A series of novel 1,3‐diamino‐7,8,9,10‐tetrahydropyrido[3,2‐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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Chan et al. (1997) studied this question.
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