Microwave assisted synthesis of 1H-tetrazole-based flavonoid derivatives and their antimicrobial activity

Abstract

A series of novel tetrazole scaffolds containing chalcones 4a-e and aurones 5a-e were synthesized under conventional and microwave irradiation conditions. All the newly synthesized compounds were characterized by IR, NMR and mass spectral data. Furthermore, the title compounds were screened in vitro for their antimicrobial activity against bacteria, such as Staphylococus aureus, Bacillus subtilis, Klebsiella pneumoniae and Escherichia coli, as well as fungi, such as Aspergillus niger, A. flavus and Fusarium oxysporum. Some of the compounds showed very good activity compared to standard drugs against all the tested pathogenic bacteria and fungi.

Design, Synthesis and Evaluation of Aurone and Indanone Derivatives as Novel Antibacterial Agents

“…Searching for antimicrobial candidates against drug-resistant bacteria from natural products and their derivatives is a popular strategy for the antibiotic resistance. The skeleton of aurone has been demonstrated to be potential for the antibacterial agents and many aurones based on modifications on Bring had been explored (Figure 1) [12][13][14][15][16][17][18][19][20]. Furthermore, it is still active when the benzofuranone was hopped to indanone, and the lipid solubility of the compound were greatly improved as well [21][22][23].…”

Microwave-Assisted Synthesis of Tetrazole Based Biphenyls Derivatives and Their Antimicrobial Activity

“…Tetrazole is a key structural motif in heterocyclic chemistry, it has been found in many drug molecules [1][2] and these possess wide a range of biological activities. [3][4][5][6][7][8][9][10] Aryl-aryl bond development is very significant in organic synthesis and has a broad range of applications in industrial interest, as well as the synthesis of pharmaceuticals, polymers, herbicides and other material. 11 The palladium-catalyzed by aryl halides with aryl boronic acid known as Suzuki cross-coupling reaction, is one of the most important and potent methods for the construction of biphenyl and polyaryls, [12][13][14] due to the broad functional group tolerance and the low toxic reagents and the probability of using of green solvents as reaction medium.…”