1030419-85-2Relevant academic research and scientific papers
One-pot Synthesis of Benzo[4,5]imidazo[1,2-a]pyridine Derivatives in Aqueous Conditions
Vodolazhenko, Maria A.,Mykhailenko, Anastasiia E.,Gorobets, Nikolay Yu.,Desenko, Sergey M.
, p. 753 - 757 (2017)
One-pot reaction of cyclic 1,3-diketones, dimethylformamide dimethylacetal (DMFDMA) and 2-(1H-benzo[d]imidaz-2-yl)acetonitrile was found to be a highly selective process leading to 4-oxo-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]quinolin-6-yl cyanides. Op
Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein
Chen, Kaixian,Chen, Zhifeng,Dang, Yongjun,Ding, Hong,Fan, Shijie,Hu, Junchi,Jiang, Hualiang,Li, Lianchun,Li, Quanfu,Lin, Tingting,Lu, Junyan,Luo, Cheng,Otomo, Chinatsu,Otomo, Takanori,Tan, Minjia,Tao, Hongru,Wan, Wei,Wen, Yi,Xie, Yuli,Xu, Pan,Yao, Zhiyi,Yue, Liyan,Zhang, Bidong,Zhang, Naixia,Zhang, Yuanyuan,Zhou, Bing,Zhu, Mingrui
, p. 26105 - 26114 (2021/11/09)
The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins, including autophagy receptors, which stands out as a promising protein–protein interaction (PPI) target for the intervention of autophagy. Post-translational modifications like acetylation of Lys49 on the LIR-interacting surface could disrupt the interaction, offering an opportunity to design covalent small molecules interfering with the interface. Through screening covalent compounds, we discovered a small molecule modulator of LC3A/B that covalently modifies LC3A/B protein at Lys49. Activity-based protein profiling (ABPP) based evaluations reveal that a derivative molecule DC-LC3in-D5 exhibits a potent covalent reactivity and selectivity to LC3A/B in HeLa cells. DC-LC3in-D5 compromises LC3B lipidation in vitro and in HeLa cells, leading to deficiency in the formation of autophagic structures and autophagic substrate degradation. DC-LC3in-D5 could serve as a powerful tool for autophagy research as well as for therapeutic interventions.
Tetrahydroquinazoline derivatives and pharmaceutical composition for preventing or treating psoriasis comprising the same
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Paragraph 0251-0252; 0261-0262, (2020/11/06)
The present invention relates to a tetrahydroquinazoline derivative and a pharmaceutical composition for preventing or treating psoriasis containing the same as an active ingredient. The compound provided in one aspect of the present invention has an effe
Synthesis of novel 3-(1,3-thiazol-2-yl)-7,8-dihydroquinoline-2,5(1H,6H)- diones
Dzhavakhishvili,Gorobets,Chernenko,Musatov,Desenko
experimental part, p. 422 - 427 (2009/06/05)
An efficient method for the synthesis of novel 3-(1,3-thiazol-2-yl)-7,8- dihydroquinoline-2,5(1H,6H)-diones from various 2- dimethylaminomethylidenecyclohexane-1,3-diones, (1,3-thiazol-2-yl)acetonitriles, and dimethylformamide dimethyl acetal was developed. These transformations proceeded through intermediate 2-[2-(4-aryl-1,3-thiazol-2-yl)-2-cyanoethenyl]-3- oxocyclohex-1-en-1-olates. They were isolated as piperidinium salts and used in further heterocyclization reactions with aromatic amines, giving novel 1-aryl-3-(1,3-thiazol-2-yl)-7,8-dihydroquinoline-2,5(1H,6H)-diones. These compounds were also obtained by preparative three-step "one pot" synthesis under controlled microwave irradiation.
