10.3184/030823409X12508790019612
The study investigates the synthesis, reactions, and antimicrobial activity of thieno[2,3-c]pyridazine derivatives. The research involves the reaction of N1-(un)substituted 4-aminosulfonamide with 6-chloropyridothienopyridazine (5) and 8-chloropyrimidothienopyridazine (14) to produce 6-substituted aminopyridothienopyridazine (9) and 8-substituted aminopyrimidothienopyridazine (16) respectively. These derivatives are characterized by analytical and spectroscopic studies and tested for their in vitro antibacterial and antifungal activity against various microorganisms. The study also explores the synthesis of other related compounds such as 7-cyano-3,4,8-triphenylpyrido[2',3' : 4,5]thieno[2,3-c]pyridazin-6(5H)-one (4), 6-chloro-7-cyano-3,4,8-triphenylpyrido[2',3' : 4,5]thieno[2,3-c]pyridazine (5), and their various substituted derivatives. The antimicrobial activity of the synthesized compounds is evaluated against Gram positive bacteria (Staphylococcus aureus, Bacillus subtilis), Gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa), yeast (Candida albicans), and fungi (Aspergillus niger). The results indicate that several compounds exhibit high and very high antimicrobial activity against the tested microorganisms, comparable to standard antibacterial and antifungal agents.
10.1007/s00044-012-0004-3
The study focuses on the synthesis, characterization, and pharmacological evaluation of a series of 1-[2-(6-nitro-4-oxo-2-phenyl-4H-quinazolin-3-yl)-ethyl]3-phenyl-urea derivatives. These compounds were synthesized using an efficient protocol involving reactions with 2-aminobenzoic acid, benzoyl chloride, ethylene diamine, and various phenyl isocyanates. The synthesized compounds were characterized using IR, 1H NMR, 13C NMR spectroscopy, ESI Mass spectrometry, and elemental analysis. The study evaluated the antibacterial and antifungal activities of these compounds against selected strains of bacteria (Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Bacillus subtilis) and fungi (Candida albicans) using Kirby Bauer disk diffusion and broth dilution techniques. The results showed that all synthesized compounds exhibited good antifungal potency against C. albicans, with some compounds showing notable antibacterial activity against certain bacterial strains. The study highlights the potential of these quinazolin-4(3H)-one derivatives as new antimicrobial agents, particularly for their antifungal properties.
10.1007/s11094-016-1392-3
The research investigates the synthesis and biological evaluation of a novel series of 2-azetidinone derivatives combined with quinazolinone. The primary purpose of this study is to develop new antimicrobial and anticancer agents, addressing the growing problem of multidrug-resistant microorganisms and the need for effective cancer treatments. The researchers synthesized 17 different 2-azetidinone derivatives using anthranilic acid as the starting material, and these compounds were characterized using techniques such as IR spectroscopy and 1H NMR. The synthesized compounds were then tested for their antimicrobial activity against bacterial strains including Bacillus subtilis, Staphylococcus aureus, and Escherichia coli, as well as fungal strains Candida albicans and Aspergillus niger. Additionally, the anticancer activity was evaluated against the human breast cancer cell line MCF-7. The results showed that compound 12 exhibited the most potent antimicrobial activity, particularly against S. aureus, B. subtilis, and C. albicans, while compound 5 demonstrated the most significant anticancer activity with an IC50 value of 49.52 μM. The study concludes that these 2-azetidinone derivatives have potential as antimicrobial and anticancer agents, though their activity is generally lower than that of standard drugs.
