Microwave assisted synthesis of novel Pyrazole derivatives and their biological evaluation as anti-bacterial agents

Aim and Objective: Microwave-assisted condensation of acetophenone 1 and aromatic aldehydes 2 gave chalcone analogs 3, which were cyclized to pyrazole derivatives 6a-f via the reaction with hydrazine hydrate and oxalic acid in the presence of the catalytic amount of acetic acid in ethanol. Materials and Methods: The structural features of the synthesized compounds were characterized by melting point, FT-IR, 1H, 13C NMR and elemental analysis. Results: The antibacterial activities of the synthesized pyrazoles was evaluated against three gram-positive bacteria such as Enterococcus durans, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria such as Escherichia coli and Salmonella typhimurium. Conclusion: All the synthesized pyrazoles showed relatively high antibacterial activity against S. aureus strain and none of them demonstrated antibacterial activity against E. coli.

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Microwave-Assisted Synthesis of Schiff Bases of Isoniazid and Evaluation of Their Anti-Proliferative and Antibacterial Activities

Molbank ◽

10.3390/m1189 ◽

2021 ◽

Vol 2021 (1) ◽

pp. M1189

Author(s):

Bayan Ahed Al-Hiyari ◽

Ashok K. Shakya ◽

Rajashri R. Naik ◽

Sanaa Bardaweel

Keyword(s):

Antibacterial Activity ◽

Schiff Bases ◽

Aromatic Aldehydes ◽

Antibacterial Activities ◽

Microwave Assisted Synthesis ◽

Microwave Assisted ◽

Ic50 Values ◽

In Vitro Inhibition ◽

Mcf 7

Three new Schiff bases of isoniazid were synthesized using microwave-assisted synthesis and conventional condensation with aromatic aldehydes. Synthesized compounds were characterized using elemental analysis, IR, NMR, and Mass spectroscopy. Synthesized compounds were evaluated for antiproliferative activity against MCF-7 cell line. The IC50 values were from 125 to 276 µM. The compounds were also evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli. Results showed that the synthesized compounds produce significant antibacterial activity in vitro. Inhibition of compounds ranged from 13 to 18 mm.

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Microwave-assisted synthesis and biological evaluation of thiazole-substituted dibenzofurans

Heterocyclic Communications ◽

10.1515/hc-2017-0247 ◽

2018 ◽

Vol 24 (3) ◽

pp. 171-176

Author(s):

N.H. Kumar Baba ◽

D. Ashok ◽

Boddu Ananda Rao ◽

Sarasija Madderla ◽

N.Y.S. Murthy

Keyword(s):

Pseudomonas Aeruginosa ◽

Antibacterial Activity ◽

Antimycobacterial Activity ◽

Biological Evaluation ◽

Microwave Assisted Synthesis ◽

Good Activity ◽

Gram Negative ◽

Microwave Assisted ◽

Synthesis And Biological Evaluation

AbstractNew thiazole-substituted dibenzofurans 7a–j were synthesized from dibenzofuran derivatives 5a–b and substituted thiosemicarbazones 6a–h under conventional and microwave irradiation conditions. The structures of all products were established on the basis of analytical and spectral data. The synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative strains. Compounds 7b, 7d and 7h are active against Bacillus subtilis (+ve), and compound 7i displays good activity against Pseudomonas aeruginosa (-ve) strain. Compounds 7a–j were also evaluated for their in vitro antimycobacterial activity, and compound 7b shows antimycobacterial activity against Mycobacterium bovis strain.

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Microwave-assisted synthesis of 1,2,3,4-tetrahydroisoquinoline sulfonamide derivatives and their biological evaluation

Journal of the Serbian Chemical Society ◽

10.2298/jsc200802076m ◽

2020 ◽

pp. 76-76

Author(s):

Stanimir Manolov ◽

Iliyan Ivanov ◽

Dimitar Bojilov

Keyword(s):

Antibacterial Activity ◽

Thin Layer ◽

In Silico ◽

Biological Evaluation ◽

Reversed Phase ◽

Microwave Assisted Synthesis ◽

Microwave Assisted ◽

In Vitro Inhibition ◽

Layer Chromatography

Herein we report an alternative eco-friendly method for the synthesis of 1,2,3,4-tetrahydroisoquinoline sulfonamide derivatives. All obtained compounds were screened for their in vitro inhibition of albumin denaturation, antioxidant, antitryptic, and antibacterial activity and have shown significant results. The lipophilicity was established using both reversed-phase thin layer chromatography and in silico calculations.

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