ChemInform Abstract: New Chemotherapeutically Active 4-Trifluoromethylpyrimidines.

Antimykotische Wirkstoffe, 20. Mitt.: Bioisostere 6-Arylpyrimidin-Derivate

Durch Kondensation von N-(2-Hydroxyethyl)-N-methylguanidinsulfat (1) mit den 1-Aryl-substituierten β-Diketonen 4a-e erhalt man die bioisosteren 2-[(2-Hydroxyethyl)-methylamino]-6-arylpyrimidine 5a-e. Die Verbindungen 5a-c besitzen signifikante antimykotische in vitro- und in vivo-Aktivitaten. Antimycotic Agents, XX Bioisosteric 6-Arylpyrimidine Derivatives Condensation of N-(2-hydroxyethyl)-N-methylguanidine-sulfate (1) with the β-diketones 4a-e bearing 1-aryl substituents leads to the bioisosteric 2-[(2-hydroxyethyl)-methylamino]-6-arylpyrimidines 5a-e. Compounds 5a-c exhibit significant antimycotic in vivo and in vitro activities.

Neue chemotherapeutisch-aktive 4-trifluormethylpyrimidine

Abstract Condensation of N -(2-hydroxyethyl)- N -methylguanidine sulfate with various β-diketonesbearing 1,1,1-trifluoromethyl substituents leads to 2-[ N -(2-hydroxyethyl)-methylamino]-4-trifluoromethylpyrimidine derivatives. These compounds exhibit antimycotic, trichomonazide and anti-HIV properties.