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Page 1
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: conn el. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Mylari BL, Armento SJ, Beebe DA, Conn EL, Coutcher JB, Dina MS, O'Gorman MT, Linhares MC, Martin WH, Oates PJ, Tess DA, Withbroe GJ, Zembrowski WJ. Mylari BL, et al. Among authors: conn el. J Med Chem. 2003 Jun 5;46(12):2283-6. doi: 10.1021/jm034065z. J Med Chem. 2003. PMID: 12773033
Design and synthesis of a novel family of triazine-based inhibitors of sorbitol dehydrogenase with oral activity: 1-[4-[3R,5S-dimethyl-4-(4-methyl-[1,3,5]triazin-2-yl)-piperazin-1-yl]-[1,3,5]triazin-2-yl]-(R) ethanol.
Mylari BL, Withbroe GJ, Beebe DA, Brackett NS, Conn EL, Coutcher JB, Oates PJ, Zembrowski WJ. Mylari BL, et al. Among authors: conn el. Bioorg Med Chem. 2003 Sep 15;11(19):4179-88. doi: 10.1016/s0968-0896(03)00490-5. Bioorg Med Chem. 2003. PMID: 12951149
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Mylari BL, Armento SJ, Beebe DA, Conn EL, Coutcher JB, Dina MS, O'Gorman MT, Linhares MC, Martin WH, Oates PJ, Tess DA, Withbroe GJ, Zembrowski WJ. Mylari BL, et al. Among authors: conn el. J Med Chem. 2005 Oct 6;48(20):6326-39. doi: 10.1021/jm050462t. J Med Chem. 2005. PMID: 16190759
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK, Piotrowski DW, Balan G, Bechle BM, Conn EL, Dirico KJ, Oliver RM, Soeller WC, Southers JA, Yang X. Humphries PS, et al. Among authors: conn el. Bioorg Med Chem Lett. 2009 May 1;19(9):2400-3. doi: 10.1016/j.bmcl.2009.03.082. Epub 2009 Mar 25. Bioorg Med Chem Lett. 2009. PMID: 19346127
Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.
Boehm M, Hepworth D, Loria PM, Norquay LD, Filipski KJ, Chin JE, Cameron KO, Brenner M, Bonnette P, Cabral S, Conn E, Ebner DC, Gautreau D, Hadcock J, Lee EC, Mathiowetz AM, Morin M, Rogers L, Smith A, VanVolkenburg M, Carpino PA. Boehm M, et al. ACS Med Chem Lett. 2013 Sep 16;4(11):1079-84. doi: 10.1021/ml400275z. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900608 Free PMC article.
Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.
Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG. Calabrese MF, et al. Among authors: conn el. Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24. Structure. 2014. PMID: 25066137 Free article.
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS. Ruggeri RB, et al. Among authors: conn el. J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28. J Med Chem. 2015. PMID: 26509551
18 results