Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

Abstract

A new series of [1,2,4]-triazole bearing amino acid derivatives were synthesized under green chemistry conditions and evaluated for their antimicrobial activities.

The Synthesis, Antimicrobial Activity, and Molecular Docking of New 1, 2, 4-Triazole, 1, 2, 4-Triazepine, Quinoline, and Pyrimidine Scaffolds Condensed to Naturally Occurring Furochromones

“…Thus, the existence of these functional groups leads to lipophilic groups in diverse places on the triazepine, pyrimidine, quinoline, triazole, pyran, and phenyl rings, and hydrophobic reactions of the triazolopyrimidine, furochromenotriazepine, and furochromenoquinoline moieties at the more active site. In current work and previous studies, most types of bacteria and fungi are affected by this class of heterocyclic compounds [ 9 , 10 , 33 , 34 , 35 , 36 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 ].…”

“…All the newly synthesized compounds of the furochromone derivatives were tested in vitro for their antimicrobial activities at a minimum inhibitory concentration [ 9 , 10 , 33 , 34 , 35 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 ] versus various bacteria and fungi; the results are shown in Table 1 and Table 2 . Some of these compounds showed high antimicrobial activity, comparable to that of cefotaxime sodium (MIC = 1–4 μmol mL −1 ).…”

“…The newly synthesized compounds were dissolved in dimethyl sulfoxide (DMSO) and tested for their antimicrobial activity by the agar disk diffusion technique. Cefotaxime sodium and nystatin [ 9 , 10 , 33 , 34 , 35 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 ] were used as standard drugs for the antibacterial and antifungal assays, respectively. A solution of 100 μg mL −1 of the tested compound and microplate wells 1 cm in diameter were used.…”

“…The plate was incubated for 24 h at 37 °C. For the assessment of the minimum inhibitory concentration (MIC) by serial plate dilution [ 9 , 10 , 33 , 34 , 35 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 ], 5 mg of each tested compound was dissolved in 1 mL of DMSO separately to prepare stock solutions. Serial dilutions were prepared from each stock solution.…”

Design, Synthesis and in Vitro Antifungal Mechanism of Novel Phenylalanine Derivatives

“…Studies have indicated that natural products have unique biological functional diversity and chemical diversity, which give them unique advantages in drug molecular design [6–8] . In recent years, the derivation of molecular structures from natural products has been one of the most effective methods to develop and design drugs with unique mechanisms of action [9,10] .…”