948859-96-9Relevant academic research and scientific papers
Preparation, thermal analyses and biological activities of Co(II) and Cr(III) complexes with 2-acetylpyridine-6-bromo-2-naphthoyl acylhydrazone
Zong, Xin-jie,Liu, Xiang-rong,Zhao, Shun-sheng,Yang, Zai-wen
, p. 303 - 311 (2019)
Novel six-coordinated octahedral Co(II) complex [C36H26Br2CoN7O5, 1] and Cr(III) complex [C36H26Br2CrN6O2, 2] were prepared by the chelation reac
Naphthalene-ring have single crystal structure of the metal complex of the hydrazone synthetic method and application (by machine translation)
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Paragraph 0048-0059, (2019/02/10)
The present invention relates to naphthalene-ring hydrazone metal complex synthetic method and application, the naphthalene ring-containing hydrazone metal complexes of the structural formula is: In the formula: M is Cr or Co, the naphthalene ring-contai
Discovery and mechanism study of SIRT1 activators that promote the deacetylation of fluorophore-labeled substrate
Wu, Jiahui,Zhang, Dengyou,Chen, Lei,Li, Jianneng,Wang, Jianling,Ning, Chengqing,Yu, Niefang,Zhao, Fei,Chen, Dongying,Chen, Xiaoyan,Chen, Kaixian,Jiang, Hualiang,Liu, Hong,Liu, Dongxiang
, p. 761 - 780 (2013/04/10)
SIRT1 is an NAD+-dependent deacetylase, whose activators have potential therapeutic applications in age-related diseases. Here we report a new class of SIRT1 activators. The activation is dependent on the fluorophore labeled to the substrate. To elucidate the activation mechanism, we solved the crystal structure of SIRT3/ac-RHKKac-AMC complex. The structure revealed that the fluorophore blocked the H-bond formation and created a cavity between the substrate and the Rossmann fold. We built the SIRT1/ac-RHKK ac-AMC complex model based on the crystal structure. Km and Kd determinations demonstrated that the fluorophore decreased the peptide binding affinity. The binding modes of SIRT1 activators indicated that a portion of the activators interacts with the fluorophore through π-stacking, while the other portion inserts into the cavity or interacts with the Rossmann fold, thus increasing the substrate affinity. Our study provides new insights into the mechanism of SIRT1 activation and may aid the design of novel SIRT1 activators.
Discovering potent inhibitors against the β-hydroxyacyl-acyl carrier protein dehydratase (FabZ) of helicobacter pylori: Structure-based design, synthesis, bioassay, and crystal structure determination
He, Lingyan,Zhang, Liang,Liu, Xiaofeng,Li, Xianghua,Zheng, Mingyue,Li, HongLin,Yu, Kunqian,Chen, Kaixian,Shen, Xu,Jiang, Hualiang,Liu, Hong
experimental part, p. 2465 - 2481 (2010/03/03)
The discovery of HpFabZ inhibitors is now of special interest in the treatment of various gastric diseases. In this work, three series of derivatives (compounds 3, 4, and 5) were designed, synthesized, and their biological activities were investigated as potential HpFabZ inhibitors in a two phased manner. First, we designed and synthesized two series of derivatives (3a-r and 4a-u) and evaluated the enzyme-based assay against HpFabZ. Five compounds (3i-k, 3m, and 3q) showed potential inhibitory activity, with IC50 values less than 2 μM. Second, a focused combinatorial library containing 280 molecules was designed employing the LD1.0 program. Twelve compounds (5a-l) were selected and synthesized. The activity of the most potent compound 5h (IC 50) 0.86 μM) was 46 times higher than that of the hit 1. The high hit rate and the potency of the new HpFabZ inhibitors demonstrated the efficiency of the strategy for the focused library design and virtual screening.
NOVEL ANTHRACENE DERIVATIVE AND ORGANIC ELECTRONIC DEVICE USING THE SAME
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Page/Page column 38, (2010/11/28)
The present invention provides a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, drive voltage, and life time.
