Design, synthesis, and in vitro biological evaluation of novel thiazolopyrimidine derivatives as antileishmanial compounds

Basit Öğe Kaydı
dc.contributor.authorIstanbullu, Huseyin
dc.contributor.authorBayraktar, Gulsah
dc.contributor.authorAkbaba, Hasan
dc.contributor.authorCavus, Ibrahim
dc.contributor.authorCoban, Gunes
dc.contributor.authorButuner, Bilge Debelec
dc.contributor.authorErciyas, Ercin
dc.date.accessioned2020-12-01T12:01:04Z
dc.date.available2020-12-01T12:01:04Z
dc.date.issued2020
dc.departmentEge Üniversitesien_US
dc.description.abstractA series of thiazolopyrimidine derivatives was designed and synthesized as aLeishmania majorpteridine reductase 1 (LmPTR1) enzyme inhibitor. TheirLmPTR1 inhibitor activities were evaluated using the enzyme produced byEscherichia coliin a recombinant way. the antileishmanial activity of the selected compounds was tested in vitro againstLeishmaniasp. Additionally, the compounds were evaluated for cytotoxic activity against the murine macrophage cell line RAW 264.7. According to the results, four compounds displayed not only a potent in vitro antileishmanial activity against promastigote forms but also low cytotoxicity. Among them, compoundL16exhibited an antileishmanial activity for both the promastigote and amastigote forms ofL. tropica, with IC(50)values of 7.5 and 2.69 mu M, respectively. in addition, molecular docking studies and molecular dynamics simulations were also carried out in this study. in light of these findings, the compounds provide a new potential scaffold for antileishmanial drug discovery.en_US
dc.description.sponsorshipTurkiye Bilimsel ve Teknolojik Arastirma KurumuTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [SBAG-213-S026]; Ege Universitesi [2014BIL003]en_US
dc.description.sponsorshipTurkiye Bilimsel ve Teknolojik Arastirma Kurumu, Grant/Award Number: SBAG-213-S026; Ege Universitesi, Grant/Award Number: 2014BIL003en_US
dc.identifier.doi10.1002/ardp.201900325en_US
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue8en_US
dc.identifier.pmid32484266en_US
dc.identifier.scopus2-s2.0-85085889453en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.201900325
dc.identifier.urihttps://hdl.handle.net/11454/62262
dc.identifier.volume353en_US
dc.identifier.wosWOS:000539399200001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectantileishmanialen_US
dc.subjectLeishmania majoren_US
dc.subjectLeishmania tropicaen_US
dc.subjectneglected diseaseen_US
dc.subjectPTR1 enzyme inhibitionen_US
dc.subjectthiazolo[5en_US
dc.subject4-d]pyrimidineen_US
dc.titleDesign, synthesis, and in vitro biological evaluation of novel thiazolopyrimidine derivatives as antileishmanial compoundsen_US
dc.typeArticleen_US

Dosyalar

Koleksiyon

WoS İndeksli Yayınlar Koleksiyonu
PubMed İndeksli Yayın Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu