磷鎓脂质体作为抗寄生虫药物。
Phosphonium lipocations as antiparasitic agents.
机构信息
Department of Pharmaceutical and Biomedical Sciences and Center for Drug Discovery, University of Georgia, Athens, GA 30602, USA.
出版信息
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2976-9. doi: 10.1016/j.bmcl.2012.02.045. Epub 2012 Feb 23.
Abstract
Phosphonium lipocations were synthesized and evaluated for inhibition of the development of Plasmodium falciparum and Trypanosoma cruzi, etiological agents of malaria and Chagas disease, respectively. Optimal phthalimides and 1,4-naphthoquinone-based lipocations were active in vitro at mid-high nM concentrations against P. falciparum and low μM concentrations against T. cruzi.
摘要
磷鎓脂质体被合成并进行了评估，以抑制疟原虫和克氏锥虫的发育，分别为疟疾和恰加斯病的病原体。最佳的邻苯二甲酰亚胺和 1,4-萘醌基脂质体在体外以中高 nM 浓度对疟原虫具有活性，以低 μM 浓度对克氏锥虫具有活性。
相似文献
1
Phosphonium lipocations as antiparasitic agents.磷鎓脂质体作为抗寄生虫药物。
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2976-9. doi: 10.1016/j.bmcl.2012.02.045. Epub 2012 Feb 23.
2
Dual Parasiticidal Activities of Phthalimides: Synthesis and Biological Profile against Trypanosoma cruzi and Plasmodium falciparum.邻苯二甲酰亚胺类化合物的双重抗寄生虫活性：合成及抗南美锥虫和恶性疟原虫的生物学特性。
ChemMedChem. 2020 Nov 18;15(22):2164-2175. doi: 10.1002/cmdc.202000331. Epub 2020 Oct 19.
3
A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts.一种源自化学工程提取物的具有生物活性的克氏锥虫溴结构域抑制剂。
ACS Comb Sci. 2018 Apr 9;20(4):220-228. doi: 10.1021/acscombsci.7b00172. Epub 2018 Mar 2.
4
Isolation, Derivative Synthesis, and Structure-Activity Relationships of Antiparasitic Bromopyrrole Alkaloids from the Marine Sponge Tedania brasiliensis.从海洋海绵 Tedania brasiliensis 中分离、衍生合成及抗寄生虫溴代吡咯生物碱的结构-活性关系研究。
J Nat Prod. 2018 Jan 26;81(1):188-202. doi: 10.1021/acs.jnatprod.7b00876. Epub 2018 Jan 3.
5
Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi.进一步研究硒代 WC-9 类似物对克氏锥虫的作用。
Bioorg Med Chem. 2019 Apr 1;27(7):1350-1361. doi: 10.1016/j.bmc.2019.02.039. Epub 2019 Feb 19.
6
In vitro and in silico studies of polycondensed diazine systems as anti-parasitic agents.聚缩二嗪系统作为抗寄生虫药物的体外和计算研究。
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1000-4. doi: 10.1016/j.bmcl.2011.12.004. Epub 2011 Dec 8.
7
Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4.来自昆虫病原 Xenorhabdus sp. PB61.4 的驱虫查亚菲米。
J Nat Prod. 2014 Apr 25;77(4):779-83. doi: 10.1021/np4007525. Epub 2014 Mar 27.
8
Antiparasitic effect of a fraction enriched in tight-binding protease inhibitors isolated from the Caribbean coral Plexaura homomalla.从加勒比海珊瑚 Plexaura homomalla 中分离得到的紧密结合蛋白酶抑制剂富集部分的抗寄生虫作用。
Exp Parasitol. 2013 Nov;135(3):611-22. doi: 10.1016/j.exppara.2013.09.013. Epub 2013 Sep 30.
9
Drug Discovery for Paediatric Chagas Disease.儿科恰加斯病的药物发现。
Mini Rev Med Chem. 2018;18(9):776-780. doi: 10.2174/1389557516666161226155204.
10
2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase.2- 烷氨基乙基-1,1-双膦酸是克氏锥虫鲨烯合酶酶活性的有效抑制剂。
Antimicrob Agents Chemother. 2012 Aug;56(8):4483-6. doi: 10.1128/AAC.00796-12. Epub 2012 May 14.
引用本文的文献
1
Repurposing of MitoTam: Novel Anti-Cancer Drug Candidate Exhibits Potent Activity against Major Protozoan and Fungal Pathogens.米托坦再利用：新型抗癌候选药物对主要原生动物和真菌病原体表现出强大的活性。
Antimicrob Agents Chemother. 2022 Aug 16;66(8):e0072722. doi: 10.1128/aac.00727-22. Epub 2022 Jul 20.
