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本文报道2,4-二氨基-6-取代哌哗嗪基喹唑啉衍生物的合成及其抗疟活性。这类化合物的合成是以间氯苯甲腈为原料,经硝化与哌哔嗪缩合,还原制得2-氨基-5-(哌哔嗪-1′)苯甲腈,再与各种卤代物反应,然后与二氰二胺环合;也可以2-硝基5-氯苯甲腈与取代的哌哔嗪缩合,经还原,然后与二氰二胺环合而得。经鼠疟抑制性治疗初筛,有4个化合物(X_(1,2,3,8)有效;经鼠疟病因性预防初筛,有3个化合物(X_(1,8,10)有效;经蚊模抑制孢子增殖初筛,当浓度0.01％时,有2个化合物(X_(8,9))使70％蚊虫的孢子增殖受到抑制。
This paper reports the synthesis of 2,4-diamino-6-substituted piperazinoquinazoline derivatives and their antimalarial activity. The synthesis of these compounds is based on m-chloronitrobenzene as raw material, nitration and piperazine condensation, reduction obtained 2-amino-5- (piperazine-1 ’) benzonitrile, and then with a variety of halogenated compounds The reaction, and then dicyandiamide ring; also 2-nitro-5-chlorobenzonitrile condensation with the substituted piperazine, after reduction, and then dicyandiamide derived. Four compounds (X_ (1, 2, 3, 8)) were validated by the inhibitory treatment of murine malaria. Three compounds (X_ (1,8,10) The mosquito mold inhibition of spore proliferation screening, when the concentration of 0.01%, two compounds (X_ (8,9)) so that 70% of the mosquito spores proliferation was inhibited.