33199-43-8Relevant articles and documents
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity
Sun, Xiaoqing,Hong, Zexin,Liu, Moyi,Guo, Su,Yang, Di,Wang, Yong,Lan, Tian,Gao, Linyu,Qi, Hongxia,Gong, Ping,Liu, Yajing
, p. 2800 - 2810 (2017/04/18)
A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant potency, and compounds 15b, 15c, 20b, 20c, and 22b were further examined for their inhibitory activity against human FXa in vitro. While compounds 15c and 22b were tested for rat venous thrombosis in vivo. The most promising compound 15c, with an IC50 (FXa) value of 0.14?μM and 98% inhibition rate, warranted further investigation as an FXa inhibitor.
Facile access to a variety of 2,5-biaryl-1,2,4-TRIAZOL-3-ones via regioselective N-arylation of triazolones
Park, Jiyeon,Chae, Junghyun
scheme or table, p. 2143 - 2146 (2010/11/16)
A selective synthetic method of the 2,5-biaryltriazolones has been developed via copper-catalyzed N-arylation reaction. Aryltriazolones, which were readily prepared from commercially available compounds, were N-arylated to 2,5-biaryltriazolones with high regioselectivity. This approach allows for access to a variety of 2,5-biaryl-1,2,4-trizol-3-ones in a simple and practical manner.
Reactions of Sulfur Monochloride with some Aromatic Aldehyde Semicarbazones and Thiosemicarbazones: New Syntheses of Substituted 2,4-Dihydro-1,2,4-triazol-3-ones, 2,4-Dihydro-1,2,4-triazole-3-thiones and 2-Amino-1,3,4-oxadiazoles
Milcent, Rene,Nguyen, Thu-Huong
, p. 881 - 883 (2007/10/02)
Treatment of various substituted semicarbazones of aromatic aldehydes with sulfur monochloride yields the corresponding substituted 2,4-dihydro-1,2,4-triazol-3-ones.With thiosemicarbazones, the products are derivatives either of the 2-amino-1,3,4-thiadiaz