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Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.
Wu Y, Aquino CJ, Cowan DJ, Anderson DL, Ambroso JL, Bishop MJ, Boros EE, Chen L, Cunningham A, Dobbins RL, Feldman PL, Harston LT, Kaldor IW, Klein R, Liang X, McIntyre MS, Merrill CL, Patterson KM, Prescott JS, Ray JS, Roller SG, Yao X, Young A, Yuen J, Collins JL. Wu Y, et al. Among authors: feldman pl. J Med Chem. 2013 Jun 27;56(12):5094-114. doi: 10.1021/jm400459m. Epub 2013 Jun 6. J Med Chem. 2013. PMID: 23678871
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.
Tavares FX, Al-Barazanji KA, Bishop MJ, Britt CS, Carlton DL, Cooper JP, Feldman PL, Garrido DM, Goetz AS, Grizzle MK, Hertzog DL, Ignar DM, Lang DG, McIntyre MS, Ott RJ, Peat AJ, Zhou HQ. Tavares FX, et al. Among authors: feldman pl. J Med Chem. 2006 Nov 30;49(24):7108-18. doi: 10.1021/jm060814b. J Med Chem. 2006. PMID: 17125263
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.
Tavares FX, Al-Barazanji KA, Bigham EC, Bishop MJ, Britt CS, Carlton DL, Feldman PL, Goetz AS, Grizzle MK, Guo YC, Handlon AL, Hertzog DL, Ignar DM, Lang DG, Ott RJ, Peat AJ, Zhou HQ. Tavares FX, et al. Among authors: feldman pl. J Med Chem. 2006 Nov 30;49(24):7095-107. doi: 10.1021/jm060572f. J Med Chem. 2006. PMID: 17125262
Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeys.
Boros EE, Samano V, Ray JA, Thompson JB, Jung DK, Kaldor I, Koble CS, Martin MT, Styles VL, Mook RA Jr, Feldman PL, Savarese JJ, Belmont MR, Bigham EC, Boswell GE, Hashim MA, Patel SS, Wisowaty JC, Bowers GD, Moseley CL, Walsh JS, Reese MJ, Rutkowske RD, Sefler AM, Spitzer TD. Boros EE, et al. Among authors: feldman pl. J Med Chem. 2003 Jun 5;46(12):2502-15. doi: 10.1021/jm020574+. J Med Chem. 2003. PMID: 12773054
Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.
Stafford JA, Pacofsky GJ, Cox RF, Cowan JR, Dorsey GF Jr, Gonzales SS, Jung DK, Koszalka GW, McIntyre MS, Tidwell JH, Wiard RP, Feldman PL. Stafford JA, et al. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3215-8. doi: 10.1016/s0960-894x(02)00512-7. Bioorg Med Chem Lett. 2002. PMID: 12372537
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
Pacofsky GJ, Stafford JA, Cox RF, Cowan JR, Dorsey GF Jr, Gonzales SS, Kaldor I, Koszalka GW, Lovell GG, McIntyre MS, Tidwell JH, Todd D, Whitesell G, Wiard RP, Feldman PL. Pacofsky GJ, et al. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3219-22. doi: 10.1016/s0960-894x(02)00513-9. Bioorg Med Chem Lett. 2002. PMID: 12372538
The formation of a covalent complex between a dipeptide ligand and the src SH2 domain.
Alligood KJ, Charifson PS, Crosby R, Consler TG, Feldman PL, Gampe RT Jr, Gilmer TM, Jordan SR, Milstead MW, Mohr C, Peel MR, Rocque W, Rodriguez M, Rusnak DW, Shewchuk LM, Sternbach DD. Alligood KJ, et al. Bioorg Med Chem Lett. 1998 May 19;8(10):1189-94. doi: 10.1016/s0960-894x(98)00195-4. Bioorg Med Chem Lett. 1998. PMID: 9871733
Potent dipeptide inhibitors of the pp60c-src SH2 domain.
Pacofsky GJ, Lackey K, Alligood KJ, Berman J, Charifson PS, Crosby RM, Dorsey GF Jr, Feldman PL, Gilmer TM, Hummel CW, Jordan SR, Mohr C, Shewchuk LM, Sternbach DD, Rodriguez M. Pacofsky GJ, et al. J Med Chem. 1998 May 21;41(11):1894-908. doi: 10.1021/jm970853a. J Med Chem. 1998. PMID: 9599239
Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: new ultra-short-acting nondepolarizing neuromuscular blockers.
Boros EE, Bigham EC, Boswell GE, Mook RA Jr, Patel SS, Savarese JJ, Ray JA, Thompson JB, Hashim MA, Wisowaty JC, Feldman PL, Samano V. Boros EE, et al. J Med Chem. 1999 Jan 28;42(2):206-9. doi: 10.1021/jm980597h. J Med Chem. 1999. PMID: 9925724 No abstract available.
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