Next generation imidazothiazole and imidazooxazole derivatives as potential drugs against brain-eating amoebae

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dc.authorscopusidRuqaiyyah Siddiqui / 18635417000
dc.authorscopusidNaveed Ahmed Khan / 58685542900
dc.authorwosidNaveed Ahmed Khan / GWD-0187-2022
dc.authorwosidRuqaiyyah Siddiqui / AIF-2100-2022
dc.contributor.authorAkbar, Noor
dc.contributor.authorSiddiqui, Ruqaiyyah
dc.contributor.authorEl-Gamal, Mohammed I.
dc.contributor.authorKhan, Naveed Ahmed
dc.contributor.authorZaraei, Seyed-Omar
dc.contributor.authorSaeed, Balsam Qubais
dc.contributor.authorAlharbi, Ahmad M.
dc.contributor.authorDash, Nihar Ranjan
dc.date.accessioned2025-04-18T10:06:07Z
dc.date.available2025-04-18T10:06:07Z
dc.date.issued2024
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Cerrahi Tıp Bilimleri Bölümü
dc.description.abstractManaging primary amoebic meningoencephalitis, induced by Naegleria fowleri poses a complex medical challenge. There is currently no specific anti-amoebic drug that has proven effectiveness against N. fowleri infection. Ongoing research endeavours are dedicated to uncovering innovative treatment strategies, including the utilization of drugs and immune modulators targeting Naegleria infection. In this study, we explored the potential of imidazo[2,1-b]thiazole and imidazooxazole derivatives that incorporate sulfonate and sulfamate groups as agents with anti-amoebic properties against N. fowleri. We assessed several synthesized compounds (1f, 1m, 1q, 1s, and 1t) for their efficacy in eliminating amoebae, their impact on cytotoxicity, and their influence on the damage caused to human cerebral microvascular endothelial (HBEC-5i) cells when exposed to the N. fowleri (ATCC 30174) strain. The outcomes revealed that, among the five compounds under examination, 1m, 1q, and 1t demonstrated notable anti-parasitic effects against N. fowleri (P <= 0.05). Compound 1t exhibited the highest anti-parasitic activity, reducing N. fowleri population by 80%. Additionally, three compounds, 1m, 1q, and 1t, significantly mitigated the damage inflicted on host cells by N. fowleri. However, the results of cytotoxicity analysis indicated that while 1m and 1q had minimal cytotoxic effects on endothelial cells, compound 1t caused moderate cytotoxicity (34%). Consequently, we conclude that imidazo[2,1-b]thiazole and imidazooxazole derivatives containing sulfonate and sulfamate groups exhibit a marked capacity to eliminate amoebae viability while causing limited toxicity to human cells. In aggregate, these findings hold promise that could potentially evolve into novel therapeutic options for treating N. fowleri infection
dc.description.sponsorshipUniversity of Sharjah, United Arab Emirates United States Department of Defense Air Force Office of Scientific Research (AFOSR) Taif University
dc.identifier.citationAkbar, N., Siddiqui, R., El-Gamal, M. I., Khan, N. A., Zaraei, S. O., Saeed, B. Q., ... & Dash, N. R. (2024). Next generation imidazothiazole and imidazooxazole derivatives as potential drugs against brain-eating amoebae. Parasitology Research, 123(6), 241.
dc.identifier.doi10.1007/s00436-024-08255-5
dc.identifier.endpage9
dc.identifier.issn0932-0113
dc.identifier.issn1432-1955
dc.identifier.issue6
dc.identifier.pmid38864931
dc.identifier.scopus2-s2.0-85195888155
dc.identifier.scopusqualityQ1
dc.identifier.startpage1
dc.identifier.urihttp://dx.doi.org/10.1007/s00436-024-08255-5
dc.identifier.urihttps://hdl.handle.net/20.500.12713/6943
dc.identifier.volume123
dc.identifier.wosWOS:001244857200001
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorSiddiqui, Ruqaiyyah
dc.institutionauthorKhan, Naveed Ahmed
dc.institutionauthoridRuqaiyyah Siddiqui / 0000-0001-9646-6208
dc.institutionauthoridNaveed Ahmed Khan / 0000-0001-7667-8553
dc.language.isoen
dc.publisherSpringer
dc.relation.ispartofParasitology research
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectBrain-Eating Amoebae
dc.subjectHuman Cell
dc.subjectTreatment
dc.subjectDrugs
dc.subjectTherapy
dc.subjectBrain Infection
dc.titleNext generation imidazothiazole and imidazooxazole derivatives as potential drugs against brain-eating amoebae
dc.typeArticle

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