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Antigiardial activity of novel guanidine compounds

Stevens, A.J., Abraham, R., Young, K.A., Russell, C.C., McCluskey, S.N., Baker, J.R., Rusdi, B., Page, S.W., O'Handley, R., O'Dea, M.ORCID: 0000-0002-2757-7585, Abraham, S. and McCluskey, A. (2022) Antigiardial activity of novel guanidine compounds. ChemMedChem . Early View.

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From four focused compound libraries based on the known anticoccidial agent robenidine, 44 compounds total were synthesised and screened for antigiardial activity. All active compounds were counter-screened for antibiotic and cytotoxic action. Of the analogues examined, 21 displayed IC50<5 μM, seven with IC50<1.0 μM. Most active were 2,2′-bis{[4-(trifluoromethoxy)phenyl]methylene}carbonimidic dihydrazide hydrochloride (30), 2,2′-bis{[4-(trifluoromethylsulfanyl)phenyl]methylene}carbonimidic dihydrazide hydrochloride (32), and 2,2′-bis[(2-bromo-4,5-dimethoxyphenyl)methylene]carbonimidic dihydrazide hydrochloride (41) with IC50=0.2 μM. The maximal observed activity was a 5 h IC50 value of 0.2 μM for 41. The clinically used metronidazole was inactive at this timepoint at a concentration of 25 μM. Robenidine off-target effects at bacteria and cell line toxicity were removed. Analogue 41 was well tolerated in mice treated orally (100 mg/kg). Following 5 h treatment with 41, no Giardia regrowth was noted after 48 h.

Item Type: Journal Article
Murdoch Affiliation(s): Harry Butler Institute
Antimicrobial Resistance and Infectious Disease Laboratory
Publisher: John Wiley and Sons Ltd
Copyright: © 2022 The Authors.
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