306954-98-3Relevant academic research and scientific papers
1,4-disubstituted thiosemicarbazide derivatives are potent inhibitors of toxoplasma gondii proliferation
Dzitko, Katarzyna,Paneth, Agata,Plech, Tomasz,Pawelczyk, Jakub,Staczek, Pawel,Stefanska, Joanna,Paneth, Piotr
, p. 9926 - 9943 (2014/08/05)
A series of 4- Arylthiosemicarbazides substituted at the N1 position with a 5-membered heteroaryl ring was synthesized and evaluated in vitro for T. gondii inhibition proliferation and host cell cytotoxicity. At non- Toxic concentrations for the host cells all studied compounds displayed excellent anti-parasitic effects when compared to sulfadiazine, indicating a high selectivity of their anti-T. gondii activity. The differences in bioactivity investigated by DFT calculations suggest that the inhibitory activity of 4- Arylthiosemicarbazides towards T. gondii proliferation is connected with the electronic structure of the molecule. Further, these compounds were tested as potential antibacterial agents. No growth-inhibiting effect on any of the test microorganisms was observed for all the compounds, even at high concentrations.
Synthesis and biological activities of some novel aminomethyl derivatives of 4-substituted-5-(2-thienyl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones
Koparir, Metin,Orek, Cahit,Parlak, Akif Evren,S?ylemez, Abdurrazak,Koparir, Pelin,Karatepe, Mustafa,Dastan, Sevgi Durna
, p. 340 - 346 (2013/07/27)
A novel series of compounds were synthesized by cyclic condensation reaction of substituted isothiocyanate (2a-c) with 2-thiophenecarboxylic acid hydrazide (1) in the presence of ethyl alcohol, to obtain intermediate thiosemicarbazides (3a-c), which were further treated with sodium hydroxide in the presence of ethanol to obtain triazole derivatives (4a-c). The latter were refluxed with substituted secondary amines and formaldehyde for 6-10 h to afford Mannich bases (5a-k). The synthesized compounds were characterized on the basis of their spectral (IR, 13C and 1H NMR) data and evaluated for biological activities. Some of the compounds were found to exhibit significant antimicrobial and antioxidant activity.
