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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antileishmanial activity of 6-mono-substituted and 3,6-di-substituted acridines obtained by acylation of proflavine.
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Synthesis and antileishmanial activity of 6-mono-substituted and 3,6-di-substituted acridines obtained by acylation of proflavine.

机译：通过原黄酮的酰化获得的6-单-取代的和3,6-二-取代的cr啶的合成和抗衰老活性。

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摘要

Two new series of diaminoacridinic derivatives obtained from proflavine and N-(6-amino-3-acridinyl)acetamide were synthesised and assessed for their cytotoxic and antileishmanial activities. Two compounds, N-[6-(acetylamino)-3-acridinyl]acetamide and N-[6-(benzoylamino)-3-acridinyl]benzamide demonstrated highly specific antileishmanial properties against the intracellular amastigote form of the parasite. Structure-activity relationships established that the antiproliferative activity against human cells was greatly enhanced by the presence of a benzoylamino group in 6-mono-substituted acridines, while the presence of two acetylamino or benzoylamino groups in 3,6-di-substituted acridines strongly increased the specificity of the molecules for Leishmania parasite, suggesting that symmetric conformations could preferentially interfere with Leishmania metabolism.
机译：合成了两个新系列的从牛黄素和N-（6-氨基-3-rid啶基）乙酰胺获得的二氨基ac啶衍生物，并评估了它们的细胞毒作用和抗菌活性。 N- [6-（乙酰氨基）-3-ac啶基]乙酰胺和N- [6-（苯甲酰基氨基）-3-ac啶基]苯甲酰胺这两种化合物对寄生虫的胞内a节肢动物形式表现出高度特异性的抗螨虫特性。构效关系确定了6-单取代-啶中苯甲酰氨基的存在大大增强了对人体细胞的抗增殖活性，而3,6-二取代a啶中两个乙酰氨基或苯甲酰氨基的存在则大大增加分子对利什曼原虫寄生虫的特异性，表明对称构象可优先干扰利什曼原虫的代谢。

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