Zani F, Massimo G, Coghi E, Bellotti A, Mazza P
Istituto di Technica Farmaceutica, Università di Parma, Italy.
Farmaco. 1990 Nov;45(11):1219-28.
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.
描述了一些1-酰基-3-酰亚氨基-2,1-苯并异噻唑啉的抗菌、抗真菌和遗传毒性活性的体外评估。化合物55、58、60和62表现出选择性抗菌活性。化合物1、2、30、59和63对灰葡萄孢有活性，化合物6、20、39和54对瓜果腐霉有活性。在枯草芽孢杆菌rec-试验中，化合物45、46、54、55、57和61表现出DNA损伤活性。通过沙门氏菌-微粒体试验，化合物10、28、29、40、44、47-53、56、58-60、62和63也被证实并表现出遗传毒性活性。结构与遗传毒性活性之间的关系表明，除化合物27外，所有含有芳香族-NO2基团的化合物均有活性。在脂肪链中含有-CH2Cl基团的衍生物中，只有化合物40表现出诱变活性。
