Antibacterial, antifungal and cytotoxic properties of some sulfonamide-derived chromones.
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 flexener) 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.
Chohan
Zahid H
ZH
Department of Chemistry, Bahauddin Zakariya University, Multan-60800, Pakistan. zchohan@mul.paknet.com.pk
Rauf
Abdul
A
Naseer
Muhammad M
MM
Somra
Muhammad A
MA
Supuran
Claudiu T
CT
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D001156:Artemia / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects / Q000378:metabolism; D002867:Chromones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D005658:Fungi / Q000187:drug effects / Q000378:metabolism; D007928:Lethal Dose 50; D008826:Microbial Sensitivity Tests; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D002867:Chromones; D013449:Sulfonamides