22958-64-1Relevant academic research and scientific papers
Synthesis of a Potent Pan-Serotype Dengue Virus Inhibitor Having a Tetrahydrothienopyridine Core
Hung, Kevin,Liu, Yugang,Simon, Oliver,Zhang, Lei,Lu, Peichao,Yeung, Bryan K. S.,Sarko, Christopher,Yokokawa, Fumiaki
, (2020)
A synthesis of the first-in-class pan-serotype dengue virus inhibitor NITD-688 is presented. The Gewald reaction of N-(tert-butoxycarbonyl)-6,6-dimethylpiperidin-3-one with malononitrile and sulfur in the presence of l-proline as a catalyst gave tert-buty
BIARYL COMPOUND, PREPARATION METHOD AND USE THEREFOR
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Paragraph 0110; 0115, (2020/01/02)
The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases.
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors
Kim, Kyung Ju,Choi, Min Ji,Shin, Ji-Sun,Kim, Minju,Choi, Hye-Eun,Kang, Seoung Mook,Jin, Jae Ho,Lee, Kyung-Tae,Lee, Jae Yeol
, p. 1958 - 1962 (2014/04/17)
As a continuous research for discovery of new COX-2 inhibitors, we present the simple chemical synthesis, in vitro biological screening, and molecular docking study of 1H-pyrrole-2,5-dione derivatives. New synthetic compounds were evaluated for the inhibitory activities on LPS-induced PGE2 production in RAW 264.7 macrophage cells as well as the COX-1 and COX-2 inhibitory potency. Among them, compound 9d (MPO-0029) was identified as more potent and selective COX-2 inhibitor [PGE2 IC50 = 8.7 nM, COX-2 IC50 = 6.0 nM; COX-2 selectivity index (SI) = >168] than celecoxib. Molecular docking experiments were further performed against COX-2 and COX-1 isozymes to determine their probable binding models. Results of molecular docking studies revealed that compound 9d (MPO-0029) has stronger binding interaction with COX-2 than with COX-1 isozyme, and provided successfully complementary theoretical support for the obtained experimental biological data.
USE OF PIPERIDINE DERIVATIVES AS AGONISTS OF CHEMOKINE RECEPTOR ACTIVITY
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Page/Page column 92, (2009/03/07)
The present invention is directed to novel piperidinc derivatives and to the use of piperidine derivatives of formula (I) as agonists of chemokine receptor activity.
