Gangadharam P R, Candler E R
Am Rev Respir Dis. 1977 Apr;115(4):705-8. doi: 10.1164/arrd.1977.115.4.705.
A series of 12 compounds, consisting of 3 known antileprosy drugs (dapsone, B663, and Ciba 1906) and 9 structural derivatives of dapsone, were tested for their antimycobacterial activity against 50 strains of Mycobacterium intracellulare. Detailed investigations of B663, the only compound showing considerable in vitro activity, were carried out. All of the strains of M. intracellulare were inhibited by a B663 concentration of 1.6 mug per ml, and 88% were inhibited by a drug concentration of 0.8 microng per ml. The rate of emergence of in vitro resistance was similar to that of M. tuberculosis against streptomycin and isoniazid. Preliminary experiments indicated that the action of the drug on M. intracellulare may be bacteriocidal in nature.
对由3种已知抗麻风病药物（氨苯砜、B663和汽巴1906）以及9种氨苯砜结构衍生物组成的12种化合物，进行了针对50株胞内分枝杆菌的抗分枝杆菌活性测试。对唯一显示出可观体外活性的化合物B663进行了详细研究。所有胞内分枝杆菌菌株在B663浓度为每毫升1.6微克时均受到抑制，88%的菌株在药物浓度为每毫升0.8微克时受到抑制。体外耐药性的出现率与结核分枝杆菌对链霉素和异烟肼的耐药率相似。初步实验表明，该药物对胞内分枝杆菌的作用本质上可能是杀菌性的。
