Boddu Ananda Rao

Design and synthesis of new 1,2,3-triazole-pyrazole hybrids as antimicrobial agents

In the present study, a series of novel 1,2,3-triazoles derivatives (4a–4c) were synthesized by the 1,3-dipolar cycloaddition (click-reaction) of 1-phenyl-3-[2-(prop-2-yn-1-yloxy)phenyl substituted]-1H-pyrazole-4-carbaldehyade (3a–3c) with various aryl azides in the presence of sodium ascorbate and copper sulphate with high yields. The required precursors 3a–3c were synthesized by the reaction of 1-(2-hydroxy phenyl substituted)ethanones (1a–1c) with propargyl bromide via 1-[2-(prop-2-yn-1-yloxy)phenyl substituted] ethanone (2a–2c), followed by reaction with phenyl hydrazine. The newly synthesized 1,2,3-triazole-pyrazole derivatives were characterized by analytical and spectral data. All synthesized compounds were evaluated in vitro for their antibacterial and antifungal activity. The most active compounds 4a5–4a7 demonstrated a broad spectrum of antibacterial activity against all strains used for testing. Compounds (4a4, 4b1, 4c1, 4c2) demonstrated significant antifungal activity at the concentration of 10 μg/mL.

Synthesis, characterisation, and antibacterial activity of some novel vanillin related hydrazone derivatives bearing 1,2,3-triazole ring

Vanillin, hydrazone and 1,2,3-triazole containing functional groups derivatives demonstrate antibacterial activity. In the present work, we present synthesis of eight new vanillin related hydrazone derivatives bearing 1,2,3-triazole ring skeleton 9a–9e, 10a–10e obtained with high yields by the coupling of aldehydes 6 and 7 with substituted benzohydrazides 8a–8e in ethanol. IR, NMR and MS data and elemental analysis confirm the structures of products. All title compounds were evaluated in vitro for their antibacterial activity against a panel of Gram positive and Gram negative bacteria and compounds 9d and 10d exhibited high activity.

Microwave-assisted synthesis of bis(N-substituted thiazol-2-amine) derivatives and their biological activities

Abstract New 4,4′-(4,6-dimethoxy-1,3-phenylene)-bis(N-substituted thiazol-2-amine) derivatives 5a–j were synthesized from 1,1′-(4,6-dimethoxy-1,3-phenylene)-bis(2-bromoethanone) 3 and substituted thioureas 4a–j under conventional and microwave irradiation conditions. All products were subjected to in vitro antibacterial and anti-TB evaluation. Some of the compounds exhibit good activities against Bacillus subtilis (+ve), Escherichia coli (−ve) strains and Mycobacterium tuberculosis H37Rv.

Synthesis and Antimicrobial Activity of ( Z )-3-{[3-Oxobenzofuran-2(3 H )-ylidene]methyl}-4 H -chromen-4-one Derivatives

A series of (Z)-3-{[3-oxobenzofuran-2(3H)-ylidene]methyl}-4H-chromen-4-one derivatives have been synthesized from 2-hydroxyl acetophenones by the Vilesmeier–Haack reaction, Claisen–Schmidt reaction and mercury(II) acetate/cupric bromide. All the synthesized compounds were characterized by IR, 1H and 13C NMR, and mass spectral data and elemental analysis. The products were tested for their in vitro antimicrobial activity.

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

Abstract New 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.