Hachtel G, Haller R, Seydel J K
Pharmazeutisches Institut der Christian-Albrechts-Universität, Kiel.
Arzneimittelforschung. 1988 Dec;38(12):1778-83.
2,4-Diamino-5-benzylpyrimidines 1-23 with lipophilic substitution in the benzylic moiety were synthesized by the morpholino-anilino-procedure. Their effects against various mycobacteria were verified by MIC (minimum inhibitory concentration) in whole cells and I50-measurements in whole cell and cell-free systems. Especially the substances 7-12 are strong inhibitors of some atypical mycobacterial strains which are sometimes associated with tuberculosis in the elderly and with AIDS. They might be promising candidates for therapy.
通过吗啉代-苯胺法合成了在苄基部分具有亲脂性取代基的2,4-二氨基-5-苄基嘧啶1-23。通过全细胞中的MIC(最低抑菌浓度)以及全细胞和无细胞系统中的I50测量,验证了它们对各种分枝杆菌的作用。特别是化合物7-12对某些非典型分枝杆菌菌株具有很强的抑制作用,这些菌株有时与老年人的结核病以及艾滋病有关。它们可能是有前景的治疗候选药物。