In vitro and in vivo antimalarial activity of amphiphilic naphthothiazolium salts with amine-bearing side chains

UlrichP.; GipsonG.R.; ClarkM.A.; TripathiA.; SullivanD.J.; CeramiC.

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In vitro and in vivo antimalarial activity of amphiphilic naphthothiazolium salts with amine-bearing side chains

机译：带有胺侧链的两亲性萘噻唑鎓盐的体外和体内抗疟活性

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Because of emerging resistance to existing drugs, new chemical classes of antimalarial drugs are urgently needed. We have rationally designed a library of compounds that were predicted to accumulate in the digestive vacuole and then decrystallize hemozoin by breaking the iron carboxylate bond in hemozoin. We report the synthesis of 16 naphthothiazolium salts with amine-bearing side chains and their activities against the erythrocytic stage of Plasmodium falciparum in vitro. KSWI-855, the compound with the highest efficacy against the asexual stages of P. falciparum in vitro, also had in vitro activity against P. falciparum gametocytes and in vivo activity against P. berghei in a murinemalaria model.

机译：由于对现有药物的抵抗力不断增强，因此迫切需要新的化学类别的抗疟药。我们合理地设计了一个化合物库，这些化合物预计会在消化液中积累，然后通过破坏血红素中的羧酸铁键使血红素结晶。我们报告了16带有胺基侧链的萘噻唑鎓盐的合成及其在体外对恶性疟原虫红细胞阶段的活性。 KSWI-855是在体外对恶性疟原虫无性阶段具有最高功效的化合物，在鼠类疟疾模型中，其还具有对恶性疟原虫配子细胞的体外活性和对伯氏疟原虫的体内活性。

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《The American Journal of Tropical Medicine and Hygiene》 |2014年第4期|共9页
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UlrichP.; GipsonG.R.; ClarkM.A.; TripathiA.; SullivanD.J.; CeramiC.;
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1. In vitro and in vivo antimalarial activity of amphiphilic naphthothiazolium salts with amine-bearing side chains [J] . UlrichP., GipsonG.R., ClarkM.A., The American Journal of Tropical Medicine and Hygiene . 2014,第4期

机译：带有胺侧链的两亲性萘噻唑鎓盐的体外和体内抗疟活性
2. Synthesis and in vitro antimalarial testing of neocryptolepines: SAR study for improved activity by introduction and modifications of side chains at C2 and C11 on indolo[2,3-b]quinolines [J] . Mei Z.-W., Wang L., Lu W.-J., Journal of Medicinal Chemistry . 2013,第4期

机译：新隐油菜碱的合成和体外抗疟测试：通过吲哚[2,3-b]喹啉在C2和C11侧链的引入和修饰来提高活性的SAR研究
3. Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin [J] . Peri? M., Fajdeti? A., Rup?i? R., Journal of Medicinal Chemistry . 2012,第3期

机译：9a-N取代的15元氮杂内酯类药物的抗疟疾活性比阿奇霉素具有更高的体内和体外活性
4. Subcellular localization and photodynamic activity of Photodithazine (glucosamine salt of chlorin e6) in murine melanoma B16-F10: an in vitro and in vivo study [C] . Bruno Andrade Ono, Layla Pires, Marcelo Saito Nogueira, Conference on optical methods for tumor treatment and detection: mechanisms and techniques in photodynamic therapy . 2018

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5. Antimalarial properties of rabbit tumour necrosis serum: "in vitro" and "in vivo" studies [D] . Rockett, Kirk Allan. 1990

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6. In vitro and In vivo Antimalarial Activity of Amphiphilic Naphthothiazolium Salts with Amine-Bearing Side Chains [O] . Peter Ulrich, Gregory R. Gipson, Martha A. Clark, 2014

机译：带有胺侧链的两亲性萘噻唑盐的体外和体内抗疟活性
7. P200 Development of new antimalarial drugs : in vitro and in vivo antimalarial activity of endoperoxides [O] . Kanako ONO, Naoki OGURA, HyeSook KIM, 2001

机译：新型抗疟药的P200开发：体外和体内抗疟疾活性的内透铁氧化物
8. Comparison of In vitro and In vivo Antimalarial Activities of 9-Phenanthrenecarbinols [R] . Childs, G. E., Lambros, C., Notsch, J. D., 1984

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In vitro and in vivo antimalarial activity of amphiphilic naphthothiazolium salts with amine-bearing side chains

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