891085-13-5Relevant academic research and scientific papers
A search for dual action HIV-1 reverse transcriptase, bacterial RNA polymerase inhibitors
Paneth, Agata,Fraczek, Tomasz,Grzegorczyk, Agnieszka,Janowska, Dominika,Malm, Anna,Paneth, Piotr
, (2017/11/20)
Using molecular modeling approach, potential antibacterial agents with triazole core were proposed. A moderate to weak level of antibacterial activity in most of the compounds have been observed, with best minimal inhibitory concentration (MIC) value of 0
Searching for novel scaffold of triazole non-nucleoside inhibitors of HIV-1 reverse transcriptase
Fr?czek, Tomasz,Paneth, Agata,Kamiński, Rafa?,Krakowiak, Agnieszka,Paneth, Piotr
, p. 481 - 489 (2016/03/26)
Azoles are a promising class of the new generation of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). From thousands of reported compounds, many possess the same basic structure of an aryl substituted azole ring linked by a thioglycolamide chain with another aromatic ring. In order to find novel extensions for this basic scaffold, we explored the 5-position substitution pattern of triazole NNRTIs using molecular docking followed by the synthesis of selected compounds. We found that heterocyclic substituents in the 5-position of the triazole ring are detrimental to the inhibitory activity of compounds with four-membered thioglycolamide linker and this substitution seems to be viable only for compounds with shorter two-membered linker. Promising compound, N-(4-carboxy-2-chlorophenyl)-2-((4-benzyl-5-methyl-4H-1,2,4-triazol-3-yl)sulfanyl)acetamide, with potent inhibitory activity and acceptable aqueous solubility has been identified in this study that could serve as lead scaffold for the development of novel water-soluble salts of triazole NNRTIs.
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.
Antimicrobial properties of 4-Aryl-3-(2-methyl-furan-3-yl) δ2-1,2,4-triazoline-5-thiones
Siwek, Agata,Wujec, Monika,Stefanska, Joanna,Paneth, Piotr
scheme or table, p. 3149 - 3159 (2010/04/26)
Four 4-aryl-3-(2-methyl-furan-3-yl)- δ2-1,2,4-triazole-5- thiones were synthesized by intramolecular cyclization of 4-aryl-1-[(2-methyl- furan-3-yl)carbonyl]thiosemicarbazides in alkaline medium. The antimicrobial activity of the synthesized tr
