68744-66-1Relevant academic research and scientific papers
Synthesis, antifungal activity, 3d-qsar, and molecular docking study of novel menthol-derived 1,2,4-triazole-thioether compounds
Duan, Wen-Gui,Huang, Mei,Li, Bao-Yu,Lin, Gui-Shan
, (2021/11/30)
A series of novel menthol derivatives containing 1,2,4-triazole-thioether moiety were designed, synthesized, characterized structurally, and evaluated biologically to explore more potent natural product-based antifungal agents. The bioassay results reveal
Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation
Vergani, Barbara,Sandrone, Giovanni,Marchini, Mattia,Ripamonti, Chiara,Cellupica, Edoardo,Galbiati, Elisabetta,Caprini, Gianluca,Pavich, Gianfranco,Porro, Giulia,Rocchio, Ilaria,Lattanzio, Maria,Pezzuto, Marcello,Skorupska, Malgorzata,Cordella, Paola,Pagani, Paolo,Pozzi, Pietro,Pomarico, Roberta,Modena, Daniela,Leoni, Flavio,Perego, Raffaella,Fossati, Gianluca,Steinkühler, Christian,Stevenazzi, Andrea
, p. 10711 - 10739 (2019/12/02)
Histone deacetylase 6 (HDAC6) is a peculiar HDAC isoform whose expression and functional alterations have been correlated with a variety of pathologies such as autoimmune disorders, neurodegenerative diseases, and cancer. It is primarily a cytoplasmic protein, and its deacetylase activity is focused mainly on nonhistone substrates such as tubulin, heat shock protein (HSP)90, Foxp3, and cortactin, to name a few. Selective inhibition of HDAC6 does not show cytotoxic effects in healthy cells, normally associated with the inhibition of Class I HDAC isoforms. Here, we describe the design and synthesis of a new class of potent and selective HDAC6 inhibitors that bear a pentaheterocyclic central core. These compounds show a remarkably low toxicity both in vitro and in vivo and are able to increase the function of regulatory T cells (Tregs) at well-tolerated concentrations, suggesting a potential clinical use for the treatment of degenerative, autoimmune diseases and for organ transplantation.
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists
Micheli, Fabrizio,Bacchi, Alessia,Braggio, Simone,Castelletti, Laura,Cavallini, Palmina,Cavanni, Paolo,Cremonesi, Susanna,Dal Cin, Michele,Feriani, Aldo,Gehanne, Sylvie,Kajbaf, Mahmud,Marchió, Luciano,Nola, Selena,Oliosi, Beatrice,Pellacani, Annalisa,Perdonà, Elisabetta,Sava, Anna,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Wong, Andrea,Visentini, Filippo,Zonzini, Laura,Heidbreder, Christian
, p. 8549 - 8576 (2016/10/03)
A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with respect to their pharmacokinetic properties both in vitro and in vivo during lead identification and early lead optimization phases. A few derivatives with overall favorable developability characteristics were selected for further late lead optimization studies.
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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Page/Page column 113; 117, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase-Structure-activity relationships and crystallographic analysis
Kirschberg, Thorsten A.,Balakrishnan, Mini,Huang, Wei,Hluhanich, Rebecca,Kutty, Nilima,Liclican, Albert C.,McColl, Damian J.,Squires, Neil H.,Lansdon, Eric B.
, p. 1131 - 1134 (2008/12/21)
A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to be identified.
5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents
Kane,Staeger,Dalton,Miller,Dudley,Ogden,Kehne,Ketteler,McCloskey,Senyah,Chmielewski,Miller
, p. 125 - 132 (2007/10/02)
Selected examples from three series of isomeric (alkylthio)-1,2,4- triazoles were prepared and examined for anticonvulsant activity versus strychnine-, maximal-electroshock-, pentylenetetrazole-, and 3- mercaptopropionic-acid-induced seizures in mice. A n
3-aryl-5-alkylthio-4H-1,2,4-triazoles
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, (2008/06/13)
This invention relates to derivatives of 3-aryl-5-alkylthio-4H-1,2,4-triazoles, to their pharmacological properties and to their use as muscle relaxants, spasmolytics, anticonvulsants and anxiolytics.
