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Page 1
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM. Backes BJ, et al. Among authors: longenecker k. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. doi: 10.1016/j.bmcl.2007.01.026. Epub 2007 Jan 19. Bioorg Med Chem Lett. 2007. PMID: 17276063
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: longenecker k. J Med Chem. 2006 Jun 15;49(12):3520-35. doi: 10.1021/jm051283e. J Med Chem. 2006. PMID: 16759095
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: longenecker k. J Med Chem. 2006 Nov 2;49(22):6439-42. doi: 10.1021/jm060955d. J Med Chem. 2006. PMID: 17064063
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: longenecker k. J Med Chem. 2007 Apr 19;50(8):1983-7. doi: 10.1021/jm061436d. Epub 2007 Mar 17. J Med Chem. 2007. PMID: 17367123
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.
Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW. Kurukulasuriya R, et al. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. doi: 10.1016/j.bmcl.2006.09.024. Epub 2006 Sep 28. Bioorg Med Chem Lett. 2006. PMID: 17010607
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM. Madar DJ, et al. Among authors: longenecker kl. J Med Chem. 2006 Oct 19;49(21):6416-20. doi: 10.1021/jm060777o. J Med Chem. 2006. PMID: 17034148
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
Patel JR, Shuai Q, Dinges J, Winn M, Pliushchev M, Fung S, Monzon K, Chiou W, Wang J, Pan L, Wagaw S, Engstrom K, Kerdesky FA, Longenecker K, Judge R, Qin W, Imade HM, Stolarik D, Beno DW, Brune M, Chovan LE, Sham HL, Jacobson P, Link JT. Patel JR, et al. Among authors: longenecker k. Bioorg Med Chem Lett. 2007 Feb 1;17(3):750-5. doi: 10.1016/j.bmcl.2006.10.074. Epub 2006 Oct 28. Bioorg Med Chem Lett. 2007. PMID: 17110106
Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif.
Krueger AC, Randolph JT, DeGoey DA, Donner PL, Flentge CA, Hutchinson DK, Liu D, Motter CE, Rockway TW, Wagner R, Beno DW, Koev G, Lim HB, Beyer JM, Mondal R, Liu Y, Kati WM, Longenecker KL, Molla A, Stewart KD, Maring CJ. Krueger AC, et al. Among authors: longenecker kl. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3487-90. doi: 10.1016/j.bmcl.2013.04.057. Epub 2013 May 1. Bioorg Med Chem Lett. 2013. PMID: 23664214
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
Sorensen B, Winn M, Rohde J, Shuai Q, Wang J, Fung S, Monzon K, Chiou W, Stolarik D, Imade H, Pan L, Deng X, Chovan L, Longenecker K, Judge R, Qin W, Brune M, Camp H, Frevert EU, Jacobson P, Link JT. Sorensen B, et al. Among authors: longenecker k. Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. doi: 10.1016/j.bmcl.2006.10.008. Epub 2006 Oct 7. Bioorg Med Chem Lett. 2007. PMID: 17070044
56 results