Abstract
Structural requirements for melanin biosynthesis inhibition were analysed by comparing known melanin biosynthesis inhibitors (MBIs) and an intermediate of melanin biosynthesis (1,3,8-trihydroxynaphthalene (1,3,8-THN)), on the assumption that the enzymatic inhibition by MBIs occurs competitively with the biosynthetic intermediate. On this basis, new chemicals in the form of phthalazine derivatives were designed. In biological tests, the synthesised phthalazine derivatives showed high activity against rice blast, caused by Pyricularia oryzae Cav. These compounds also inhibited the melanisation of this fungus at a low concentration, which suggested that they are similar to other MBIs in their mode of action.
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