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Abstract: A series of bicyclic N-substituted and unsubstituted β-lactams were synthesized and evaluated as targeted potential antimalarials. The compounds MNR4 and MNR5 were found to have highest potency against Plasmodium falciparum in vitro. [Copyright &y& Elsevier]

Abstract: Five series of curcumin derivatives with sulfonamides 3a–3e, 4a–4e, 5a–5e, 6a–6e and 7a–7e have been synthesized and evaluated for in vitro antibacterial activity against selected medically important gram-(+) and gram-(−) bacterial species viz. Staphylococcus aureus, Bacillus cereus, Salmonella typhi, Pseudomonas aeruginosa and Escherichia coli, and antifungal activity against few pathogenic fungal species viz. Aspergillus niger, Aspergillus flavus, Trichoderma viride and Curvularia lunata. The cytotoxicity has been determined by measuring IC50 values against human cell lines HeLa, Hep G-2, QG-56 and HCT-116. Among the compounds screened, 3a–3e showed the most potent biological activity against tested bacteria and fungi. Compounds 3a–3e displayed higher cytotoxicity than curcumin. The curcumin derivatives were also evaluated for in vivo anti-inflammatory activity. In contrast, the compounds 6a–6e and 7a–7e showed dramatically decrease in biological activity. [Copyright &y& Elsevier]

Abstract: 3,4-Dihydropyrimidinones of curcumin were synthesized in excellent yield by multi-component one-pot condensation of curcumin, substituted aromatic aldehydes and urea/thiourea under solvent free conditions using SnCl2·2H2O catalyst. All the synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, Mass spectra as well as elemental analyses. The synthesized compounds 4a–n were evaluated for their synergistic antimicrobial (antibacterial and antifungal) activity against bacteria and fungi. Zone of inhibition was measured by adopting disc diffusion method. In vitro minimum inhibitory concentrations were measured using broth microdilution and food poisoning method. In addition to this in vitro cytotoxicity of synthesized compounds against three human cancer lines Hep-G2, HCT-116 and QG-56 were also evaluated. Most of the compounds showed interesting antimicrobial and cytotoxic activity as compared to curcumin, that is, the compounds derived from 2-hydroxy benzaldehyde, 4-hydroxy benzaldehyde and 4-hydroxy-3-methoxy benzaldehyde showed the highest biological activity as compared to other compounds. [Copyright &y& Elsevier]

Abstract: A novel, one-pot, simple, efficient procedure for 4H-pyrimido[2,1-b]benzothiazole (4a–h), pyrazole (6a–d) and benzylidene (7a–d) derivatives of curcumin under solvent and solvent free conditions in microwave with good yield is have been synthesized. The synthesized compounds were evaluated for their antibacterial activity against gram-positive and gram-negative bacteria viz. Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus and Providencia rettgeri and antifungal activity against fungi viz Aspergillus niger, Aspergillus fumigates, Aspergillus flavus. Detailed mechanistic study shows reaction proceeds through Knoevenagel type intermediate 3a which has been suggested as key intermediate for reaction (). [Copyright &y& Elsevier]