Zani F, Vicini P
Dipartimento Farmaceutico, Via delle Scienze 78, 43100 Parma, Italy.
Arch Pharm (Weinheim). 1998 Jun;331(6):219-23. doi: 10.1002/(sici)1521-4184(199806)331:6<219::aid-ardp219>3.0.co;2-u.
Some sulfonamide and sulfonylurea derivatives of unsubstituted and 5-methylsubstituted 1,2-benzisothiazole were studied in vitro for their antimicrobial properties against bacteria and fungi. Compounds 7 and 8 exhibited good antibacterial activity against Gram positive bacteria. A strong synergism was observed when their growth-inhibitory effect was assayed in combination with trimethoprim by using Bacillus subtilis and Staphylococcus aureus as test microorganisms. The antimycotic action of benzenesulfonylurea derivative 9 was very marked for Madurella mycetomatis and dermatophytes Epidermophyton floccosum, Microsporum gypseum and Trichophyton spp.. Structure-activity relations are discussed.
对未取代的和5-甲基取代的1,2-苯并异噻唑的一些磺胺和磺酰脲衍生物进行了体外研究，考察它们对细菌和真菌的抗菌性能。化合物7和8对革兰氏阳性菌表现出良好的抗菌活性。当以枯草芽孢杆菌和金黄色葡萄球菌作为测试微生物，将它们与甲氧苄啶联合测定生长抑制作用时，观察到强烈的协同作用。苯磺酰脲衍生物9对马杜拉足分支菌和皮肤癣菌絮状表皮癣菌、石膏样小孢子菌和毛癣菌属的抗真菌作用非常显著。讨论了构效关系。
