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Journal Abstract Search


96 related items for PubMed ID: 22444683

  • 1. A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
    Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2811-7. PubMed ID: 22444683
    [Abstract] [Full Text] [Related]

  • 2. A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.
    Graham TH, Liu W, Verras A, Reibarkh M, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xie D, Xu S, Xiao J, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2818-22. PubMed ID: 22444685
    [Abstract] [Full Text] [Related]

  • 3. Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
    Shen HC, Ding FX, Zhou C, Xiong Y, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen D, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL.
    Bioorg Med Chem Lett; 2011 Mar 01; 21(5):1299-305. PubMed ID: 21315588
    [Abstract] [Full Text] [Related]

  • 4. Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
    Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2013 Dec 01; 23(23):6228-33. PubMed ID: 24157366
    [Abstract] [Full Text] [Related]

  • 5. Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
    Wu Z, Yang C, Xiong Y, Feng Z, Lombardo M, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen Q, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1774-8. PubMed ID: 22248857
    [Abstract] [Full Text] [Related]

  • 6. Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
    Shen HC, Ding FX, Jiang J, Verras A, Chabin RM, Xu S, Tong X, Chen Q, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Murphy BA, Gorski JN, Wiltsie J, SinhaRoy R, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1550-6. PubMed ID: 22264488
    [Abstract] [Full Text] [Related]

  • 7. Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
    Wu Z, Yang C, Graham TH, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Shen Z, Chen Q, Bleasby K, Sinharoy R, Hale JJ, Tata JR, Pinto S, Colletti SL, Shen DM.
    Bioorg Med Chem Lett; 2012 Feb 15; 22(4):1727-30. PubMed ID: 22290078
    [Abstract] [Full Text] [Related]

  • 8. The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
    Graham TH, Shen HC, Liu W, Xiong Y, Verras A, Bleasby K, Bhatt UR, Chabin RM, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Lassman ME, Shen Z, Tong X, Tung EC, Xie D, Xu S, Colletti SL, Tata JR, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2012 Jan 01; 22(1):658-65. PubMed ID: 22079761
    [Abstract] [Full Text] [Related]

  • 9. Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.
    Zhou C, Garcia-Calvo M, Pinto S, Lombardo M, Feng Z, Bender K, Pryor KD, Bhatt UR, Chabin RM, Geissler WM, Shen Z, Tong X, Zhang Z, Wong KK, Roy RS, Chapman KT, Yang L, Xiong Y.
    J Med Chem; 2010 Oct 14; 53(19):7251-63. PubMed ID: 20857914
    [Abstract] [Full Text] [Related]

  • 10. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.
    Sun S, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z.
    Bioorg Med Chem; 2013 Dec 15; 21(24):7724-34. PubMed ID: 24211162
    [Abstract] [Full Text] [Related]

  • 11. Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.
    Graham TH, Shu M, Verras A, Chen Q, Garcia-Calvo M, Li X, Lisnock J, Tong X, Tung EC, Wiltsie J, Hale JJ, Pinto S, Shen DM.
    Bioorg Med Chem Lett; 2014 Apr 01; 24(7):1657-60. PubMed ID: 24636945
    [Abstract] [Full Text] [Related]

  • 12. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors.
    Yun W, Ahmad M, Chen Y, Gillespie P, Conde-Knape K, Kazmer S, Li S, Qian Y, Taub R, Wertheimer SJ, Whittard T, Bolin D.
    Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7205-9. PubMed ID: 22001092
    [Abstract] [Full Text] [Related]

  • 13. Prolylcarboxypeptidase (PrCP) inhibitors and the therapeutic uses thereof: a patent review.
    Graham TH.
    Expert Opin Ther Pat; 2017 Oct 01; 27(10):1077-1088. PubMed ID: 28699813
    [Abstract] [Full Text] [Related]

  • 14. Discovery of potent and orally bioavailable 17β-hydroxysteroid dehydrogenase type 3 inhibitors.
    Harada K, Kubo H, Abe J, Haneta M, Conception A, Inoue S, Okada S, Nishioka K.
    Bioorg Med Chem; 2012 May 15; 20(10):3242-54. PubMed ID: 22512907
    [Abstract] [Full Text] [Related]

  • 15. Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
    Lachance N, Gareau Y, Guiral S, Huang Z, Isabel E, Leclerc JP, Léger S, Martins E, Nadeau C, Oballa RM, Ouellet SG, Powell DA, Ramtohul YK, Tranmer GK, Trinh T, Wang H, Zhang L.
    Bioorg Med Chem Lett; 2012 Jan 15; 22(2):980-4. PubMed ID: 22209206
    [Abstract] [Full Text] [Related]

  • 16. Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
    Bosanac T, Hickey ER, Ginn J, Kashem M, Kerr S, Kugler S, Li X, Olague A, Schlyer S, Young ER.
    Bioorg Med Chem Lett; 2010 Jun 15; 20(12):3746-9. PubMed ID: 20471253
    [Abstract] [Full Text] [Related]

  • 17. Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
    Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.
    Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7006-12. PubMed ID: 22018461
    [Abstract] [Full Text] [Related]

  • 18. Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
    Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV.
    Bioorg Med Chem Lett; 2011 Mar 01; 21(5):1425-8. PubMed ID: 21282055
    [Abstract] [Full Text] [Related]

  • 19. The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
    Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P.
    Bioorg Med Chem Lett; 2010 May 01; 20(9):2897-902. PubMed ID: 20363126
    [Abstract] [Full Text] [Related]

  • 20. Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series.
    Lethu S, Ginisty M, Bosc D, Dubois J.
    J Med Chem; 2009 Oct 22; 52(20):6205-8. PubMed ID: 19772293
    [Abstract] [Full Text] [Related]


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