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Items: 1 to 20 of 96

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. doi: 10.1016/j.bmcl.2012.02.075. Epub 2012 Mar 1.

PMID:
22444683
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. doi: 10.1016/j.bmcl.2012.02.077. Epub 2012 Mar 1.

PMID:
22444685
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 1;21(5):1299-305. doi: 10.1016/j.bmcl.2011.01.090. Epub 2011 Jan 26.

PMID:
21315588
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 1;23(23):6228-33. doi: 10.1016/j.bmcl.2013.09.094. Epub 2013 Oct 8.

PMID:
24157366
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. doi: 10.1016/j.bmcl.2011.12.064. Epub 2011 Dec 24.

PMID:
22248857
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. doi: 10.1016/j.bmcl.2012.01.002. Epub 2012 Jan 10.

PMID:
22264488
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. doi: 10.1016/j.bmcl.2011.12.098. Epub 2012 Jan 8.

PMID:
22290078
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 1;22(1):658-65. doi: 10.1016/j.bmcl.2011.10.060. Epub 2011 Oct 24.

PMID:
22079761
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. doi: 10.1021/jm101013m.

PMID:
20857914
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. doi: 10.1016/j.bmc.2013.10.023. Epub 2013 Oct 28.

PMID:
24211162
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 1;24(7):1657-60. doi: 10.1016/j.bmcl.2014.02.070. Epub 2014 Mar 6.

PMID:
24636945
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 1;21(23):7205-9. doi: 10.1016/j.bmcl.2011.09.039. Epub 2011 Sep 22.

PMID:
22001092
13.

Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG.

J Med Chem. 2000 Feb 24;43(4):721-35.

PMID:
10691697
14.

Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.

Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3383-6.

PMID:
12419366
15.

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. doi: 10.1016/j.bmc.2012.03.052. Epub 2012 Apr 1.

PMID:
22512907
16.

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. doi: 10.1016/j.bmcl.2011.12.002. Epub 2011 Dec 8.

PMID:
22209206
17.

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. doi: 10.1016/j.bmcl.2010.04.069. Epub 2010 Apr 21.

PMID:
20471253
18.

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 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.

PMID:
22018461
19.

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 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11.

PMID:
21282055
20.

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 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10.

PMID:
20363126
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