- Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues
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The interaction between Lymphocyte function-associated antigen 1 (LFA-1) and intercellular-adhesion molecule-1 (ICAM-1) plays important roles in the cell-mediated immune response and inflammation associated with dry eye disease. LFA-1/ICAM-1 antagonists can be used for the treatment of dry eye disease, such as Lifitegrast which has been approved by the FDA in 2016 as a new drug for the treatment of dry eye disease. In this study, we designed and synthesized some new structure compounds that are analogues to Lifitegrast, and their biological activities were evaluated by in vitro cell-based assay and also by in vivo mouse dry eye model. Our results demonstrated that one of these analogues of Lifitegrast (compound 1b) showed good LFA-1/ICAM-1 antagonist activity in in vitro assay; meanwhile, it also significantly reduced ocular surface epithelial cells damage, increased goblet cell density in dry eye mouse and highly improved the symptoms of dry eye mouse. [Figure not available: see fulltext.]
- An, Yuanlong,Du, Guoxin,Du, Weiwei,Gong, Qi,Hao, Feifei,He, Wei,He, Xiangdong,Jiang, Hualiang,Tong, Xiaochu,Wang, Minnan,Zhang, Donglei,Zheng, Mingyue
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- THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
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Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
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Paragraph 0464-0465
(2019/02/13)
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- CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
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The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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Page/Page column
(2013/06/04)
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- CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
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The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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Page/Page column 217
(2013/06/05)
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- Design, synthesis, and biological activities of novel 2-cyanoacrylates containing oxazole, oxadiazole, or quinoline moieties
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A series of novel 2-cyanoacrylates containing an oxazole, oxadiazole, or quinoline moiety were designed and synthesized, and their structures were characterized by 1H NMR and elemental analysis (or high-resolution mass spectrometry). Their herbicidal activities against four weeds were evaluated, and the result indicated that some of the title compounds showed excellent herbicidal activities against rape and amaranth pigweed in postemergence treatment at a dose of 375 g/ha. Furthermore, most of these cyanoacrylates exhibited interesting plant growth regulatory activities.
- Zhao, Qiqi,Liu, Shaohua,Li, Yonghong,Wang, Qingmin
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experimental part
p. 2849 - 2855
(2010/04/30)
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- NITROGEN-CONTAINING HETEROCYCLYL KETONES AND METHODS OF USE
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Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 168-169
(2008/12/08)
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- Bicyclomycin fluorescent probes: Synthesis and biochemical, biophysical, and biological properties
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Bicyclomycin (1) is a commercially available antibiotic whose primary site of action in Escherichia coli is the transcription termination factor rho. Key aspects of the 1·rho interaction - Kd, stoichiometry for 1·rho binding, and whether 1 and
- Brogan, Andrew P.,Widger, William R.,Kohn, Harold
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p. 5575 - 5587
(2007/10/03)
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