349629-96-5Relevant academic research and scientific papers
Study of direction of cyclization of 1-azolil-4-aryl/alkyl- thiosemicarbazides
Siwek, Agata,Wujec, Monika,Dobosz, Maria,Wawrzycka-Gorczyca, Irena
experimental part, p. 521 - 532 (2011/08/03)
On a four series of 1-azolil-4-aryl/alkyl-thiosemicabazides, a study on the influence of azole moiety on the capability for intramolecular cyclization and its direction was carried out. It was found that for 4-aryl/alkyl- thiosemicabazides with triazole, imidazole, or pyrrole moiety at N-1 nitrogen atom possible products were only s-triazoles, both in alkaline and acidic medium. Successful dehydrocyclization of 1-azolil-4-aryl/alkyl- thiosemicarbazides leading to a thiadiazole has been documented only for a series of 1-(4-methyl-1,2,3-thiadiazol-5-yl-carbonyl)-4-aryl/alkyl- thiosemicarbazides. It can be speculative that the determination of pK a value of oxygen atom of 1-azolil-4-aryl/alkyl-thiosemicarbazide can be a very valuable parameter in the prediction of the possibility of dehydrocyclization to form thiadiazole.
Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles
Liesen, André P.,De Aquino, Thiago M.,Carvalho, Cristiane S.,Lima, Vania T.,De Araújo, Janete M.,De Lima, José G.,De Faria, Ant?nio R.,De Melo, Edésio J.T.,Alves, Antonio J.,Alves, Elias W.,Alves, Anselmo Q.,Góes, Alexandre J.S.
experimental part, p. 3685 - 3691 (2010/11/03)
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, 1H, 13C 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).
