4432-41-1Relevant academic research and scientific papers
Discovery of Novel Pyrazolo[3,4- b] Pyridine Derivatives with Dual Activities of Vascular Remodeling Inhibition and Vasodilation for the Treatment of Pulmonary Arterial Hypertension
Hu, Liqing,Li, Lijun,Chang, Qi,Fu, Songsen,Qin, Jia,Chen, Zhuo,Li, Xiaohui,Liu, Qinglian,Hu, Gaoyun,Li, Qianbin
, p. 11215 - 11234 (2020/11/09)
Current pulmonary arterial hypertension (PAH) therapeutic strategies mainly focus on vascular relaxation with less emphasis on vascular remodeling, which results in poor prognosis. Hence, dual pathway regulators with vasodilation effect via soluble guanylate cyclase (sGC) stimulation and vascular remodeling regulation effect by AMP-activated protein kinase (AMPK) inhibition provide more advantages and potentialities. Herein, we designed and synthesized a series of novel pyrazolo[3,4-b] pyridine derivatives based on sGC stimulator and AMPK inhibitor scaffolds. In vitro, 2 exhibited moderate vasodilation activity and higher proliferation and migration suppressive effects compared to riociguat. In vivo, 2 significantly decreased right ventricular systolic pressure (RVSP), attenuated pulmonary artery medial thickness (PAMT), and right ventricular hypertrophy (RVH) in hypoxia-induced PAH rat models (i.g.). Given the unique advantages of significant vascular remodeling inhibition and moderate vascular relaxation based on the dual pathway regulation, we proposed 2 as a promising lead for anti-PAH drug discovery.
Direct synthesis of 2-substituted benzonitriles: Via alkylcyanation of arynes with N, N -disubstituted aminomalononitriles
Bao, Wen,Gao, Zhu-Peng,Jin, Da-Ping,Xue, Cao-Gen,Liang, Huan,Lei, Ling-Sheng,Xu, Xue-Tao,Zhang, Kun,Wang, Shao-Hua
supporting information, p. 7641 - 7644 (2020/08/25)
An efficient alkylcyanation of in situ generated arynes by N,N-disubstituted aminomalononitriles is described, enabling the direct synthesis of 2-substituted benzonitriles.
The synthesis of cyanoformamides via a CsF-promoted decyanation/oxidation cascade of 2-dialkylamino-malononitriles
Lei, Lin-Sheng,Xue, Cao-Gen,Xu, Xue-Tao,Jin, Da-Ping,Wang, Shao-Hua,Bao, Wen,Liang, Huan,Zhang, Kun,Asiri, Abdullah M.
supporting information, p. 3723 - 3726 (2019/04/17)
A mild and efficient method for the synthesis of cyanoformamides from N,N-disubstituted aminomalononitriles with CsF as the promoter has been developed. This method features a wide substrate scope and high reaction efficiency, and will facilitate corresponding cyanoformamide-based biological studies and synthetic methodology development.
FLUORINE-SUBSTITUTED INDAZOLE COMPOUNDS AND USES THEREOF
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Paragraph 00345, (2018/11/10)
Fluorine-substituted indazole compounds, pharmaceutical compositions containing these compounds and uses thereof. The compounds and pharmaceutical compositions can be used as soluble guanylate cyclase simulators.
Synthetic method for N,N-disubstituted amino-malononitrile compounds
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Page/Page column 4, (2017/01/02)
The invention relates to a synthetic method for N,N-disubstituted amino-malononitrile compounds. The method has a general reaction formula as described in the specification. According to the synthetic method, amino-substituted malononitrile is formed from N,N-disubstituted formamide and trimethylsilyl cyanide (TMSCN) under the action of a metal copper catalyst. The method provided by the invention has the advantages of easily available raw materials, mild reaction conditions and no need of protection of inert gas; and a concise and highly-efficient preparation method is provided for amino-substituted malononitrile compounds.
