64826-45-5Relevant academic research and scientific papers
INHIBITORS OF ENL/AF9 YEATS
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, (2021/06/26)
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease
Mo, Jun,Chen, Tingkai,Yang, Hongyu,Guo, Yan,Li, Qi,Qiao, Yuting,Lin, Hongzhi,Feng, Feng,Liu, Wenyuan,Chen, Yao,Liu, Zongliang,Sun, Haopeng
, p. 330 - 343 (2019/12/30)
Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer’s disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50 values (15b, eeAChE IC50 = 0.39 ± 0.11 μM; 15j, eqBChE IC50 = 0.16 ± 0.04 μM) towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Kinetic and molecular modelling studies revealed that 15b and 15j act in a competitive manner. 15b and 15j showed neuroprotective effect against H2O2-induced oxidative damage on PC12 cells. This effect was further supported by their antioxidant activity determined in a DPPH assay in vitro. Morris water maze test confirmed the memory amelioration effect of the two compounds in a scopolamine-induced mouse model. Moreover, the hepatotoxicity of 15b and 15j was lower than tacrine. In summary, these data suggest 15b and 15j are promising multifunctional agents against AD.
Benzylpiperidine-benzimidazole derivative or pharmaceutically acceptable salt thereof, and preparation method and application thereof
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Paragraph 0049; 0055; 0060-0061, (2020/02/29)
The invention discloses a benzylpiperidine-benzimidazole derivative with a structure as shown in a general formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The derivative disclosed by the invention has good cholinesterase inhibition activity, can be used for preparing cholinesterase inhibitors, and is of important significance to treatment of neurodegenerative diseases.
Benzimidazolone p38 inhibitors
Dombroski, Mark A.,Letavic, Michael A.,McClure, Kim F.,Barberia, John T.,Carty, Thomas J.,Cortina, Santo R.,Csiki, Csilla,Dipesa, Alan J.,Elliott, Nancy C.,Gabel, Christopher A.,Jordan, Crystal K.,Labasi, Jeff M.,Martin, William H.,Peese, Kevin M.,Stock, Ingrid A.,Svensson, Linne,Sweeney, Francis J.,Yu, Chul H.
, p. 919 - 923 (2007/10/03)
The synthesis and in vitro p38α activity of a novel series of benzimidazolone inhibitors is described. The p38α SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38α in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors. Potent p38α activity comparable to that of several previously reported p38 inhibitors is observed for this novel chemotype.
