• Archives of Pharmacal Research
• /
• 제13권1호
• /
• pp.78-81
• /
• 1990

N-Aryl-N'(4-hydroxy-6-methyl-2-pyrimidinyl)guanidines (IIa-c) were prepared by cyclization of N-arybiguanides (Ia-c) with ethyl acetoacetate. Coupling of compounds (IIa-c) with the appropriate diazotized arylamine gave N-aryl-N'-(5-arylhydrazono-6-methyl-4-oxopyrimidin-2-yl) guanidines (IIIa-f). Whereas, their chlorination with phosphorus oxychloride followed by treatment of N-aryl-N'-(4-Chloro-6-methyl-2-pyrimidinyl)guanidimes (IVac) with the appropriate arylamine afforded the corresponding 4-arylamino derivatives (Vaf). Compounds (IIa-f) were also formed when compounds (1a-c) were treated with ethyl 2-arylhydrazono-3-oxobutyrates. The antimircobial testing of some of the prepared compounds against some pathogenic microorganisms revealed that only two have a marked effect against Escherichia coli.