Discovery of Potent and Selective Halogen-Substituted Imidazole-Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro via Structure-Based Design

Autor:	Agata Paneth, Lidia Węglińska, Adrian Bekier, Edyta Stefaniszyn, Monika Wujec, Nazar Trotsko, Anna Hawrył, Miroslaw Hawrył, Katarzyna Dzitko
Jazyk:	angličtina
Rok vydání:	2019
Předmět:	thiosemicarbazides anti-Toxoplasma gondii activity cytotoxicity selectivity ratio structure-activity relationship (SAR) analysis Organic chemistry QD241-441
Zdroj:	Molecules, Vol 24, Iss 8, p 1618 (2019)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules24081618
Popis:	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.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/9957c93ab72f4fa7b5d03bd36871ef9a Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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