Potential anti-amoebic effects of synthetic 1,4-benzothiazine derivatives against Acanthamoeba castellanii

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dc.authoridTaha, Muhammad/0000-0003-3047-9289
dc.authoridSalar, Uzma/0000-0003-1871-9112
dc.authoridSiddiqui, Ruqaiyyah/0000-0001-9646-6208
dc.authoridKhan, Naveed/0000-0001-7667-8553
dc.authorwosidKhan, Naveed/KCK-0156-2024
dc.authorwosidTaha, Muhammad/AAE-6102-2019
dc.authorwosidSalar, Uzma/KBB-0834-2024
dc.authorwosidSiddiqui, Ruqaiyyah/AIF-2100-2022
dc.authorwosidKhan, Naveed/AAM-2892-2021
dc.contributor.authorAlishba
dc.contributor.authorAhmed, Usman
dc.contributor.authorTaha, Muhammad
dc.contributor.authorKhan, Naveed Ahmed
dc.contributor.authorSalar, Uzma
dc.contributor.authorKhan, Khalid Mohammed
dc.contributor.authorAnwar, Ayaz
dc.date.accessioned2024-05-19T14:39:18Z
dc.date.available2024-05-19T14:39:18Z
dc.date.issued2024
dc.departmentİstinye Üniversitesien_US
dc.description.abstractA rare but lethal central nervous system disease known as granulomatous amoebic encephalitis (GAE) and potentially blinding Acanthamoeba keratitis are diseases caused by free-living Acanthamoeba. Currently, no therapeutic agent can completely eradicate or prevent GAE. Synthetic compounds are a likely source of bioactive compounds for developing new drugs. This study synthesized seventeen 1,4-benzothiazine derivatives (I -XVII) by a base-catalyzed one-pot reaction of 2-amino thiophenol with substituted bromo acetophenones. Different spectroscopic techniques, such as EI-MS, H-1-, and C-13 NMR (only for the new compounds), were used for the structural characterization and conformation of compounds. These compounds were assessed for the first time against Acanthamoeba castellanii. All compounds showed anti-amoebic potential in vitro against A. castellanii, reducing its ability to encyst and excyst at 100 mu M. Compounds IX, X, and XVI showed the most potent activities among all derivatives and significantly reduced the viability to 5.3 x 10(4) (p < 0.0003), 2 x 10(5) (p < 0.006), and 2.4 x 10(5) (p < 0.002) cells/mL, respectively. The cytotoxicity profile revealed that these molecules showed lower to moderate cytotoxicity, i.e., 36 %, 2 %, and 21 %, respectively, against human keratinocytes in vitro. These results indicate that 1,4-benzothiazines showed potent in vitro activity against trophozoites and cysts of A. castellanii. Hence, these 1,4-benzothiazine derivatives should be considered to develop new potential therapeutic agents against Acanthamoeba infections.en_US
dc.identifier.doi10.1016/j.heliyon.2023.e23258
dc.identifier.issn2405-8440
dc.identifier.issue1en_US
dc.identifier.pmid38205285en_US
dc.identifier.scopus2-s2.0-85180610662en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org10.1016/j.heliyon.2023.e23258
dc.identifier.urihttps://hdl.handle.net/20.500.12713/4750
dc.identifier.volume10en_US
dc.identifier.wosWOS:001147769600001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherCell Pressen_US
dc.relation.ispartofHeliyonen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.snmz20240519_kaen_US
dc.subjectBenzothiazineen_US
dc.subjectOne -Pot Synthesisen_US
dc.subjectAcanthamoebaen_US
dc.subjectAmoebicidalen_US
dc.titlePotential anti-amoebic effects of synthetic 1,4-benzothiazine derivatives against Acanthamoeba castellaniien_US
dc.typeArticleen_US

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