In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.

Yapi AD; Valentin A; Chezal JM; Chavignon O; Chaillot B; Gerhardt R; Teulade JC; Blache Y

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In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.

机译：1,10-菲咯啉骨架衍生物的体外和体内抗疟活性。

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A series of trisubstituted 1,10-phenanthrolines was prepared. These compounds exhibited mild to high biological activities in vitro both toward chloroquino-resistant FcB1-Columbia and FcM29-Cameron strains and Nigerian chloroquino-sensitive strain of Plasmodium falciparum. Cytotoxicity of the most active compounds was estimated showing that one compound (10) exhibited a selective activity against malaria parasite (selectivity indexes of 52 and 144). Antiplasmodial activity of this derivative was optimized by N-10 alkylation and the phenanthrolinium salt (15) submitted to an in vivo study using mice infected by P. vinckei petteri showing an ED50 of 7.86 mg/kg/day.

机译：制备了一系列三取代的1，10-菲咯啉。这些化合物在体外对耐氯喹诺酮的FcB1-Columbia和FcM29-Cameron菌株以及尼日利亚对氯喹诺酮敏感的恶性疟原虫均具有中等至高的生物学活性。估计最具活性的化合物的细胞毒性表明一种化合物（10）对疟原虫具有选择性活性（选择性指数分别为52和144）。该衍生物的抗血浆活性通过N-10烷基化进行了优化，菲咯啉盐（15）进行了体内研究，研究对象是感染了温氏小孢子菌的小鼠，ED50为7.86 mg / kg /天。

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《Archiv der Pharmazie》 |2006年第4期|共6页
作者
Yapi AD; Valentin A; Chezal JM; Chavignon O; Chaillot B; Gerhardt R; Teulade JC; Blache Y;
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正文语种 eng
中图分类药学;
关键词
Antimalarials; Phenanthrolines; Plasmodium falciparum; 抗疟药; 菲绕啉类; 疟原虫; 恶性;

机译：Antimalarials;Phenanthrolines;Plasmodium falciparum;抗疟药;菲绕啉类;疟原虫;恶性;

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1. In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework. [J] . Yapi AD, Valentin A, Chezal JM, Archiv der Pharmazie . 2006,第4期

机译：1,10-菲咯啉骨架衍生物的体外和体内抗疟活性。
2. Self-assembly of novel molecular complexes of 1,10-phenanthroline and 5-amino-1,10-phenanthroline and evaluation of their in vitro antitumour activity. [J] . Kaloyanov N, Alexandrova R, Wesselinova DW, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第6期

机译：1,10-菲咯啉和5-氨基-1,10-菲咯啉新型分子复合物的自组装及其体外抗肿瘤活性的评价。
3. Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework. [J] . Sall C, Yapi AD, Desbois N, Bioorganic and Medicinal Chemistry Letters . 2008,第16期

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4. ELECTROCHEMICAL DNA SENSORS BASED ON POLYMERIC INDICATOR: USE OF A POLY(4-VINYLPYRIDINE) DERIVATIVE BEARING Os(5,6-5,6-dimethyl-1,10-phenanthroline)_2Cl~(2+) [C] . Aihua Liu, Jun-ichi Anzai Proceedings vol.2004-08; International Symposium on Chemical Sensors VI: Chemical and Biological Sensors and Analytical Systems and Joint International Meeting of the Electrochemical Society(ECS) and Electrochemical Society of Japan; 20041003-08; Honolul . 2004

机译：基于聚合物指示剂的电化学DNA传感器：使用聚（4-乙烯基吡啶）衍生物轴承Os（5,6-5,6-二甲基-1,10-菲咯啉）_2Cl〜（2+）
5. Preparation of 1,10-phenanthroline derivatives with B-ring functionalization and their application. [D] . Kohler, Lars. 2011

机译：具有B环功能化的1,10-菲咯啉衍生物的制备及其应用。
6. Synthesis and antiplasmodial activity of novel phenanthroline derivatives: An in vivo study [O] . Azar Tahghighi, Safoura Karimi, Arezoo Rafie Parhizgar, 2018

机译：新型菲咯啉衍生物的合成及其抗血浆活性：体内研究
7. In vitro and in vivo studies into the biological activities of\ud 1,10-phenanthroline, 1,10-phenanthroline-5,6-dione and its copper(II)\ud and silver(I) complexes [O] . McCann, Malachy, Santos, Andre L. S., Da Silva, Bianca A., 2012

机译：体外和体内研究\ ud生物活性 1,10-菲咯啉，1,10-菲咯啉-5,6-二酮及其铜（II）\ ud 和银（I）络合物
8. Comparison of In vitro and In vivo Antimalarial Activities of 9-Phenanthrenecarbinols [R] . Childs, G. E., Lambros, C., Notsch, J. D., 1984

机译：9-菲炔醇的体外和体内抗疟活性的比较

In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.

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