- Discovery of a Potent Botulinum Neurotoxin A Inhibitor ZM299 with Effective Protections in Botulism Mice
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Botulinum neurotoxins serotype A (BoNT/A) is the deadliest toxins known to humans and the "Category A" agent for bioterrorism. Over the past 20 years, significant efforts have been put forth to develop effective inhibitors of BoNT/A. Unfortunately, few id
- Gao, Jie,He, Zhili,Hong, Zhanying,Li, Tao,Luo, Deyan,Miao, Zhenyuan,Ning, Nianzhi,Wang, Hui,Wang, Jianxin,Wu, Yuelin,Xv, Xiguo,Zhang, Wannian,Zhang, Yanming,Zhuang, Chunlin
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p. 357 - 364
(2021/12/24)
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- MERCAPTONICOTINIC ACID COMPOUND AND PREPARATION METHOD AND USE THEREOF
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The present invention discloses a class of mercaptonicotinic acid compound and preparation method and use thereof; the general structural formula of the compound is as shown in Formula I. Experiment demonstrates that the mercaptonicotinic acid compound co
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Paragraph 0166-0170
(2016/04/19)
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- BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
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- Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase
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Cyclooxygenase-1/2 (COX-1/2) and 5-lipoxygenase (5-LOX) are enzymes in two different pathways in the inflammatory process. In the present study, a variety of new nimesulide derivatives were synthesized through incorporation of a 5-LOX pharmacophore into nimesulide followed with some structural modifications, which were then characterized for dual enzyme inhibitors for these two types of enzymes. Their structure-activity relationships (SARs) were studied, and compound 20f was found to be an excellent dual enzyme inhibitor. Its binding conformation and interaction mode were studied with molecular docking experiments. Compound 20f could become a lead compound for further development for potential anti-inflammatory drugs.
- Li, Yue,Chen, Shu-Han,Ou, Tian-Miao,Tan, Jia-Heng,Li, Ding,Gu, Lian-Quan,Huang, Zhi-Shu
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p. 2074 - 2083
(2011/05/05)
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- HETEROCYCLYL COMPOUNDS
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a , R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharm
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Page/Page column 31-32
(2010/02/11)
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