Patel Navin B, Patel Virendra N, Patel Hemant R, Shaikh Faiyaz M, Patel Jaymin C
Department of Chemistry, Veer Narmad South Gujarat University, Surat-395 007, India.
Acta Pol Pharm. 2010 May-Jun;67(3):267-75.
2-[(2,6-Dichlorophenyl)amino]phenylacetic acid (A) on reaction with thionyl chloride gave corresponding acid chloride (B). A series of (4-oxo-thiazolidinyl)sulfonamides of quinazolin-4(3H)ones (4a-l) were prepared from Schiff bases (3a-l) of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-[(4-aminophenyl)sulfonamido-1-yl]quinazolin-4(3H)one (D) and substituted aromatic aldehyde. Newly synthesized compounds have been examined on the basis of elemental analysis, IR, 1H NMR and 13C NMR spectra. Antibacterial activity (minimum inhibitory concentration - MIC) against Gram-positive (S. aureus & S. pyogeneus) and Gram-negative (P. aeruginosa and E. coli) bacteria, as well as antifungal acivities (MIC) against C. albicans, A. niger and A. clavatus were determined by broth dilution method. Some of the compounds were endowed with a remarkable antibacterial as well as antifungal acivities.
2-[(2,6-二氯苯基)氨基]苯乙酸(A)与亚硫酰氯反应生成相应的酰氯(B)。由2-[2-(2,6-二氯苯基)氨基]苯甲基-3-[(4-氨基苯基)磺酰胺基-1-基]喹唑啉-4(3H)酮(D)与取代芳香醛的席夫碱(3a-l)制备了一系列喹唑啉-4(3H)酮的(4-氧代噻唑烷-2-基)磺酰胺(4a-l)。通过元素分析、红外光谱、1H核磁共振谱和13C核磁共振谱对新合成的化合物进行了表征。采用肉汤稀释法测定了对革兰氏阳性菌(金黄色葡萄球菌和化脓性链球菌)和革兰氏阴性菌(铜绿假单胞菌和大肠杆菌)的抗菌活性(最低抑菌浓度-MIC)，以及对白色念珠菌、黑曲霉和棒曲霉的抗真菌活性(MIC)。部分化合物具有显著的抗菌和抗真菌活性。
