Synthesis and antimicrobial activity of N-(1,2-benzisothiazol-3-yl)amidines.
Several N-(1,2-benzisothiazol-3-yl)amidines were synthesized and examined for their in vitro antimicrobial activity. Some of the compounds studied were effective against bacteria and fungi. Amidines carrying unsaturated alkylic chains showed the highest antimicrobial activity, the propenyl derivative 7 proving to be the most potent with minimum inhibitory concentrations of 25 micrograms/ml against Gram positive bacteria and mould and of 3-12 micrograms/ml against yeasts. The results indicate that an unsaturated moiety is an important function for enhancing the antimicrobial activity in the compounds under investigation.
Vicini
P
P
Dipartimento Farmaceutico, Università di Parma, Italy.
Zani
F
F
D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D005658:Fungi / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000578:Amidines; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D013844:Thiazoles