Activity of Selected 2,4-Diaminoquinazolines against Candida albicans in Vitro 1

Abstract

Summary

A series of nine 2,4-diamino-quinazolines bearing a variety of substitu-ents at positions 5 and 6 was evaluated against three human isolates of Candida albicans in vitro. An established drug, 5-fluo-rocytosine, was chosen as a standard of comparison and each isolate was found to be sensitive to this agent. The two most active compounds, 6-(3,4-dichlorophenylacetam-ido)-2,4-diaminoquinazoline and 6-(3,4-dichlorobenzamido)-2,4-diaminoquinazo-line, were selected for acute toxicity studies in mice. At the highest dose tested (250 mg/ kg) the latter compound showed evidence of toxicity while both compounds were substantially free of untoward effects at lower doses.