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.
- Abraham, S.
- McCluskey, A.
DOIAbstract
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 in...
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