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Molecules ; 12(10): 2413-26, 2007 Oct 30.
Article in English | MEDLINE | ID: mdl-17978766

ABSTRACT

Synthesis of ten 3-(arylideneamino)-2-phenylquinazoline-4(3H)-ones is reported. All the compounds contained a common phenyl group at the 2-position, while the substituents on the arylideneamino group were varied. The compounds were investigated for their antimicrobial activity against both Gram-positive (Staphylococcus aureus 6571 and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli K12 and Shigella dysenteriae 6) using a turbidometric assay method. It was found that the incorporation of the 3-arylideneamino substituent enhanced the anti-bacterial activity of the quinazolone system. The preliminary QSAR studies were done using some computer derived property descriptors, calculated values of partition coefficients as well as usual Hammett's sigma constants and the substituent's molar refractivity.


Subject(s)
Anti-Bacterial Agents/pharmacology , Quantitative Structure-Activity Relationship , Quinazolines/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Bacillus subtilis/drug effects , Escherichia coli/drug effects , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Structure , Quinazolines/chemical synthesis , Quinazolines/chemistry , Shigella dysenteriae/drug effects , Staphylococcus aureus/drug effects
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