Discovery and development of a small molecule library with lumazine synthase inhibitory activity

(E)-5-Nitro-6-(2-hydroxystyryl)pyrimidine-2,4(1H,3H)-dione is identified as a novel inhibitor of Schizosaccharomyces pombe lumazine synthase by using high-throughput screening of a 100000 compound library. The optimization of the enzyme inhibitory activity through the structure modification of the lead compound (E)-5-nitro-6-(2-hydroxystyryl)pyrimidine-2,4(1H,3H)-dione has led to (E)-5-nitro-6-(4-nitrostyryl)pyrimidine-2,4(1H,3H)-dione.