Antigiardial Activity of Novel Guanidine Compounds.

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 inact

SUBMITTER: Stevens AJ 

PROVIDER: S-EPMC9828538 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature