[Synthesis and antimycobacterial action of lipophilic substituted 2,4-diamino-5-benzylpyrimidines].
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.
Hachtel
G
G
Pharmazeutisches Institut der Christian-Albrechts-Universität, Kiel.
Haller
R
R
Seydel
J K
JK
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D002627:Chemistry, Physical; D005493:Folic Acid Antagonists; D066298:In Vitro Techniques; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D009249:NADP / Q000378:metabolism; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D005493:Folic Acid Antagonists; D011725:Pyridines; D009249:NADP
Synthese und antimykobakterielle Wirkung einiger lipophil substituierter 2,4-Diamino-5-benzylpyrimidine.