Chio L C, Bolyard L A, Nasr M, Queener S F
Department of Pharmacology and Toxicology, Indiana University School of Medicine, Indianapolis 46202-5120, USA.
Antimicrob Agents Chemother. 1996 Mar;40(3):727-33. doi: 10.1128/AAC.40.3.727.
Sulfanilanilides with 3',5'-halogen substitutions had Ki values 6- to 57-fold lower than the Ki of sulfamethoxazole when tested against dihydropteroate synthase from Toxoplasma gondii. The compounds acted as competitive inhibitors. These compounds were also active against dihydropteroate synthase from Pneumocystis carinii, Mycobacterium avium, and Escherichia coli but were not significantly more active than sulfamethoxazole. The compounds were significantly more active in culture than were standard agents. Against T. gondii in culture, 50% inhibitory concentrations were 7- to 30-fold lower than that of sulfadiazine; against P. carinii in culture, a concentration of 100 microM caused 33 to 95% inhibition of growth, compared with 9% inhibition with 100 microM sulfamethoxazole.
当针对来自刚地弓形虫的二氢蝶酸合酶进行测试时，具有3'，5'-卤素取代的磺胺苯胺类化合物的Ki值比磺胺甲恶唑的Ki值低6至57倍。这些化合物起竞争性抑制剂的作用。这些化合物对来自卡氏肺孢子虫、鸟分枝杆菌和大肠杆菌的二氢蝶酸合酶也有活性，但活性并不比磺胺甲恶唑显著更高。这些化合物在培养物中的活性明显高于标准药物。在培养物中，针对刚地弓形虫，50%抑制浓度比磺胺嘧啶低7至30倍；针对卡氏肺孢子虫，100微摩尔浓度导致生长抑制33%至95%，而100微摩尔磺胺甲恶唑的抑制率为9%。
