Azole-based compounds as potential anti-Acanthamoeba agents

Basit Öğe Kaydı
dc.contributor.authorQubais, Saeed, B.
dc.contributor.authorHamdy, R.
dc.contributor.authorAkbar, N.
dc.contributor.authorSajeevan, S.E.
dc.contributor.authorKhan, N.A.
dc.contributor.authorSoliman, S.S.M.
dc.date.accessioned2024-05-19T14:34:33Z
dc.date.available2024-05-19T14:34:33Z
dc.date.issued2024
dc.departmentİstinye Üniversitesien_US
dc.description.abstractAcanthamoeba castellanii is an opportunistic pathogen with public health implications, largely due to its invasive nature and non-specific symptoms. Our study focuses on the potential of azole compounds, particularly those with triazole scaffolds, as anti-amoebic agents. Out of 10 compounds, compounds T1 and T8 exhibited effective anti-Acanthamoeba activity with MIC50 values of 125.37 and 143.92 ?g mL?1, respectively. Interestingly, compounds T1, T4, T5 and T8 revealed profound anti-excystation activity with MIC50 at 32.01, 85.53, 19.54 and 80.57 ?g mL?1, respectively, alongside limited cytotoxicity to human cells. The study underscores the potential of T1, T4, T5, and T8, thiazole-based compounds, as anti-Acanthamoeba agents by both eliminating amoeba viability and preventing excystation, via preserving the amoeba in its latent cyst form, exposing them to elimination by the immune system. Notably, compounds T1, T4, T5, and T8 showed optimal molecular properties, moderate oral bioavailability, and stable complex formation with Acanthamoeba CYP51. They also display superior binding interactions. Further research is needed to understand their mechanisms and optimize their efficacy against Acanthamoeba infections. © 2024 RSC.en_US
dc.description.sponsorshipSafety, Security, and Mission Services, SSMS; Air Force Office of Scientific Research, AFOSR; University of Sharjah, UOS: 2101090286en_US
dc.description.sponsorshipThe authors acknowledge the generous funding from the University of Sharjah (Grant# 2101090286) to BQ and SSMS and the support from the Air Force Office of Scientific Research (AFOSR), USA to NK.en_US
dc.identifier.doi10.1039/d4md00029c
dc.identifier.issn2632-8682
dc.identifier.scopus2-s2.0-85189544192en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1039/d4md00029c
dc.identifier.urihttps://hdl.handle.net/20.500.12713/4509
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherRoyal Society of Chemistryen_US
dc.relation.ispartofRSC Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240519_kaen_US
dc.titleAzole-based compounds as potential anti-Acanthamoeba agentsen_US
dc.typeArticleen_US

Dosyalar

Koleksiyon

Scopus İndeksli Yayınlar Koleksiyonu