scavenging activity by DPPH and H2O2 methods, and antimicrobial activity against bacteria (Gram‐positive and Gram‐negative) and fungi using the disc diffusion technique. They exhibited potent in vitro antioxidant and moderate antimicrobial activity.
A simple and efficient one‐pot microwave‐assisted click formation of 1‐(substituted)‐1H‐1,2,3‐triazol‐4‐yl)methyl)diphenylphosphineoxide derivatives via Huisgen regioselective [3+2]‐cycloaddition of an in situ generated organic azides and diphenyl(prop‐2‐yn‐1‐yl)phosphine oxide in highly polar DMSO‐H2O medium. This synthetic protocol is mild, requires shorter reaction time, and afforded products in excellent yields with high regioselectivity.
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