Antibacterial, antifungal and cytotoxic properties of some sulfonamide-derived chromones

被引:44
作者
Chohan, Zahid H.
Rauf, Abdul
Naseer, Muhammad M.
Somra, Muhammad A.
Supuran, Claudiu T.
机构
[1] Univ Florence, Lab Chim Bioorgan, I-50019 Sesto Fiorentino, Florence, Italy
[2] Islamia Univ, Dept Chem, Bahawalpur, Pakistan
[3] Bahauddin Zakariya Univ, Dept Chem, Multan 60800, Pakistan
关键词
sulfonamide; chromones; antibacterial; antifungal; cytotoxicity;
D O I
10.1080/14756360500533059
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
A series of antibacterial and antifungal sulfonamide (sulfanilamide, sulfaguanidine, sulfamethaxozole, 4-aminoethylbenzene-sulfonamide and 4-amino-6-trifluoromethyl-benzene-1,3-disulfonamide) derived chromones, previously reported as inhibitors of carbonic anhydrase, have been screened for in-vitro antibacterial activity against four Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi and Shigella flexeneri) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains, and for in-vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, Candida glaberata. All compounds (1) - (5) showed significant antibacterial activity against all four Gram-negative species and both Gram-positive species. However, three of them, (1), (4) and (5), were found to be comparatively much more active compared to (2) and (3). Of these, (5) was found to be the most active one. For antifungal activity, generally compounds (1) and (2) showed significant activity against more than three strains whereas (3) - (5) also showed significant activity against varied fungal strains. In the brine shrimp bioassay for in-vitro cytotoxic properties, only two compounds, (4) and (5) displayed potent cytotoxic activity, LD50 = 2.732 X 10(-4) M) and LD50 = 2.290 X 10(-4)M) respectively, against Artemia salina.
引用
收藏
页码:173 / 177
页数:5
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