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疟疾防治药物的研究——Ⅵ.2,4-二氨基-6-取代氨基-磺酰基喹唑啉衍生物的合成及其抗疟作用
引用本文:张秀平,沈德福,张秀菊,陈林,戴祖瑞,舒康全. 疟疾防治药物的研究——Ⅵ.2,4-二氨基-6-取代氨基-磺酰基喹唑啉衍生物的合成及其抗疟作用[J]. 药学学报, 1981, 16(11): 877-880
作者姓名:张秀平  沈德福  张秀菊  陈林  戴祖瑞  舒康全
作者单位:上海医药工业研究院,上海医药工业研究院,上海医药工业研究院,第二军医大学,第二军医大学,第二军医大学 上海,上海,上海
摘    要:磺胺是对氨基苯甲酸拮抗剂,有较强的广谱抗菌作用,细菌代谢与疟原虫代谢有许多相似之处,早在1937年Hill等就用百浪多息(Prontosil,Ⅰ)治疗疟疾病人,以后发现多种磺胺可以抑制疟原虫的生长与繁殖。2,4-二氨基-6-取代氨基喹唑啉衍生物(Ⅱ)对伯氏鼠疟原

收稿时间:1980-12-17

STUDIES ON ANTIMALARIALS Ⅵ. SYNTHESIS AND ANTIMALARIAL ACTIVITIES OF SOME 2,4-DIAMINO-6-SUBSTITUTED AMINO SULFONYL QUINAZOLINE DERIVATIVES
Zhang Xiuping,Shen Defu and Zhang Xiuju Chen Lin,Dai Zurui and Shu Kangquan. STUDIES ON ANTIMALARIALS Ⅵ. SYNTHESIS AND ANTIMALARIAL ACTIVITIES OF SOME 2,4-DIAMINO-6-SUBSTITUTED AMINO SULFONYL QUINAZOLINE DERIVATIVES[J]. Acta pharmaceutica Sinica, 1981, 16(11): 877-880
Authors:Zhang Xiuping  Shen Defu  Zhang Xiuju Chen Lin  Dai Zurui  Shu Kangquan
Abstract:In the present communication sixteen derivatives of 2, 4-diamino-6-substitutedaminosulfonylquinazolines were synthesized as potential antimalarial agents.Screening tests for therapeutic effect on mice infected with Plasmodium berghei and for prophylactic effect on mice infected with P. yoelii sporozoites,.showed that 2,4-diamino-6-(piperidyl-1) sulfonyl quinazoline acetate (Ⅲ) at daily oral dose of 0.31 mg/kg for 3 consecutive days possess pronounced causal prophylactic activity against P. yoelii.
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