10.1016/0223-5234(87)90277-7
The research aimed to synthesize and evaluate the anti-microbial properties of 2-methyl-3-substituted-4(3H)-quinazolinones, a class of quinazolinone derivatives known for their broad spectrum of biological activities, including anti-microbial effects. The study focused on derivatives with a thiazoline or thiazolidinedione moiety at the 3-position, which were hypothesized to exhibit anti-bacterial and anti-fungal activities. The synthesis involved the use of 3-amino-2-methyl-4(3H)-quinazolinone and various alkyl-, aryl-, or aralkylisothiocyanates to form 2-methyl-3-substituted thiocarbamoylamino-4(3H)-quinazolinones, which were then cyclized to form thiazoline and thiazolidinone derivatives. The anti-microbial activity of these compounds was tested against Gram-positive and Gram-negative bacteria. The results were generally discouraging, with most compounds showing little activity, but some, like compounds 5, 8, 10, and 11, exhibited higher activity against Gram-positive bacteria. Notably, compounds 5 and 8 were equipotent, and compounds 11 and 12 were more potent against Bacillus cereus compared to the reference standard, penicillin G. The study concluded that while the majority of the synthesized compounds did not show promising anti-microbial activity, a few specific derivatives demonstrated potential as anti-microbial agents.
10.1002/ardp.19873200609
The research investigates the condensation reaction between 5-phenyl-1,2,4-triazole-3-thiol and monochloroacetaldehyde. The purpose is to study the chemical and spectral properties of the resulting products. The study found that the reaction in acetone at room temperature yielded a compound that did not react with 2,4-DNPH and was identified as a hydroxythiazolin derivative through IR, UV, and 1H-NMR spectroscopy. Further reactions under different conditions produced various derivatives, including thiazolo[3,2-b]1,2,4-triazoles and thiazolines. The research concludes that the structure and properties of these compounds are influenced by the reaction conditions and the presence of different functional groups, providing insights into the mechanisms and outcomes of such condensation reactions.