Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles

European Journal of Medicinal Chemistry
2010.0

Abstract

In this work we reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d. All synthesized compounds were characterized by IR, (1)H, (13)C NMR and HRMS. The majority of the tested compounds show excellent anti-T. gondii activity when compared to hydroxyurea and sulfadiazine. In addition it was also shown that most of the compounds in this study have a better performance against intracellular tachyzoites. The results for antimicrobial activity evaluation showed weak antibacterial and antifungal activities for all the tested molecules, when compared with the standard drugs (chloramphenicol and rifampicin for antibacterial activity; nistatin and ketoconazole for antifungal activity).

Knowledge Graph

Similar Paper

Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles
European Journal of Medicinal Chemistry 2010.0
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids
Bioorganic & Medicinal Chemistry 2008.0
Synthesis of thiosemicarbazone and 4-thiazolidinone derivatives and their in vitro anti-Toxoplasma gondii activity
Bioorganic & Medicinal Chemistry Letters 2005.0
Evaluating anti-Toxoplasma gondii activity of new serie of phenylsemicarbazone and phenylthiosemicarbazones in vitro
Medicinal Chemistry Research 2013.0
4-Arylthiosemicarbazide derivatives – Pharmacokinetics, toxicity and anti-Toxoplasma gondii activity in vivo
European Journal of Medicinal Chemistry 2022.0
Design, synthesis and biological characterization of thiazolidin-4-one derivatives as promising inhibitors of Toxoplasma gondii
European Journal of Medicinal Chemistry 2014.0
Synthesis and Evaluation of 4-Acyl-2-thiazolylhydrazone Derivatives for Anti-Toxoplasma Efficacy in Vitro
Journal of Medicinal Chemistry 2009.0
Synthesis and antimycobacterial activities of some new N-acylhydrazone and thiosemicarbazide derivatives of 6-methyl-4,5-dihydropyridazin-3(2H)-one
Medicinal Chemistry Research 2012.0
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety
European Journal of Medicinal Chemistry 2010.0
Synthesis and evaluation of antibacterial and antitubercular activities of some novel imidazo[2,1-b][1,3,4]thiadiazole derivatives
Medicinal Chemistry Research 2013.0