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Items: 1 to 20 of 190

1.

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
2.

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
3.

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
4.

Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.

Zhang L, Chen J, Ning M, Zou Q, Leng Y, Shen J.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2748-52. doi: 10.1016/j.bmcl.2012.02.095. Epub 2012 Mar 3.

PMID:
22440625
5.

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
6.

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
7.

Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).

Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ, Ogg D, Packer MJ, Rees A, Revill J, Schofield P, Selmi N, Swales JG, Whittamore PR.

J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r. Epub 2012 Jun 19.

PMID:
22691057
8.

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
9.

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
10.

Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors.

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

ChemMedChem. 2010 Jul 5;5(7):1026-44. doi: 10.1002/cmdc.201000081.

PMID:
20486152
11.

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
12.

The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.

Yan X, Wang Z, Sudom A, Cardozo M, DeGraffenreid M, Di Y, Fan P, He X, Jaen JC, Labelle M, Liu J, Ma J, McMinn D, Miao S, Sun D, Tang L, Tu H, Ursu S, Walker N, Ye Q, Powers JP.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7071-5. doi: 10.1016/j.bmcl.2010.09.097. Epub 2010 Sep 29.

PMID:
20971000
13.

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
14.

Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

Ye XY, Yoon D, Chen SY, Nayeem A, Golla R, Seethala R, Wang M, Harper T, Sleczka BG, Apedo A, Li YX, He B, Kirby M, Gordon DA, Robl JA.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):654-60. doi: 10.1016/j.bmcl.2013.11.066. Epub 2013 Dec 5.

PMID:
24360604
15.

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
16.

Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.

Kwon SW, Kang SK, Lee JH, Bok JH, Kim CH, Dal Rhee S, Jung WH, Kim HY, Bae MA, Song JS, Ha DC, Cheon HG, Kim KY, Ahn JH.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):435-9. doi: 10.1016/j.bmcl.2010.10.123. Epub 2010 Nov 2.

PMID:
21093259
17.

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
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.

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
20.

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