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A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma.
Long DD, Frieman B, Hegde SS, Hill CM, Jiang L, Kintz S, Marquess DG, Purkey H, Shaw JP, Steinfeld T, Wilson MS, Wrench K. Long DD, et al. Among authors: steinfeld t. Bioorg Med Chem Lett. 2013 Feb 15;23(4):939-43. doi: 10.1016/j.bmcl.2012.12.058. Epub 2012 Dec 22. Bioorg Med Chem Lett. 2013. PMID: 23317571
Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and β₂ agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Hughes AD, Chen Y, Hegde SS, Jasper JR, Jaw-Tsai S, Lee TW, McNamara A, Pulido-Rios MT, Steinfeld T, Mammen M. Hughes AD, et al. Among authors: steinfeld t. J Med Chem. 2015 Mar 26;58(6):2609-22. doi: 10.1021/jm501915g. Epub 2015 Feb 9. J Med Chem. 2015. PMID: 25629394
In vivo pharmacodynamic assays for M2 and M3 muscarinic receptors.
Armstrong S, Steinfeld T, Pulido-Rios MT, Hegde SS. Armstrong S, et al. Among authors: steinfeld t. Curr Protoc Pharmacol. 2010 Mar;Chapter 12:Unit 12.13. doi: 10.1002/0471141755.ph1213s48. Curr Protoc Pharmacol. 2010. PMID: 22294364
18 results