68744-66-1Relevant articles and documents
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
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.
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.