Research Output
Bringing forward the new generation of alkoxy-thiourea as potential treatment for Acanthamoeba keratitis
Cytotoxicity effects of alkoxy substituted thiourea derivatives towards Acanthamoeba sp.
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Publication
Alkoxy substituted thiourea derivatives with general formula of A-ArC(O)NHC(S)NHAr-D which A represents the methoxy group and D denotes -OCnH2n+1 have been successfully synthesised and characterized. In turn, all the synthesised molecules were assayed for anti-amoebic activities towards Acanthamoeba sp to examine the cytotoxicity effect at their IC50 and membrane permeability. As predicted, the findings showed that the synthesised molecules owing promising anti-amoebic activity towards Acanthamoeba sp. To support, the Acridine-orange/Propidium iodide (AOPI) staining result under fluorescence microscopy revealed the treated amoeba cells by these alkoxy thiourea derivatives exhibited loss in their membrane permeability.
Publication
In this study, the effort was to design and synthesize five new members of alkoxy substituted thiourea derivatives (3a–3e) featuring general formula of A-ArC(O)NHC(S)NHAr-D in which A represents the methoxy group and D as –OCnH2n+1 (alkoxyl group, where n = 6,7,8,9, and 10) have been successfully designed, prepared, characterized, and evaluated for anti-amoebic activities. They were spectroscopically characterized by 1H and 13C Nuclear Magnetic Resonance (NMR), Fourier Transform Infrared (FT-IR) spectroscopy, and Ultraviolet–visible (UV–vis) spectroscopy analysis. In turn, they were used to investigate the cytotoxicity effect on Acanthamoeba sp. at their IC50 values and membrane permeability. Compounds 3a and 3b revealed to have good activity towards Acanthamoeba sp. compared to other compounds of 3c, 3d, and 3e. The observation under fluorescence microscopy by AOPI (Acridine-orange/Propidium iodide) staining indicated that treated amoeba cells by 3a–3e show loss of their membrane permeability.