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喹喔啉研究。23. 潜在抗疟药。制备了取代的5,8 - 二甲氧基 - 6 - [N - (ω - 二甲基氨基烷基)氨基]喹喔啉:第一系列具有相同的2,3 - 取代基H、CH3、C6H5、C6H4 - 4 - Cl和CH2C6H5;第二系列具有相同的苯乙烯基CH = CHC6H5、CH = CHC6H4 - 4 - Cl、CH = CHC6H3 - 3,4 - Cl2、CH = CHC6H4 - 4 - F、CH = CHC6H4 - 4 - CF3和CH = CHC6H4 - 4 - NO2。这些物质均无抗疟活性;有几种在最高剂量水平时有毒。

Quinoxaline studies. 23. Potential antimalarials. Substituted 5,8-dimethoxy-6-[N-(omega-dimethylaminoalkyl)amino]quinoxalines were prepared: the first series with identical 2,3-substituents H, CH3, C6H5, C6H4-4-Cl, and CH2C6H5; and the second with identical styryl groups CH=CHC6H5, CH=CHC6H4-4-Cl, CH=CHC6H3-3,4-Cl2, CH=CHC6H4-4-F, CH=CHC6H4-4-CF3, and CH=CHC6H4-4-NO2. None of the substances possessed antimalarial activity; several were toxic at highest dosage levels.

作者信息

Pifferi G, Parravicini F, Carpi C, Dorigotti L

出版信息

J Med Chem. 1975 Jul;18(7):741-6. doi: 10.1021/jm00241a020.

Abstract

3-Hydrazinopyridazines substituted in position 6 with a primary amine, secondary amine, or an alkoxy group were synthesized and screened for antihypertensive activity. In general, the 6-dialklamino derivatives are the most active; the (2-hydroxypropyl)methylamino chain provides the best combination of high antihypertensive activity and toxicity.

摘要

合成了在6位被伯胺、仲胺或烷氧基取代的3-肼基哒嗪,并对其抗高血压活性进行了筛选。一般来说,6-二烷基氨基衍生物活性最高;(2-羟丙基)甲基氨基链在高抗高血压活性和毒性之间提供了最佳组合。

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