2
Menadione: a platform and a target to valuable compounds synthesis.甲萘醌：一种用于合成有价值化合物的平台和目标。
Beilstein J Org Chem. 2022 Apr 11;18:381-419. doi: 10.3762/bjoc.18.43. eCollection 2022.
3
Phthalimide analogs for antimalarial drug discovery.用于抗疟药物研发的邻苯二甲酰亚胺类似物。
RSC Med Chem. 2021 Aug 13;12(11):1854-1867. doi: 10.1039/d1md00244a. eCollection 2021 Nov 17.
4
Trialkyl(vinyl)phosphonium Chlorophenol Derivatives as Potent Mitochondrial Uncouplers and Antibacterial Agents.三烷基（乙烯基）鏻氯酚衍生物作为强效线粒体解偶联剂和抗菌剂。
ACS Omega. 2021 Jul 29;6(31):20676-20685. doi: 10.1021/acsomega.1c02909. eCollection 2021 Aug 10.
5
Indolylalkyltriphenylphosphonium Analogues Are Membrane-Depolarizing Mycobactericidal Agents.吲哚烷基三苯基鏻类似物是使细胞膜去极化的杀分枝杆菌剂。
ACS Med Chem Lett. 2017 Oct 9;8(11):1165-1170. doi: 10.1021/acsmedchemlett.7b00287. eCollection 2017 Nov 9.
6
Caged Garcinia Xanthones, a Novel Chemical Scaffold with Potent Antimalarial Activity.笼形藤黄属氧杂蒽酮，一种具有强效抗疟活性的新型化学骨架。
Antimicrob Agents Chemother. 2016 Dec 27;61(1). doi: 10.1128/AAC.01220-16. Print 2017 Jan.
7
1,4-naphthoquinone cations as antiplasmodial agents: hydroxy-, acyloxy-, and alkoxy-substituted analogues.1,4-萘醌阳离子作为抗疟药：羟基、酰氧基和烷氧基取代类似物
ACS Med Chem Lett. 2012 Oct 1;3(12):1029-33. doi: 10.1021/ml300242v. eCollection 2012 Dec 13.
本文引用的文献
1
Mitochondria and trypanosomatids: targets and drugs.线粒体与利什曼原虫：靶点与药物。
Pharm Res. 2011 Nov;28(11):2758-70. doi: 10.1007/s11095-011-0586-3. Epub 2011 Sep 21.
2
Drug-resistant malaria: molecular mechanisms and implications for public health.抗药性疟疾：分子机制及其对公共卫生的影响。
FEBS Lett. 2011 Jun 6;585(11):1551-62. doi: 10.1016/j.febslet.2011.04.042. Epub 2011 Apr 23.
3
Preclinical evaluation of novel triphenylphosphonium salts with broad-spectrum activity.新型具有广谱活性的三苯基膦盐的临床前评价。
PLoS One. 2010 Oct 4;5(10):e13131. doi: 10.1371/journal.pone.0013131.
4
Risedronate metal complexes potentially active against Chagas disease.利塞膦酸盐金属配合物可能对恰加斯病有效。
J Inorg Biochem. 2010 Dec;104(12):1252-8. doi: 10.1016/j.jinorgbio.2010.08.004. Epub 2010 Aug 14.
5
Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series.疟原虫蛋白酶抑制剂：2-嘧啶甲腈先导系列的优化研究。
J Med Chem. 2010 Aug 26;53(16):6129-52. doi: 10.1021/jm100556b.
6
Animal and human studies with the mitochondria-targeted antioxidant MitoQ.动物和人体研究使用靶向线粒体的抗氧化剂 MitoQ。
Ann N Y Acad Sci. 2010 Jul;1201:96-103. doi: 10.1111/j.1749-6632.2010.05627.x.
7
Chagas disease.恰加斯病。
Lancet. 2010 Apr 17;375(9723):1388-402. doi: 10.1016/S0140-6736(10)60061-X.
8
Mitochondria as a target in treatment.线粒体作为治疗靶点。
Environ Mol Mutagen. 2010 Jun;51(5):462-75. doi: 10.1002/em.20554.
9
Inhibitors of the mitochondrial electron transport chain and de novo pyrimidine biosynthesis as antimalarials: The present status.线粒体电子传递链抑制剂和从头嘧啶生物合成作为抗疟药：现状。
Curr Med Chem. 2010;17(10):929-56. doi: 10.2174/092986710790820660.
10
New benzophenone-derived bisphosphonium salts as leishmanicidal leads targeting mitochondria through inhibition of respiratory complex II.新型苯甲酮衍生双膦盐类化合物作为通过抑制呼吸复合物 II 靶向线粒体的抗利什曼原虫先导化合物。
J Med Chem. 2010 Feb 25;53(4):1788-98. doi: 10.1021/jm901677h.
Zotero 插件