- Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity
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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.
- Sun, Xiaoqing,Hong, Zexin,Liu, Moyi,Guo, Su,Yang, Di,Wang, Yong,Lan, Tian,Gao, Linyu,Qi, Hongxia,Gong, Ping,Liu, Yajing
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p. 2800 - 2810
(2017/04/18)
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- Synthesis of triazolidines and triazole using DMAP
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An efficient methodology has been developed for the synthesis of 1,2,4-triazolidine-3-thione and 3-ethoxy-5-phenyl-4H-1,2,4 triazole using N,N-dimethylpyridine-4-amine (DMAP). Aldehydes and thiosemicarbazide were reacted in water at ambient temperature in
- Mali, Devidas A.,Telvekar, Vikas N.
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supporting information
p. 324 - 329
(2017/02/10)
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- CONVERSION OF 2-AMINO-5-R-PHENYL-1,3,4-OXADIAZOLES INTO 3-R-PHENYL-5-ALKOXY-1,2,4-TRIAZOLES
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2-Amino-5-R-phenyl-1,3,4-oxadiazoles have been shown to isomerize in alcoholic potassium hydroxide solution to 3-R-phenyl-5-alkoxy-1,2,4-triazoles.The dissociative ionization of 3-R-phenyl-5-alkoxy-1,2,4-triazoles and 3-R-phenyl-1,2,4-triazolin-5-ones has
- Alekseeva, V. Ya.,Boitkov, Yu. A.,Viktorovskii, I. V.,V'yunov, K. A.
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p. 1258 - 1261
(2007/10/02)
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- Heterocycles from N-Benzoylthioamides and Dinucleophilic Reagents
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N-Benzoylthioamides (I) react with hydrazines and hydroxylamine to form 1H-1,2,4-triazoles and 1,2,4-oxazoles, respectively.A similar treatment of the S-methyl derivatives of 1 with amidines leads to 1,3,5-triazines.Ethyl N-benzoylthiocarbamate undergoes analogous reactions to yield the corresponding ethoxyheterocycles.
- Whitfield, Lawrence L.,Papadopoulos, Eleftherios P.
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p. 1197 - 1201
(2007/10/02)
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