23195-59-7Relevant academic research and scientific papers
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.
A new, high-yield synthesis of 3-aryl-1,2,4-triazoles
Guirado, Antonio,López-Caracena, Libertad,López-Sánchez, José I.,Sandoval, José,Vera, María,Bautista, Delia,Gálvez, Jesús
, p. 8055 - 8060 (2016/11/19)
A convenient new synthetic approach to 3-aryl-1,2,4-triazoles has been developed. Chloralamides were obtained by high yield reactions between benzamides and chloral hydrate. These reacted with a phosphorus pentachloride/phosphorus oxychloride mixture unde
PHARMACEUTICAL COMPOUNDS
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Page/Page column 29, (2012/03/27)
The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to subs
NUCLEAR TRANSPORT MODULATIORS AND USES THEREOF
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Page/Page column 101-102, (2011/10/03)
The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g
SUBSTITUENT AND COORDINATION EFFECTS IN SINGLET REACTIONS OF 3-DIAZO-3H-1,2,4-TRIAZOLES WITH SUBSTITUTED BENZENES AND NITRO COMPOUNDS
Glinka, J.,Fiscus, D.,Rao, C. B.,Shechter, H.
, p. 3221 - 3224 (2007/10/02)
3-Diazo-3H-1,2,4-triazoles convert to singlet 3H-1,2,4-triazol-3-ylidenes which (1) effect directed electrophilic substitutions of benzenes and (2) coordinate with benzenoid substituents and nitro compounds to give decomposition or rearrangement products.
SYNTHESIS OF TRIAZOLES AND OXADIAZOLES FROM 2-ARYL-3-PHENYL-4-IMINO-5-CYANO-3,4-DIHYDROPYRIMIDINES
Robev, Stefan K.
, p. 2903 - 2906 (2007/10/02)
2-Aryl-3-phenyl-4-imino-5-cyano-3,4-dihydropyrimidines I were transformed to 1,2,4-triazoles II,IV and 1,2,4-oxadiazoles III by treatment with hydrazine, arylhydrazines or hydroxylamine in yields up to 90percent.
