新型芳香脒类化合物抗克氏锥虫的分析。
, , and Analyses of Novel Aromatic Amidines against Trypanosoma cruzi.
机构信息
Laboratory of Cellular Biology (LBC), Oswaldo Cruz Institute (Fiocruz), Rio de Janeiro, RJ, Brazil.
Laboratory of Structural Biology (LBE), Oswaldo Cruz Institute (Fiocruz), Rio de Janeiro, RJ, Brazil.
出版信息
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.02205-17. Print 2018 Feb.
Abstract
Five bis-arylimidamides were assayed as anti- agents by , , and approaches. None were considered to be pan-assay interference compounds. They had a favorable pharmacokinetic landscape and were active against trypomastigotes and intracellular forms, and in combination with benznidazole, they gave no interaction. The most selective agent (28SMB032) tested led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. target fishing suggested DNA as the main target, but ultrastructural data did not match.
摘要
五种双芳基脒类化合物通过,, 和 方法被评估为抗 药物。没有一种被认为是泛分析干扰化合物。它们具有良好的药代动力学特征，对滋养体和内体形式均有效，并且与苯并咪唑联合使用时没有相互作用。测试的最具选择性的化合物（28SMB032）导致寄生虫血症减少 40%（0.1 毫克/千克体重/5 天腹腔内注射），但没有保护死亡率。 靶点捕捞表明 DNA 是主要靶点，但超微结构数据不匹配。
相似文献
1
, , and Analyses of Novel Aromatic Amidines against Trypanosoma cruzi.
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.02205-17. Print 2018 Feb.
2
In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.
Antimicrob Agents Chemother. 2016 Mar 25;60(4):2425-34. doi: 10.1128/AAC.01667-15. Print 2016 Apr.
3
In vitro and in vivo studies of the biological activity of novel arylimidamides against Trypanosoma cruzi.
Antimicrob Agents Chemother. 2014 Jul;58(7):4191-5. doi: 10.1128/AAC.01403-13. Epub 2014 Mar 3.
4
Phenotypic evaluation and in silico ADMET properties of novel arylimidamides in acute mouse models of infection.
Drug Des Devel Ther. 2017 Apr 3;11:1095-1105. doi: 10.2147/DDDT.S120618. eCollection 2017.
5
In vitro and in vivo biological effects of novel arylimidamide derivatives against Trypanosoma cruzi.
Antimicrob Agents Chemother. 2014 Jul;58(7):3720-6. doi: 10.1128/AAC.02353-14. Epub 2014 Apr 21.
6
In vitro investigation of the efficacy of novel diamidines against Trypanosoma cruzi.
Parasitology. 2014 Sep;141(10):1272-6. doi: 10.1017/S0031182014000407. Epub 2014 Apr 15.
7
Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi.
Exp Parasitol. 2011 Feb;127(2):429-35. doi: 10.1016/j.exppara.2010.10.010. Epub 2010 Nov 11.
8
Experimental models in Chagas disease: a review of the methodologies applied for screening compounds against Trypanosoma cruzi.
Parasitol Res. 2018 Nov;117(11):3367-3380. doi: 10.1007/s00436-018-6084-3. Epub 2018 Sep 19.
9
Repurposing Strategy of Atorvastatin against Trypanosoma cruzi: Monotherapy and Combined Therapy with Benznidazole Exhibit Synergistic Trypanocidal Activity.
Antimicrob Agents Chemother. 2018 Aug 27;62(9). doi: 10.1128/AAC.00979-18. Print 2018 Sep.
10
The efficacy of novel arylimidamides against Trypanosoma cruzi in vitro.
Parasitology. 2011 Dec;138(14):1863-9. doi: 10.1017/S0031182011001429. Epub 2011 Sep 9.
引用本文的文献
1
Phenotypic investigation of 4-nitrophenylacetyl- and 4-nitro-1-imidazoyl-based compounds as antileishmanial agents.
