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Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
dc.creator | Konstantinović, Jelena M. | |
dc.creator | Videnović, Milica | |
dc.creator | Orsini, Stefania | |
dc.creator | Bogojević, Katarina | |
dc.creator | D'Alessandro, Sarah | |
dc.creator | Scaccabarozzi, Diletta | |
dc.creator | Terzić-Jovanović, Nataša | |
dc.creator | Gradoni, Luigi | |
dc.creator | Basilico, Nicoletta | |
dc.creator | Šolaja, Bogdan | |
dc.date.accessioned | 2020-08-19T21:09:22Z | |
dc.date.available | 2019-05-06 | |
dc.date.issued | 2018 | |
dc.identifier.issn | 1948-5875 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/3626 | |
dc.description.abstract | In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 LT 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 LT 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice. | en |
dc.publisher | American Chemical Society (ACS) | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS// | |
dc.relation | Ministero dellIstruzione, dellUniversita e della Ricerca (PRIN) Project [20154JRJPP_004] | |
dc.relation | Serbian Academy of Sciences and Arts, Executive Programme of Scientific and Technological Cooperation between the Italian Republic and the Republic of Serbia | |
dc.rights | embargoedAccess | |
dc.source | Acs Medicinal Chemistry Letters | |
dc.subject | Leishmania infantum | en |
dc.subject | promastigote | en |
dc.subject | amastigote | en |
dc.subject | mice model | en |
dc.subject | aminoquinoline | en |
dc.title | Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Градони, Луиги; Константиновиц, Јелена; Виденовић, Милица; Шолаја, Богдан; Басилицо, Ницолетта; Орсини, Стефаниа; Богојевић, Катарина; Д'Aлессандро, Сарах; Сцаццабароззи, Дилетта; Терзић Јовановић, Наташа; | |
dc.citation.volume | 9 | |
dc.citation.issue | 7 | |
dc.citation.spage | 629 | |
dc.citation.epage | 634 | |
dc.citation.other | 9(7): 629-634 | |
dc.citation.rank | M21 | |
dc.description.other | This is the peer-reviewed version of the following article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. [https://doi.org/10.1021/acsmedchemlett.8b00053] | |
dc.description.other | The published version: [http://cer.ihtm.bg.ac.rs/handle/123456789/2428] | |
dc.identifier.pmid | 30034591 | |
dc.identifier.doi | 10.1021/acsmedchemlett.8b00053 | |
dc.identifier.fulltext | https://cer.ihtm.bg.ac.rs/bitstream/id/17186/ACC_2018_acsmedchemlett.8b00053.pdf | |
dc.identifier.scopus | 2-s2.0-85046787760 | |
dc.identifier.wos | 000442964000011 | |
dc.type.version | acceptedVersion |