Literature DB >> 20541294

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

André P Liesen1, Thiago M de Aquino, Cristiane S Carvalho, Vânia T Lima, Janete M de Araújo, José G de Lima, Antônio R de Faria, Edésio J T de Melo, Antonio J Alves, Elias W Alves, Anselmo Q Alves, Alexandre J S Góes.   

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). 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 20541294     DOI: 10.1016/j.ejmech.2010.05.017

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  22 in total

1.  1,3,4-Thiadiazoles Effectively Inhibit Proliferation of Toxoplasma gondii.

Authors:  Lidia Węglińska; Adrian Bekier; Katarzyna Dzitko; Barbara Pacholczyk-Sienicka; Łukasz Albrecht; Tomasz Plech; Piotr Paneth; Agata Paneth
Journal:  Cells       Date:  2021-04-29       Impact factor: 6.600

2.  Synthesis and Aldose Reductase Inhibitory Effect of Some New Hydrazinecarbothioamides and 4-Thiazolidinones Bearing an Imidazo[2,1-b]Thiazole Moiety.

Authors:  Nuray Ulusoy Güzeldemirci; Selin Cimok; Net Daş-Evcimen; Mutlu Sarikaya
Journal:  Turk J Pharm Sci       Date:  2018-12-31

3.  Organocatalysis in heterocyclic synthesis: DABCO as a mild and efficient catalytic system for the synthesis of a novel class of quinazoline, thiazolo [3,2-a]quinazoline and thiazolo[2,3-b] quinazoline derivatives.

Authors:  Haider Behbehani; Hamada Mohamed Ibrahim
Journal:  Chem Cent J       Date:  2013-05-07       Impact factor: 4.215

4.  Synthesis, DNA Binding, and Antiproliferative Activity of Novel Acridine-Thiosemicarbazone Derivatives.

Authors:  Sinara Mônica Vitalino de Almeida; Elizabeth Almeida Lafayette; Lúcia Patrícia Bezerra Gomes da Silva; Cézar Augusto da Cruz Amorim; Tiago Bento de Oliveira; Ana Lucia Tasca Gois Ruiz; João Ernesto de Carvalho; Ricardo Olímpio de Moura; Eduardo Isidoro Carneiro Beltrão; Maria do Carmo Alves de Lima; Luiz Bezerra de Carvalho Júnior
Journal:  Int J Mol Sci       Date:  2015-06-09       Impact factor: 5.923

5.  Discovery of potential anti-infectives against Staphylococcus aureus using a Caenorhabditis elegans infection model.

Authors:  Cin Kong; Wageeh A Yehye; Noorsaadah Abd Rahman; Man-Wah Tan; Sheila Nathan
Journal:  BMC Complement Altern Med       Date:  2014-01-06       Impact factor: 3.659

6.  4-Arylthiosemicarbazide derivatives as a new class of tyrosinase inhibitors and anti-Toxoplasma gondii agents.

Authors:  Adrian Bekier; Lidia Węglińska; Agata Paneth; Piotr Paneth; Katarzyna Dzitko
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

7.  2-(4-Oxo-3-phenyl-1,3-thia-zolidin-2-yl-idene)malononitrile.

Authors:  Ola K Sakka; Daisy H Fleita; William T A Harrison
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-02-06

8.  Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives.

Authors:  Lukasz Popiołek; Urszula Kosikowska; Liliana Mazur; Maria Dobosz; Anna Malm
Journal:  Med Chem Res       Date:  2012-11-11       Impact factor: 1.965

9.  Synthesis, Structure and Antioxidant Activity of (Tetra-O-acetyl-β-D-galactopyranosyl)thiosemicarbazones of Substituted Benzaldehydes.

Authors:  Nguyen D Thanh; Le T Hoai
Journal:  Indian J Pharm Sci       Date:  2012-01       Impact factor: 0.975

10.  Synthesis and antioxidant activity evaluation of new compounds from hydrazinecarbothioamide and 1,2,4-triazole class containing diarylsulfone and 2,4-difluorophenyl moieties.

Authors:  Stefania-Felicia Barbuceanu; Diana Carolina Ilies; Gabriel Saramet; Valentina Uivarosi; Constantin Draghici; Valeria Radulescu
Journal:  Int J Mol Sci       Date:  2014-06-17       Impact factor: 5.923

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