Abstract
Employing a simple synthetic protocol, a series of highly effective halogen-substituted imidazole-thiosemicarbazides with anti-Toxoplasma gondii effects against the RH tachyzoites, much better than sulfadiazine, were obtained (IC50s 10.30—113.45 µg/mL vs. ~2721.45 µg/mL). The most potent of them, 12, 13, and 15, blocked the in vitro proliferation of T. gondii more potently than trimethoprim (IC50 12.13 µg/mL), as well. The results of lipophilicity studies collectively suggest that logP would be a rate-limiting factor for the anti-Toxoplasma activity of this class of compounds.
Highlights
Toxoplasma gondii is a common zoonotic infection of humans, and estimates prove that up to one third of the world’s population is chronically infected [1,2]
RH leads strainto tothe sulfadiazine and trimethoprim, inhibitory effect against gondii proliferation increases with halogen size from fluorine to iodine; we further investigated the efficacy of 5–16 in blocking T. gondii proliferation
Assessment theexample results in terms of features leads to the followinglisted conclusions: For example, metaand para-bromo derivatives and show higher selectivity ratios and only the inhibitory effect against T. gondii proliferation increases with halogen size from fluorine to slightly inhibitory thanand control trimethoprim
Summary
Toxoplasma gondii is a common zoonotic infection of humans, and estimates prove that up to one third of the world’s population is chronically infected [1,2]. 2 of 15 effect of suppose that the2019, deactivation of the N4 phenyl ring, through the inductive withdrawing halogen atoms, should result in compounds with potent activity against T. gondii tachyzoites growth. This goal by further exploiting the N4 phenyl position of the imidazole-thiosemicarbazide core with. Halogenation the blood-brain barrier permeability, insertion of halogens during the synthesisenhances of final compounds [20,21,22] This strategy is based on the which is a observation that that incorporation the halogen atoms intoanti-toxoplasma a new bioactive chemical pre-requisite for drugs need toofreach the CNS, like drugsentity andimproves many others [24].
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