Biological studies on 2,1-benzisothiazole derivatives. I. Evaluation of antibacterial, antifungal and genotoxic activities of 1-acyl-3-acylimino-2,1-benzisothiazolines.
The in vitro evaluation of antibacterial, antifungal and genotoxic activities of some 1-acyl-3-acylimino-2,1-benzisothiazolines is described. Compounds 55, 58, 60 and 62 exhibited a selective antibacterial activity. Compounds 1, 2, 30, 59 and 63 were active against Botrytis cinerea, compounds 6, 20, 39 and 54 against Pythium irregulare. DNA-damaging activity in the Bacillus subtilis rec-assay was demonstrated for compounds 45, 46, 54, 55, 57 and 61. By the Salmonella-microsome assay, genotoxic activity was confirmed and demonstrated also for compounds 10, 28, 29, 40, 44, 47-53, 56, 58-60, 62 and 63. Relationships between structure and genotoxic activity showed that all compounds containing an aromatic -NO2 group, except compound 27, were active. Among derivatives containing a -CH2Cl group in the acylic chain, only compound 40 showed mutagenic activity.
Zani
F
F
Istituto di Technica Farmaceutica, Università di Parma, Italy.
Massimo
G
G
Coghi
E
E
Bellotti
A
A
Mazza
P
P
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001412:Bacillus subtilis / Q000187:drug effects / Q000235:genetics; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D007097:Imines / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests; D009152:Mutagenicity Tests; D009153:Mutagens / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D012486:Salmonella typhimurium / Q000187:drug effects / Q000235:genetics; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D007097:Imines; D009153:Mutagens; D013844:Thiazoles