Imidazothiazole derivatives exhibited potent effects against brain-eating amoebae

dc.authoridNaveed Ahmed Han / 0000-0001-7667-8553en_US
dc.authoridRuqaiyyah Siddiqui / 0000-0001-9646-6208en_US
dc.authorscopusidNaveed Ahmed Han / 7401797675
dc.authorscopusidRuqaiyyah Siddiqui / JYL-4605-2024
dc.authorwosidRuqaiyyah Siddiqui / JYL-4605-2024en_US
dc.authorwosidNaveed Ahmed Han / AAM-2892-2021en_US
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorEl-Gamal, Mohammed, I
dc.contributor.authorBoghossian, Anania
dc.contributor.authorSaeed, Balsam Qubais
dc.contributor.authorOh, Chang-Hyun
dc.contributor.authorAbdel-Maksoud, Mohammed S.
dc.contributor.authorAlharbi, Ahmad M.
dc.contributor.authorAlfahemi, Hasan
dc.contributor.authorKhan, Naveed Ahmed
dc.date.accessioned2022-12-02T07:39:09Z
dc.date.available2022-12-02T07:39:09Z
dc.date.issued2022en_US
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Cerrahi Tıp Bilimleri Bölümüen_US
dc.description.abstractNaegleria fowleri (N. fowleri) is a free-living, unicellular, opportunistic protist responsible for the fatal central nervous system infection, primary amoebic meningoencephalitis (PAM). Given the increase in temperatures due to global warming and climate change, it is estimated that the cases of PAM are on the rise. However, there is a current lack of awareness and effective drugs, meaning there is an urgent need to develop new therapeutic drugs. In this study, the target compounds were synthesized and tested for their anti-amoebic properties against N. fowleri. Most compounds exhibited significant amoebicidal effects against N. fowleri; for example, 1h, 1j, and 1q reduced N. fowleri's viability to 15.14%, 17.45% and 28.78%, respectively. Furthermore, the majority of the compounds showed reductions in amoeba-mediated host death. Of interest are the compounds 1f, 1k, and 1v, as they were capable of reducing the amoeba-mediated host cell death to 52.3%, 51%, and 56.9% from 100%, respectively. Additionally, these compounds exhibit amoebicidal properties as well; they were found to decrease N. fowleri's viability to 26.41%, 27.39%, and 24.13% from 100%, respectively. Moreover, the MIC50 values for 1e, 1f, and 1h were determined to be 48.45 mu M, 60.87 mu M, and 50.96 mu M, respectively. Additionally, the majority of compounds were found to exhibit limited cytotoxicity, except for 1l, 1o, 1p, 1m, 1c, 1b, 1zb, 1z, 1y, and 1x, which exhibited negligible toxicity. It is anticipated that these compounds may be developed further as effective treatments against these devastating infections due to brain-eating amoebae.en_US
dc.identifier.citationSiddiqui, R., El-Gamal, M. I., Boghossian, A., Saeed, B. Q., Oh, C. H., Abdel-Maksoud, M. S., ... & Khan, N. A. (2022). Imidazothiazole Derivatives Exhibited Potent Effects against Brain-Eating Amoebae. Antibiotics, 11(11), 1515.en_US
dc.identifier.doi10.3390/antibiotics11111515en_US
dc.identifier.issn2079-6382en_US
dc.identifier.issue11en_US
dc.identifier.scopus2-s2.0-85141795224en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttp://dx.doi.org/10.3390/antibiotics11111515
dc.identifier.urihttps://hdl.handle.net/20.500.12713/3401
dc.identifier.volume11en_US
dc.identifier.wosWOS:000880683700001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorSiddiqui, Ruqaiyyah
dc.institutionauthorKhan, Naveed Ahmed
dc.language.isoenen_US
dc.publisherMDPIen_US
dc.relation.ispartofANTIBIOTICS-BASELen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectNaegleria Fowlerien_US
dc.subjectAmoebicidalen_US
dc.subjectAnti-Amoebicen_US
dc.subjectMortalityen_US
dc.subjectCytotoxicityen_US
dc.subjectCytopathogenicityen_US
dc.titleImidazothiazole derivatives exhibited potent effects against brain-eating amoebaeen_US
dc.typeArticleen_US

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