934539-24-9Relevant articles and documents
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor
Xue, Tao,Ding, Shi,Guo, Bin,Zhou, Yuren,Sun, Peng,Wang, Heyao,Chu, Wenjing,Gong, Guoqing,Wang, Yinye,Chen, Xiaoyan,Yang, Yushe
, p. 7770 - 7791 (2014)
The blood coagulation enzyme factor Xa (FXa) is a particularly promising target for anticoagulant therapy, and identification of oral small-molecule inhibitors of FXa remains a research focus. On the basis of the X-ray crystal structure of FXa and its inhibitor rivaroxaban, we designed and synthesized a series of conformationally restricted mimics containing a novel [6,6,5] tricyclic fused oxazolidinone scaffold. Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles. Druggability evaluation of compound 11a was undertaken and elicited positive outcomes. All results indicate that compound 11a is a promising drug candidate for the prevention and treatment of thromboembolic diseases in venous and arterial systems.
A mild and metal-free synthesis of chiral 2,3-dihydro-3-hydroxymethyl-1,4-benzoxazines
Cheng, Shihao,Huang, Haihong,Li, Shengnan,Lin, Ziyun,Zhang, Dongfeng,Zhao, Hongyi
, (2021/07/06)
Various functionalized enantiomerically pure 3-hydroxymethyl-1,4-benzoxazine derivatives, including four stereoisomers, were synthesized from chiral 2,3-epoxy-4-trityloxybutanol. The synthesis was mild and metal-free. Yields of 52%–94%, and stereoselectiv
Tricyclic oxazolidone comound, and preparation method and use thereof
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, (2016/10/07)
The invention relates to a novel tricyclic oxazolidone comound, and a preparation method and a use thereof, and concretely discloses a compound with the structure represented by formula I, an enantiomer, a diastereomer or a raceme thereof or a mixture of the enantiomer, the diastereomer and the raceme, or a pharmaceutically acceptable salt thereof. The formula I is shown in the specification. The invention also discloses a preparation method of the compound, and an application of the compound in FXa target related disease treatment drugs.