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Items: 1 to 20 of 179

1.

Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11β-hydroxysteroid dehydrogenase type I.

Valeur E, Christmann-Franck S, Lepifre F, Carniato D, Cravo D, Charon C, Bozec S, Musil D, Hillertz P, Doare L, Schmidlin F, Lecomte M, Schultz M, Roche D.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5909-14. doi: 10.1016/j.bmcl.2012.07.070. Epub 2012 Jul 31.

PMID:
22901389
2.

Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Roche D, Carniato D, Leriche C, Lepifre F, Christmann-Franck S, Graedler U, Charon C, Bozec S, Doare L, Schmidlin F, Lecomte M, Valeur E.

Bioorg Med Chem Lett. 2009 May 15;19(10):2674-8. doi: 10.1016/j.bmcl.2009.03.140. Epub 2009 Apr 1.

PMID:
19395260
3.

Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.

Lepifre F, Christmann-Franck S, Roche D, Leriche C, Carniato D, Charon C, Bozec S, Doare L, Schmidlin F, Lecomte M, Valeur E.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3682-5. doi: 10.1016/j.bmcl.2009.02.123. Epub 2009 Mar 5.

PMID:
19450980
4.

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
5.

Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).

Sun D, Wang Z, Di Y, Jaen JC, Labelle M, Ma J, Miao S, Sudom A, Tang L, Tomooka CS, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3513-6. doi: 10.1016/j.bmcl.2008.05.025. Epub 2008 May 10.

PMID:
18511278
6.

Potent and novel 11β-HSD1 inhibitors identified from shape and docking based virtual screening.

Xia G, Xue M, Liu L, Yu J, Liu H, Li P, Wang J, Li Y, Xiong B, Shen J.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5739-44. doi: 10.1016/j.bmcl.2011.08.019. Epub 2011 Aug 8.

PMID:
21873057
7.

Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.

Yang H, Dou W, Lou J, Leng Y, Shen J.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1340-5. doi: 10.1016/j.bmcl.2008.01.020. Epub 2008 Jan 11.

PMID:
18242087
8.

Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.

Webster SP, Ward P, Binnie M, Craigie E, McConnell KM, Sooy K, Vinter A, Seckl JR, Walker BR.

Bioorg Med Chem Lett. 2007 May 15;17(10):2838-43. Epub 2007 Feb 25.

PMID:
17350260
9.

Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.

Flyrén K, Bergquist LO, Castro VM, Fotsch C, Johansson L, St Jean DJ Jr, Sutin L, Williams M.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3421-5. Epub 2007 Mar 30.

PMID:
17442567
10.

Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.

Venier O, Pascal C, Braun A, Namane C, Mougenot P, Crespin O, Pacquet F, Mougenot C, Monseau C, Onofri B, Dadji-Faïhun R, Leger C, Ben-Hassine M, Van-Pham T, Ragot JL, Philippo C, Güssregen S, Engel C, Farjot G, Noah L, Maniani K, Nicolaï E.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2244-51. doi: 10.1016/j.bmcl.2011.02.111. Epub 2011 Mar 23.

PMID:
21439819
11.

3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor.

Lee Y, Shin YJ, Ahn SK.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1421-5. doi: 10.1016/j.bmcl.2014.01.017. Epub 2014 Jan 13.

PMID:
24507919
12.

Discovery of novel sulfonamides as potent and selective inhibitors against human and mouse 11β-hydroxysteroid dehydrogenase type 1.

Xia G, Liu L, Xue M, Liu H, Yu J, Li P, Chen Q, Xiong B, Liu X, Shen J.

Mol Cell Endocrinol. 2012 Jul 6;358(1):46-52. doi: 10.1016/j.mce.2012.02.017. Epub 2012 Mar 3.

PMID:
22410288
13.

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.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3168-72. doi: 10.1016/j.bmcl.2008.04.069. Epub 2008 May 1.

PMID:
18485702
14.

Design and synthesis of (R)-1-arylsulfonylpiperidine-2-carboxamides as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Xia G, Liu L, Liu H, Yu J, Xu Z, Chen Q, Ma C, Li P, Xiong B, Liu X, Shen J.

ChemMedChem. 2013 Apr;8(4):577-81. doi: 10.1002/cmdc.201300022. Epub 2013 Mar 7.

PMID:
23471829
15.

Design, synthesis and SAR of piperidyl-oxadiazoles as 11β-hydroxysteroid dehydrogenase 1 inhibitors.

Xia G, You X, Liu L, Liu H, Wang J, Shi Y, Li P, Xiong B, Liu X, Shen J.

Eur J Med Chem. 2013 Apr;62:1-10. doi: 10.1016/j.ejmech.2012.12.059. Epub 2013 Jan 10.

PMID:
23353742
16.

Adamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Su X, Halem HA, Thomas MP, Moutrille C, Culler MD, Vicker N, Potter BV.

Bioorg Med Chem. 2012 Nov 1;20(21):6394-402. doi: 10.1016/j.bmc.2012.08.056. Epub 2012 Sep 12.

17.

Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1.

Su X, Pradaux-Caggiano F, Vicker N, Thomas MP, Halem H, Culler MD, Potter BV.

ChemMedChem. 2011 Sep 5;6(9):1616-29. doi: 10.1002/cmdc.201100182. Epub 2011 Jun 28.

18.

Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.

Julian LD, Wang Z, Bostick T, Caille S, Choi R, DeGraffenreid M, Di Y, He X, Hungate RW, Jaen JC, Liu J, Monshouwer M, McMinn D, Rew Y, Sudom A, Sun D, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP.

J Med Chem. 2008 Jul 10;51(13):3953-60. doi: 10.1021/jm800310g. Epub 2008 Jun 14.

PMID:
18553955
19.

Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes.

Deng X, Shen Y, Yang J, He J, Zhao Y, Peng LY, Leng Y, Zhao QS.

Eur J Med Chem. 2013 Jul;65:403-14. doi: 10.1016/j.ejmech.2013.05.010. Epub 2013 May 18.

PMID:
23747808
20.

Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.

Stanetty C, Czollner L, Koller I, Shah P, Gaware R, Cunha TD, Odermatt A, Jordis U, Kosma P, Classen-Houben D.

Bioorg Med Chem. 2010 Nov 1;18(21):7522-41. doi: 10.1016/j.bmc.2010.08.046. Epub 2010 Sep 28.

PMID:
20851614
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