| 10579848 |
Rosowsky A, Cody V, Galitsky N, Fu H, Papoulis AT, Queener SF: Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain. J Med Chem. 1999 Nov 18;42(23):4853-60.
As part of a larger search for potent as well as selective inhibitors of dihydrofolate reductase (DHFR) enzymes from opportunistic pathogens found in patients with AIDS and other immune disorders, N-[(2,4-diaminopteridin-6-yl) methyl] dibenz [b,f] azepine (4a) and the corresponding dihydrodibenz [b,f] azepine, dihydroacridine, phenoxazine, phenothiazine, carbazole, and diphenylamine analogues were synthesized from 2, 4-diamino-6-(bromomethyl) pteridine in 50-75% yield by reaction with the sodium salts of the amines in dry tetrahydrofuran at room temperature. |
33(0,1,1,3) |
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