SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 2,4-DIAMINO-5-FLUORO-6-SUBSTITUTED BENZYLAMINO QUINAZOLINES

The title compounds were synthesized by condensation of 5-fluoro- 2,4,6-triaminoquinazoline(6a) with various substituted benzaldehydes to produce the corresponding Schiffbases,followed by reduction.11 and III were obtained by formylation and nitrosation of I,respectively,IV were obtained by reduction of II. Primary screening for suppressive therapeutic effects against P. berghei mice showed that six ofthe twenty-two compounds produced 100%suppression when administered orally at dose of lmg·kg^-1.All compounds exhibited potent activity against L₁₂₁₀ cell in uitro. Among themI₄ wasmore active than MTX. A number of compounds showed moderate activities against Diplococcus pneumoniae in in vitro tests.