An
economic, sustainable, and straightforward environmentally friendly
synthesis of highly diversified polyfunctional dihydrothiophenes is
successfully achieved via diisopropyl ethyl ammonium acetate as a
room-temperature ionic liquid. Multicomponent synthesis contains domino
processes; the benefit of this present protocol is highlighted by
its readily available starting materials, superior functional group
tolerance, purity of synthesized compounds was checked by high-performance
liquid chromatography results in up to 99.7% purity for the synthesized
compounds, reaction mass efficiency, effective mass yield, and excellent
atom economy. In addition, a series of 2-(N-carbamoyl
acetamide)-substituted 2,3-dihydrothiophene analogs were synthesized,
and selected samples were chosen for testing their in vitro antibacterial
and antifungal activities. Furthermore, a molecular docking study
against sterol 14α-demethylase could provide valuable insight
into the mechanism of antifungal action providing an opportunity for
structure-based lead optimization.
In Search of novel antimicrobial agents with improved potency, we designed and synthesized a series of 3-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)-2-(4-fluorophenyl)-4H-chromen-4-ones 5a-f using click chemistry. The structures of synthesized compounds were found using IR, 1 H NMR, 13 C NMR, and MS. All the synthesized compounds were assayed for their in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa and antifungal activity against Candida albicans, Candida glabrata, and Candida tropicalis by micro broth dilution method. The antimicrobial data suggested that from the series, compounds 3e, 4e, 5e, and 5f shows pronounced antimicrobial activity against the tested strain with low MIC value. Molecular docking study was used to rationalize binding interaction at the active site and the results showed good binding interaction.Electronic supplementary material The online version of this article (
Herein, we report a convenient and facile methodology for the synthesis of new series of pyrazole and pyrimidine derivatives 2a–f and 3a–f under ultrasound irradiation. Pyrazole and pyrimidine derivatives have been synthesized in better yields and shorter reaction times compared with the conventional method. The chemical structures of all the synthesized compounds were elucidated by their IR, 1H NMR, 13C NMR, MS, and elemental analysis. Further, the target compounds were screened for their antimicrobial activity against four bacteria (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa) and two fungi (Candida albicans, Aspergillus niger). In particular, compounds 2a, 2d, 2e, 3a, 3e, and 3f exhibited potent antimicrobial activity.
In the development of novel antimicrobial agents, we synthesized novel 1,2,3‐triazole‐based pyrazole and pyrimidine derivatives 6(a–f) and 7(a–f) by ultrasound‐assisted method. The synthesized compounds were characterized by IR, 1H NMR, 13C NMR, MS, and elemental analysis. All compounds were assessed in vitro for their efficacy as antimicrobial agents against four bacteria (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa) and two fungi (Candida albicans and Aspergillus niger). In particular, compounds 6a, 6e, 7a, 7c, and 7e exhibited highly potent antimicrobial activity.
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