316-69-8Relevant academic research and scientific papers
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.
COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
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Paragraph 0347, (2017/09/15)
The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).
Substituted Disulfonamide Compounds
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Page/Page column 49, (2010/06/22)
Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8
Jenkins, Tracy J.,Guan, Bing,Dai, Mingshi,Li, Gang,Lightburn, Thomas E.,Huang, Shan,Freeze, B. Scott,Burdi, Douglas F.,Jacutin-Porte, Swanee,Bennett, Robert,Chen, Weirong,Minor, Charles,Ghosh, Shomir,Blackburn, Christopher,Gigstad, Kenneth M.,Jones, Matthew,Kolbeck, Roland,Yin, Wei,Smith, Sean,Cardillo, Daniel,Ocain, Timothy D.,Harriman, Geraldine C.
, p. 566 - 584 (2008/04/18)
The design, synthesis, and structure-activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are
GLYT1 TRANSPORTER INHIBITORS
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Page/Page column 62-63, (2010/02/12)
The invention provides a compound of formula (I): or a salt, solvate or a physiologically functional derivative thereof, wherein R1 to R10 are as defined in the specification and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
CCR8 INHIBITORS
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Page 158-159, (2008/06/13)
Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I). Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a CCR8 inhibitor represented by Structural Formula (I). Also disclosed is a method of treating inflammatory disorders in a subject by administering a CCR8 inhibitor to the subject.
CCR8 INHIBITORS
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Page 168-169, (2008/06/13)
Disclosed are CCR8 inhibitors represented by Structural Formulas (I). The variables in Structural Formula (I) are described herein. Also disclosed are methods of treating a subject with a CCR8 mediated condition, especially asthma, by administering one of the disclosed CCR8 inhibitors to the subject.
Arylsulfone derivatives
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, (2008/06/13)
The invention provides compounds of the formula and methods of using those compounds for treating a disease or condition in a mammal wherein a 5-HT receptor, such as a 5-HT6 receptor, is implicated and modulation of a 5-HT function is desired,
Bispiperidines as antithrombotic agents
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, (2008/06/13)
Novel compounds which are inhibitors of the binding of fibrinogen to the Gp IIb/IIIa platelet receptors, and which can be used therepeutically as antithrombotic agents
