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Page 1
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Nirschl AA, Zou Y, Krystek SR Jr, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG. Nirschl AA, et al. Among authors: simpkins lm. J Med Chem. 2009 May 14;52(9):2794-8. doi: 10.1021/jm801583j. J Med Chem. 2009. PMID: 19351168
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG. Magnin DR, et al. Among authors: simpkins lm. J Med Chem. 2004 May 6;47(10):2587-98. doi: 10.1021/jm049924d. J Med Chem. 2004. PMID: 15115400
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Wang H, Ruan Z, Li JJ, Simpkins LM, Smirk RA, Wu SC, Hutchins RD, Nirschl DS, Van Kirk K, Cooper CB, Sutton JC, Ma Z, Golla R, Seethala R, Salyan ME, Nayeem A, Krystek SR Jr, Sheriff S, Camac DM, Morin PE, Carpenter B, Robl JA, Zahler R, Gordon DA, Hamann LG. Wang H, et al. Among authors: simpkins lm. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3168-72. doi: 10.1016/j.bmcl.2008.04.069. Epub 2008 May 1. Bioorg Med Chem Lett. 2008. PMID: 18485702
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: simpkins lm. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG. Simpkins LM, et al. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. doi: 10.1016/j.bmcl.2007.09.090. Epub 2007 Oct 1. Bioorg Med Chem Lett. 2007. PMID: 17937986
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG. Zhao G, et al. Among authors: simpkins lm. Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5. doi: 10.1016/j.bmcl.2005.06.043. Bioorg Med Chem Lett. 2005. PMID: 16046120
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.
O'Connor SP, Wang Y, Simpkins LM, Brigance RP, Meng W, Wang A, Kirby MS, Weigelt CA, Hamann LG. O'Connor SP, et al. Among authors: simpkins lm. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6273-6. doi: 10.1016/j.bmcl.2010.08.090. Epub 2010 Aug 22. Bioorg Med Chem Lett. 2010. PMID: 20833042
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R, Harrity T, Stoffel R, Taylor DS, Lavoie TB, Kish K, Jacobson BL, Sheriff S, Adam LP, Ewing WR, Robl JA. Sulsky R, et al. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. doi: 10.1016/j.bmcl.2006.12.044. Epub 2006 Dec 21. Bioorg Med Chem Lett. 2007. PMID: 17502136
17 results