- Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors
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Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can provide safe and effective antithrombotic effects. In this study, a series of anthranilamide compounds were designed by utilizing structure-based design strategies. Optimization at P1 and P4 groups led to the discovery of compound 16g: a highly potent, selective fXa inhibitor with pronounced in vitro anticoagulant activity. Moreover, 16g also displayed excellent in vivo antithrombotic activity in the rat venous thrombosis (VT) and arteriovenous shunt (AV-SHUNT) models. The bleeding risk evaluation showed that 16g had a safer profile than that of betrixaban at 1 mg/kg and 5 mg/kg dose. Additionally, 16g also exhibited satisfactory PK profiles. Eventually, 16g was selected to investigate its effect on hypoxia-reoxygenation- induced H9C2 cell viability. MTT results showed that H9C2 cell viability can be remarkably alleviated by 16g.
- Xing, Junhao,Yang, Lingyun,Zhou, Jinpei,Zhang, Huibin
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p. 5987 - 5999
(2018/11/23)
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- Rhodium(III)-Catalyzed Annulation of Pyridinones with Alkynes via Double C-H Activation: A Route to Functionalized Quinolizinones
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A Rh(III)-catalyzed oxidative annulation of pyridin-2(1H)-ones with alkynes via double C-H activation to produce highly functionalized 4H-quinolizin-4-ones is disclosed. This reaction features easily available starting materials, simple manipulation, a relatively wide substrate scope, and good functional group tolerance. The application of this protocol is demonstrated by the synthesis of a known fluorescent quinolizino[3,4,5,6-ija]quinolinium salt.
- Li, Juan,Yang, Yudong,Wang, Zhigang,Feng, Boya,You, Jingsong
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supporting information
p. 3083 - 3086
(2017/06/23)
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- 3,4-dibenzamido benzamide derivative, preparation method and application thereof
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The invention discloses a 3,4-dibenzamido benzamide derivative (I), wherein R1, R2 and R3 are respectively and individually hydrogen, fluorine, chlorine, bromine, hydroxyl groups, alkoxy groups, amino groups or substituted amino groups. The alkoxy groups
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- Tetrabutylammonium pyridin-2-olate: A new reagent for the efficient synthesis of N-aryl pyridin-2-ones
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A new reagent, tetrabutylammonium pyridin-2-olate, was prepared and its application to the efficient synthesis of N-aryl pyridine-2-ones was demonstrated using CuI-catalyzed coupling reactions with aryl iodides. This coupling reaction is mild, high-yielding, and remarkably chemoselective (N- vs. O-arylation). It is also compatible with substrates containing labile functional groups. Georg Thieme Verlag Stuttgart.
- Zhang, Huiping,Chen, Bang-Chi,Wang, Bei,Chao, Sam T.,Zhao, Rulin,Lim, Ngiapkie,Balasubramanian, Balu
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experimental part
p. 1523 - 1526
(2009/04/06)
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- AMINOTHIAZOLE DERIVATIVES AS HUMAN STEAROYL-COA DESATURASE INHIBITORS
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Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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Page/Page column 49
(2008/06/13)
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- Preparation of N-aryl pyridones
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A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. These compounds are useful as intermediates for the synthesis of clinical candidates.
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Page/Page column 10
(2008/06/13)
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- An efficient copper-catalyzed coupling reaction of pyridin-2-ones with aryl and heterocyclic halides based on Buchwald's protocol
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An efficient copper-catalyzed coupling reaction based on the Buchwald's protocol has been established for pyridin-2-ones with aryl iodides, aryl bromides, and heterocyclic bromides.
- Li, Chun Sing,Dixon, Darryl D.
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p. 4257 - 4260
(2007/10/03)
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- Pyridopyrimidones, quinolines and fused N-heterocycles as bradykinin antagonists
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This invention relates to a compound of the formula: STR1 wherein Z is a group of the formula: STR2 in which X1 is N or C--R1, X2 is N or C--R9, X3 is N or C--R2, R1 is lower alk
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