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Type: Journal article
Title: Antigiardial activity of novel guanidine compounds
Author: 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.
Abraham, S.
McCluskey, A.
Citation: ChemMedChem: chemistry enabling drug discovery, 2022; 17(21):e202200341-1-e202200341-6
Publisher: Wiley
Issue Date: 2022
ISSN: 1860-7179
Statement of
Andrew J. Stevens, Rebecca Abraham, Kelly A. Young, Cecilia C. Russell, Siobhann N. McCluskey, Jennifer R. Baker, Bertha Rusdi, Stephen W. Page, Ryan O'Handley, Mark O'Dea, Sam Abraham, Adam McCluskey
Abstract: 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.
Keywords: Animals
Anti-Bacterial Agents
Rights: © 2022 The Authors. ChemMedChem published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
DOI: 10.1002/cmdc.202200341
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Appears in Collections:Animal and Veterinary Sciences publications

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