Akbar, Noor El-Gamal, Mohammed, I Saeed, Balsam Qubais Oh, Chang-Hyun Abdel-Maksoud, Mohammed S. Khan, Naveed Ahmed Alharbi, Ahmad M. Alfahemi, Hasan Siddiqui, Ruqaiyyah 2024-01-19T11:03:59Z 2024-01-19T11:03:59Z 2022-09-29 2022-09 https://pubs.kist.re.kr/handle/201004/114582 We examined the antiamoebic effect of several imidazothiazole derivatives on Acanthamoeba castellanii of the T4 genotype. Trypan blue exclusion assays and haemocytometer counting were used to determine the reduction in A. castellanii trophozoite proliferation, in response to treatment with these compounds. To determine the effects of these compounds on host cells, lactate dehydrogenase assay was performed using HeLa cell lines. Amoebicidal assays revealed that the tested compounds at concentrations of 50 mu M significantly inhibited amoebae trophozoites compared to controls. Compounds 1m and 1zb showed the highest amoebicidal effects eradicating 70% and 67% of A. castellanii, respectively. The compounds blocked both the encystation and excystation process in A. castellanii. Compounds 1m and 1zb blocked 61% and 55%, respectively, of amoeba binding to human cells. Moreover, the compounds showed minimal cytotoxic effects against host cells and considerably reduced amoeba-mediated host cell death. Overall, our study revealed that compounds 1m and 1zb have excellent antiamoebic potential, and should be considered in the development of curative antiamoebic medications in future studies. Further work is critical to determine the translational value of these findings. English Multidisciplinary Digital Publishing Institute (MDPI) Antiamoebic Activity of Imidazothiazole Derivatives against Opportunistic Pathogen Acanthamoeba castellanii Article 10.3390/antibiotics11091183 1 Antibiotics, v.11, no.9 Antibiotics 11 9 Y scie scopus 000856150200001 Infectious Diseases Pharmacology & Pharmacy Infectious Diseases Pharmacology & Pharmacy Article IN-VITRO ANTIPROLIFERATIVE ACTIVITY CLINICAL STRAINS INHIBITORS KERATITIS AMEBAS Acanthamoeba castellanii amoebicidal encystation excystation cytotoxicity cytopathogenicity imidazothiazole