- Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis
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Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a
- Du, Fangyu,Sun, Wenjiao,Morisseau, Christophe,Hammock, Bruce D.,Bao, Xuefei,Liu, Qiu,Wang, Chao,Zhang, Tan,Yang, Hao,Zhou, Jun,Xiao, Wei,Liu, Zhongbo,Chen, Guoliang
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- sEH inhibitor and preparation method and application thereof
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The invention provides an sEH inhibitor and a preparation method and application thereof, and relates to the technical field of endogenous active substance regulation and control. The sEH inhibitor provided by the invention has a structure as shown in a f
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Paragraph 0234; 0236; 0241-0242
(2020/07/28)
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- Nitro reduction-based fluorescent probes for carbon monoxide require reactivity involving a ruthenium carbonyl moiety
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Recently, several arylnitro-based fluorescent CO probes have been reported. The design was based on CO's ability to reduce an arylnitro group for fluorescence turn-on. In this work, we assessed the response of three published arylnitro-based fluorescent C
- Yuan, Zhengnan,Yang, Xiaoxiao,De La Cruz, Ladie Kimberly,Wang, Binghe
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supporting information
p. 2190 - 2193
(2020/02/27)
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- Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus
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The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.
- Xie, Hui,Ng, Danny,Savinov, Sergey N.,Dey, Barna,Kwong, Peter D.,Wyatt, Richard,Smith III, Amos B.,Hendrickson, Wayne A.
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p. 4898 - 4908
(2008/03/11)
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- Benzamide therapeutics for the treatment of inflammatory bowel disease
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Benzamides are disclosed to be useful for treating and preventing inflammatory bowel disease.
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- Aminobenzamide compounds for the treatment of neurodegenerative disorders
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A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.
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