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Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase.
Stafford JA, Veal JM, Feldman PL, Valvano NL, Baer PG, Brackeen MF, Brawley ES, Connolly KM, Domanico PL, Han B, et al. Stafford JA, et al. Among authors: feldman pl. J Med Chem. 1995 Dec 22;38(26):4972-5. doi: 10.1021/jm00026a003. J Med Chem. 1995. PMID: 8544172 No abstract available.
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. Among authors: feldman pl. 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
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
35 results