Homoisocitrate dehydrogenase is involved in the α-aminoadipate pathway of l-lysine biosynthesis in higher fungi such as yeast and human pathogenic fungi. This enzyme catalyzes the oxidative decarboxylation of (2R, 3S)-homoisocitrate into 2-ketoadipate using NAD+ as a coenzyme. A series of aza-, oxa-, and thia-analogues of homoisocitrate was designed and synthesized as an inhibitor for homoisocitrate dehydrogenase. Among them ...