92878-94-9Relevant academic research and scientific papers
1-[2-(2-methoxy-5-nitro-phenoxy)]-ethyl 3-methylimidazole salt and preparation method thereof
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Paragraph 0022-0024, (2020/01/25)
The invention belongs to the technical field of agrochemistry, and relates to a novel plant growth regulator 1-[2-(2-methoxy-5-nitro-phenoxy)]-ethyl 3-methylimidazole salt compound, a preparation method and use thereof. The structure of the compound is sh
N-[2-(2-methoxy-5-nitro-phenoxy) ethyl] pyridine halide and preparation method and application thereof
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Paragraph 0032-0034, (2020/02/14)
The invention belongs to the technical field of agrochemistry, and relates to a novel plant growth regulator N-[2-(2-methoxy-5-nitro-phenoxy) ethyl] pyridine halide compound and a preparation method and application thereof. The structure of the compound i
2-(2-methoxy-5-nitro-phenoxy)ethyltriethylammonium halide, preparation method and application thereof
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Paragraph 0023-0024, (2020/04/17)
Belonging to the technical field of agrochemistry, the invention relates to a novel plant growth regulator 2-(2-methoxy-5-nitro-phenoxy)ethyltriethylammonium halide, a preparation method and application thereof. The structure of the compound is shown as t
Structure-activity relationship investigation of Phe-Arg mimetic region of human glutaminyl cyclase inhibitors
Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Van Manh, Nguyen,Ann, Jihyae,Kim, Eunhye,Cui, Minghua,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo
, p. 3133 - 3144 (2018/05/23)
Glutamyl cyclase (QC) is a promising therapeutic target because of its involvement in the pathogenesis of Alzheimer's disease. In this study, we developed novel QC inhibitors that contain 3-aminoalkyloxy-4-methoxyphenyl and 4-aminoalkyloxyphenyl groups to replace the previously developed pharmacophore. Several potent inhibitors were identified, showing IC50 values in a low nanomolar range, and were further studied for in vitro toxicity and in vivo activity. Among these, inhibitors 51 and 53 displayed the most potent AβN3pE?40-lowering effects in in vivo acute model with reasonable BBB penetration, without showing cytotoxicity and hERG inhibition. The molecular modeling analysis of 53 indicated that the salt bridge interaction and the hydrogen bonding in the active site provided a high potency. Given the potent activity and favorable BBB penetration with low cytotoxicity, we believe that compound 53 may serve as a potential candidate for anti-Alzheimer's agents.
