SYNTHESIS OF MINO-7,8,9,10-TETRAHYDROPYRIDO[3,2-F]-QUINAZOLINES - INHIBITORS OF CANDIDA-ALBICANS DIHYDROFOLATE-REDUCTASE AS POTENTIAL ANTIFUNGAL AGENTS
Jh. Chan et al., SYNTHESIS OF MINO-7,8,9,10-TETRAHYDROPYRIDO[3,2-F]-QUINAZOLINES - INHIBITORS OF CANDIDA-ALBICANS DIHYDROFOLATE-REDUCTASE AS POTENTIAL ANTIFUNGAL AGENTS, Journal of heterocyclic chemistry, 34(1), 1997, pp. 145-151
A series of novel amino-7,8,9,10-tetrahydropyrido[3,2-f]quinazolines w
ere synthesized starting from 6-amino-5-cyanoquinoline (4). These comp
ounds inhibited Candida albicans dihydrofolate reductase with K-i valu
es of less than or equal to 0.60 nM. One analogue exhibited moderate i
n vivo efficacy in a C. albicans-infected mouse model.