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An efficient method is described for the synthesis of 2-aminobenzothiazolomethyl naphthol derivatives by one-pot three-component reaction of aldehydes, 2-naphthol, and 2-amino benzothiazole using triton X-100 as a catalyst in water with good yield. The synthesized compounds have been characterized by IR, H NMR, C NMR, and mass spectra. The synthesized compounds were screened for their antibacterial activity against gram-positive and gram-negative bacteria viz. Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus, and Providencia rettegeri and fungal activity against fungal strain such as Aspergillus niger, Aspergillus fumigatus, and Aspergillus flavus. Synthesized compounds exhibited MICs value between 3.25 and 12.5 μg/mL against bacterial strains and 6.25 and 12.5 μg/mL against fungal strains as shown in Tables 4 and 5, respectively. Derivatives 5c and 5h were equipotent activity as ciprofloxacin against E. coli and 5k against P. aeruginosa and B. cereus. Derivatives 5e, 5g, and 5k exhibited excellent antifungal activity against all tested fungal strains. Ciprofloxacin and fluconazole have been used as standard drugs for antibacterial and antifungal activity, respectively. [ABSTRACT FROM AUTHOR]

Aluminum trichloride acts as readily available, inexpensive, and efficient catalyst for one-pot three-component condensation reaction of aldehydes, dicarbonyl, and 2-amino benzothiazole under the solvent-free conditions to afford the 4H-pyrimido[2,1-b][1,3]benzothiazole derivatives 4 with good yield. The compounds synthesized in this study were evaluated for their antibacterial activities against gram-positive and gram-negative bacteria, viz., Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus, and Providencia rettegeri. Compounds 4c, 4d, 4f, 4g, and 4h showed their good activities against tested bacterial species. Pyrimidine derivatives 4d, 4f, and 4g have shown good antifungal activities against tested fungal strains, such as Aspergillus niger, Aspergillus fumigates, Aspergillus flavus, etc. Graphical abstract: [Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

Synthesis and evaluation of the antimalarial activity of new pyridine quinoline hybrid molecules against a chloroquine-susceptible strain of Plasmodium falciparum and as inhibitors of β-hematin formation are described. Two novel pyridine quinoline hybrid molecules and one bisquinoline molecule were synthesized and purified by column chromatography and evaluated for antimalarial and haem polymerization inhibition (HPIA) activities. The molecules were found to be very good haem polymerization inhibitors but showed poor antimalarial activity. This was attributed to their low vacuole accumulation ratio (VAR) in comparison to chloroquine. These molecules can be used as templates for designing new antimalarials targeting haem detoxification pathway of malaria parasite. Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids B.N Acharya, D. Thavaselvam# and M.P Kaushik* Discovery Centre, Process Technology Development Division Defence R & D Establishment, Jhansi Road, Gwalior-474002 (MP) INDIA #Division of Microbiology, Defence Research and Development Establishment,Gwalior-474002, India Synthesis and evaluation of antimalarial activity of new pyridine–quinoline hybrid molecules against a chloroquine-susceptible strain of Plasmodium falciparum and as inhibitors of β-hematin formation are described. [ABSTRACT FROM AUTHOR]