Parasitology. 2022 Apr;149(4):490-495. doi: 10.1017/S0031182021002079. Epub 2022 Feb 3.
2
Differentiating Trypanosoma cruzi in a Host Mammalian Cell Imaged in Aqueous Liquid by Atmospheric Scanning Electron Microscopy.
Microbiol Spectr. 2022 Feb 23;10(1):e0141321. doi: 10.1128/spectrum.01413-21. Epub 2022 Jan 5.
3
7-Aryl-7-deazapurine 3'-deoxyribonucleoside derivative as a novel lead for Chagas' disease therapy: and pharmacology.
JAC Antimicrob Resist. 2021 Nov 17;3(4):dlab168. doi: 10.1093/jacamr/dlab168. eCollection 2021 Dec.
4
Review on Experimental Treatment Strategies Against .
J Exp Pharmacol. 2021 Mar 31;13:409-432. doi: 10.2147/JEP.S267378. eCollection 2021.
5
Drug screening using shape-based virtual screening and experimental models of cutaneous Leishmaniasis.
Parasitology. 2021 Jan;148(1):98-104. doi: 10.1017/S0031182020001900. Epub 2020 Oct 7.
6
and Evaluation of an Adamantyl-Based Phenyl Sulfonyl Acetamide against Cutaneous Leishmaniasis Models of .
Antimicrob Agents Chemother. 2020 Nov 17;64(12). doi: 10.1128/AAC.01188-20.
7
Imidazole Derivatives as Promising Agents for the Treatment of Chagas Disease.
Antimicrob Agents Chemother. 2019 Mar 27;63(4). doi: 10.1128/AAC.02156-18. Print 2019 Apr.
本文引用的文献
1
Assessing anti-T. cruzi candidates in vitro for sterile cidality.
Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):165-170. doi: 10.1016/j.ijpddr.2016.08.003. Epub 2016 Aug 26.
2
Pred-hERG: A Novel web-Accessible Computational Tool for Predicting Cardiac Toxicity.
Mol Inform. 2015 Oct;34(10):698-701. doi: 10.1002/minf.201500040. Epub 2015 Jul 20.
3
The BENEFIT Trial: Where Do We Go from Here?
PLoS Negl Trop Dis. 2016 Feb 25;10(2):e0004343. doi: 10.1371/journal.pntd.0004343. eCollection 2016 Feb.
4
Hit and lead criteria in drug discovery for infectious diseases of the developing world.
Nat Rev Drug Discov. 2015 Nov;14(11):751-8. doi: 10.1038/nrd4683. Epub 2015 Oct 5.
5
The use of posaconazole against Chagas disease.
Curr Opin Infect Dis. 2015 Oct;28(5):397-407. doi: 10.1097/QCO.0000000000000192.
6
Recent clinical trials for the etiological treatment of chronic chagas disease: advances, challenges and perspectives.
J Eukaryot Microbiol. 2015 Jan-Feb;62(1):149-56. doi: 10.1111/jeu.12184. Epub 2014 Nov 13.
7
ProTox: a web server for the in silico prediction of rodent oral toxicity.
Nucleic Acids Res. 2014 Jul;42(Web Server issue):W53-8. doi: 10.1093/nar/gku401. Epub 2014 May 16.
8
Tuning HERG out: antitarget QSAR models for drug development.
Curr Top Med Chem. 2014;14(11):1399-415. doi: 10.2174/1568026614666140506124442.
9
SWISS-MODEL: modelling protein tertiary and quaternary structure using evolutionary information.
Nucleic Acids Res. 2014 Jul;42(Web Server issue):W252-8. doi: 10.1093/nar/gku340. Epub 2014 Apr 29.
10
Structure-dependent binding of arylimidamides to the DNA minor groove.
Chembiochem. 2014 Jan 3;15(1):68-79. doi: 10.1002/cbic.201300622. Epub 2013 Dec 9.
Zotero 插件