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. 2022 Nov 23;209:105473. doi: 10.1016/j.antiviral.2022.105473

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© 2022 The Authors

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Fig. 2 — Thiosemicarbazide (class I) shows target specificity, and its analogs show regions for their antiviral potency. a) Structure of newly-synthesized thiosemicarbazide derivatives. The modified moieties compared to compound 1 or 1f are highlighted in green (2-pyridine), purple (thiosemicarbazide), orange (pyridine), and blue (p-trifuloromethylphenyl). b) Potency (IC₅₀ or EC₅₀ (μM)), cytotoxicity (CC₅₀ (μM)), and selective index (SI = CC₅₀/EC₅₀ (MERS-CoV infection assay)) of thiosemicarbazide derivatives as evaluated in alpha test, pseudovirus assay, and immunofluorescence-based MERS-CoV infection assay. CC₅₀ values that are >50 μM were considered as 50 μM when calculating SI. n.d; not determined. c) Schematic presentation of the ELISA using hDPP4 and the RBD of the S1 of MERS-CoV spike. d-f) Three compounds, 1 (d), 1g-8 (e), and 1j (f) tested for their inhibiting activity on the binding between hDDP4 and RBD. Each data point represents the mean of triplicate assays with ±SEM, and their IC₅₀ values were calculated through curve fitting analysis using Prism 6.0.