63279-36-7Relevant articles and documents
Palladium-catalyzed cross-coupling reactions on a bromo-naphthalene scaffold in the search for novel human CC chemokine receptor 8 (CCR8) antagonists
Verhaegen, Yenthel,Liu, Libao,Nguyen, Tien T.,Van Loy, Tom,Voet, Arnout R.D.,Schols, Dominique,Dehaen, Wim,De Jonghe, Steven
, (2021)
The naphthalene sulfonamide scaffold is known to possess CCR8 antagonistic properties. In order to expand the structure–activity relationship study of this compound class, a variety of palladium-catalyzed cross-coupling reactions was performed on a bromo-
From hit to lead: Structure-based discovery of naphthalene-1-sulfonamide derivatives as potent and selective inhibitors of fatty acid binding protein 4
Gao, Ding-Ding,Dou, Hui-Xia,Su, Hai-Xia,Zhang, Ming-Ming,Wang, Ting,Liu, Qiu-Feng,Cai, Hai-Yan,Ding, Hai-Peng,Yang, Zhuo,Zhu, Wei-Liang,Xu, Ye-Chun,Wang, He-Yao,Li, Ying-Xia
, p. 44 - 59 (2018/05/24)
Fatty acid binding protein 4 (FABP4) plays a critical role in metabolism and inflammatory processes and therefore is a potential therapeutic target for immunometabolic diseases such as diabetes and atherosclerosis. Herein, we reported the identification of naphthalene-1-sulfonamide derivatives as novel, potent and selective FABP4 inhibitors by applying a structure-based design strategy. The binding affinities of compounds 16dk, 16do and 16du to FABP4, at the molecular level, are equivalent to or even better than that of BMS309403. The X-ray crystallography complemented by the isothermal titration calorimetry studies revealed the binding mode of this series of inhibitors and the pivotal network of ordered water molecules in the binding pocket of FABP4. Moreover, compounds 16dk and 16do showed good metabolic stabilities in liver microsomes. Further extensive in vivo study demonstrated that 16dk and 16do exhibited a dramatic improvement in glucose and lipid metabolism, by decreasing fasting blood glucose and serum lipid levels, enhancing insulin sensitivity, and ameliorating hepatic steatosis in obese diabetic (db/db) mice.
Naphthalenesulfonamide type compound, preparation method of naphthalenesulfonamide type compound and application of naphthalenesulfonamide type compound to adjustment of plant growth activity
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Paragraph 0057; 0058; 0059, (2017/08/28)
The invention discloses a naphthalenesulfonamide type compound, a preparation method of the naphthalenesulfonamide type compound and the application of the naphthalenesulfonamide type compound to adjustment of plant growth activity. The structure general formula of the naphthalenesulfonamide type compound is shown as the formula I. Please see the formula I in the specifications. The naphthalenesulfonamide type compound is simple in structure and has the excellent function of adjusting the plant growth activity, the preparation method of the naphthalenesulfonamide type compound is simple and practicable, and mass production is facilitated.