Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials.

Gravestock D; Rousseau AL; Lourens AC; Moleele SS; van Zyl RL; Steenkamp PA

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Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials.

机译：新型2，N6-二取代的1,2-二氢-1,3,5-三嗪-4,6-二胺作为潜在的抗疟疾药物的快速合成和生物学评估。

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A small set of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines was prepared possessing a flexible tether between the exocyclic nitrogen bonded to C-6 of the 1,2-dihydro-1,3,5-triazine-4,6-diamine heterocycle and the distal aryl ring. Three zones were varied in this series of compounds, namely the nature of the substituent(s) on C-2; the nature of the substituent(s) on the distal aryl ring; as well as the nature and length of the flexible tether between the rings. The compound showing the best antimalarial activity (cycloguanil-resistant FCR-3 Plasmodium falciparum IC50=0.99 muM) was N6-(3-(4-chlorophenoxy)propyl)-2-(furan-2-yl)-1,2-dihydro-1,3,5-triazine-4,6-diam ine hydrochloride.

机译：制备了少量新的2，N6-二取代的1,2-二氢-1,3,5-三嗪-4,6-二胺，在键合于1,2-的C-6的环外氮之间具有柔性系链二氢-1,3,5-三嗪-4,6-二胺杂环和远端芳基环。在这一系列化合物中，三个区域是不同的，即C-2上取代基的性质;远端芳基环上取代基的性质;以及环之间的柔性系绳的性质和长度。表现出最佳抗疟活性的化合物（耐环鸟嘌呤FCR-3恶性疟原虫IC50 = 0.99μM）为N6-（3-（4-氯苯氧基）丙基）-2-（呋喃-2-基）-1,2-二氢-1,3,5-三嗪-4,6-二胺盐酸盐。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第6期|共9页
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Gravestock D; Rousseau AL; Lourens AC; Moleele SS; van Zyl RL; Steenkamp PA;
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中图分类药学;
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机译：新型2，N6-二取代的1,2-二氢-1,3,5-三嗪-4,6-二胺作为潜在的抗疟疾药物的快速合成和生物学评估。
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9. Synthesis of C-Nucleosides Related to Adenosine as Potential Antimalarials. [R] . Davis, G. D. 1974

机译：作为潜在抗疟药的腺苷相关C-核苷的合成。

Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials.

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