111118-65-1Relevant academic research and scientific papers
The novel compound MP407 inhibits platelet aggregation through cyclic AMP-dependent processes
Lin, Chung-Shuen,Chen, Tso-Hsiao,Lin, I-Hsin,Lee, An-Rong,Chou, Tz-Chong
, p. 324 - 331 (2017)
Platelet hyperactivity plays a critical role for initiating several vascular diseases such as atherothrombosis. Therefore, development of effective antiplatelet agents is necessary for ameliorating platelet-related diseases. In this study, we investigated the effects of the new synthesized compound, MP407 on platelet aggregation and further elucidated the underlying mechanisms. Our results demonstrated that MP407 dose-dependently inhibited collagen-induced platelet aggregation, thromboxane B2 (TXB2) production, intracellular Ca2+ mobilization, platelet membrane GPIIb/IIIa expression, and the phosphorylation of Akt, GSK3β, p38MAPK, and phospho (Ser) PKC substrate (p47). Moreover, MP407 is able to increase the cyclic AMP formation both in resting and activated platelets. However, blocking cyclic AMP formation with 2′5′-ddAdo, an inhibitor of adenylate cyclase, greatly reversed the antiplatelet activity of MP407 and related platelet-activating pathways. MP407 also enhanced VASP phosphorylation at Ser157 in collagen-stimulated platelets, which was attenuated by addition of 2′5′-ddAdo. Therefore, the antiplatelet activity of MP407 may be modulated by cyclic AMP-dependent regulation of Akt, GSK3β, p38MAPK and VASP phosphorylation. Notably, treatment with MP407 markedly reduced the pulmonary thrombosis and the numbers of paralysis and death in mice induced by ADP injection, but did not affect the bleeding time. Taken together, MP407 may be a potential candidate or lead compound for developing novel antiplatelet or antithrombotic agents for platelet hyperactivity-triggered disease therapy.
Copper-catalyzed C-H [3 + 2] annulation of: N-substituted anilines with α-carbonyl alkyl bromides via C(sp3)-Br/C(sp2)-H functionalization
Cao, An-Zhu,Li, Jin-Heng,Song, Ren-Jie,Wu, Yan-Chen,Xiao, Yu-Ting,Xie, Ye-Xiang
, p. 2170 - 2174 (2020)
A copper-catalyzed C-H [3 + 2] annulation of N-substituted anilines with α-carbonyl alkyl bromides for the synthesis of 3,3′-disubstituted oxindoles is developed. Tandem C-H cycloamidation reactions of various α-carbonyl alkyl bromide derivatives including tertiary-α-bromoalkyl ketone esters, malonic esters and cycloalkanes, with N-Aryl or alkyl substituted anilines, can be performed using this system, affording a vast array of valuable 3,3′-disubstituted oxindoles in moderate to good yields.
Synthesis method of 3,3'-disubstituted-2-indolone compound
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Paragraph 0030-0034; 0038; 0043, (2019/07/16)
The invention discloses a synthesis method of a 3,3'-disubstituted-2-indolone compound. The synthesis method comprises the following steps: with an aniline compound as a raw material, directly carrying out a reaction with ethyl bromoacetate compound for o
Synthesis of 1,3-dihydro-3,3-dimethyl-2H-indol-2-one derivatives as possible nonsteroidal cardiotonics
Lee,Huang,Lin,Shih,Lee,Lin
, p. 1 - 11 (2007/10/02)
New substituted 1,3-dihydro-3,3-dimethyl-2H-indol-2-one derivatives 19-29 and 34-43 were synthesized and examined for their inotropic activity in isolated dog ventricular tissues. Among them, compound 26 (2-(2,3-dimethoxybenzylamino)-N-(3,3,7-trimethyl-2-oxo-2,3-dihydro-1H-i ndol-5-yl)acetamide) showed very potent activity.
