Synthesis of 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]-quinazolines. Inhibitors of Candida albicans dihydrofolate reductase as potential antifungal agents |
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| Authors: | Joseph H Chan David P Baccanari Robert L Tansik Christine M Boytos Sharon K Rudolph Andrew D Brown Jean S Hong Lee F Kuyper Michael L Jones |
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| Abstract: | A series of novel 1,3-diamino-7,8,9,10-tetrahydropyrido3,2-f]quinazolines were synthesized starting from 6-amino-5-cyanoquinoline (4). These compounds inhibited Candida albicans dihydrofolate reductase with Ki values of ≤0.60 aM. One analogue exhibited moderate in vivo efficacy in a C. albicans-infected mouse model. |
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