SYNTHESIS OF 4-METHYL-5-SUBSTITUTED PHENOXY- PKIMAQUINE ANALOGUES AND PRELIMINARY EVALUATION ON THEIR ANTIMAL ARIAL ACTIVITY

On basis of our previous work, seven 4-methyl-5-substituted Dhcnoxy-6-methoxy-8-(l-methyl-4-amino-butylamino)-quirtdines(Ⅱ_2～8)were synthesized and their antimalarial activities were preliminarily evaluated．The target compounds were prepared from 2-nitro-4-methoxy-5-bromo-aceXanilide as previously described．The structures 0f Ⅱ_2～8 and all of the unknow intermediates were confirmed by elementary and spectral analyses．Preliminary biological evaluation revealed that all of Ⅱ_2～8 exhibited significant blood schizontieidal activity and were 4～8 times as effective as primaquine in causal prophylactic test in mice．