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Efficient Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and -thiones Using ZrO2 as a Reusable Heterogeneous Catalyst. -(GOPALAKRISHNAN*, M.; SURESHKUMAR, P.; KANAGARAJAN, V.; THANUSU, J.; GOVINDARAJU, R.; EZHILARASI, M. R.; Lett.

A convenient synthesis of 1-thiocarbamoyl-3-phenyl-5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives (2a-2g) was carried out by the condensation reaction of (E)-3-(phenyl)-1-(biphenyl-2-yl)-3-arylprop-2-en-1-ones (1a-1g) with thiosemicarbazide, sodium hydroxide as a catalyst in the presence of ethanol as solvent. Further, (E)-3-(phenyl)-1-(biphenyl-2-yl)-3-arylprop-2-en-1-ones were synthesized by the Claisen-Schmidt condensation reaction of substituted aldehydes with 4-acetylbiphenyl in the presence of basic ethanolic solution. The structure of synthesized compounds were confirmed by FT-IR, 1 H NMR, 13 C NMR and 1 H-1 H COSY. The antimicrobial susceptibility tests of synthesized compounds were screened against Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Pseudomonas aeruginosa. The docking studies also carried out by using 1UAG receptor for all the synthesized compounds (2a-2g).

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The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1one derivatives chemical structures were confirmed from spectral data such as FT-IR, 1 H and 13 C NMR. 2-Pyrazoline derivatives were docked with bacterial (1UAG) and breast cancer (1OQA) protein. Based on high binding affinity score, the best compound was subjected to in vitro anticancer activity by MTT assay. Also, antimicrobial activity were studied for synthesized 2-pyrazoline derivatives.

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A novel approach towards the synthesis of spiropiperidinyl 1,2,4-triazolidine-3-thiones was proposed, exploiting microwave activation coupled with solvent-free reaction conditions. In search for new leads towards potent antimicrobial agents, we tested all the synthesized compounds for their in vitro antibacterial activity against Bacillus subtilis and Micrococcus luteus and antifungal activity against Aspergillus niger, Candida albicans, Candida-6, and Candida-51. Two of the compounds exerted strong in vitro antibacterial activity against B. subtilis and M. luteus, and all the synthesized compounds were potent against the tested fungal strains.