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Papers authored by Fotsch C

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Cytochrome P450-Mediated Epoxidation of 2-Aminothiazole-Based AKT Inhibitors: Identification of Novel GSH Adducts and Reduction of Metabolic Activation through Structural Changes Guided by in Silico and in Vitro Screening.

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Subramanian R, Lee MR, Allen JG, Bourbeau MP, Fotsch C, Hong FT, Tadesse S, Yao G, Yuan CC, Surapaneni S, Skiles GL, Wang X, Wohlhieter GE, Zeng Q, Zhou Y, Zhu X,

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Chemical research in toxicology 23(3):653-63, 2010 Mar 15 - Who cited this? | PubMed ID: 20095585 | Fulltext

Azole-based inhibitors of AKT/PKB for the treatment of cancer.

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Zeng Q, Allen JG, Bourbeau MP, Wang X, Yao G, Tadesse S, Rider JT, Yuan CC, Hong FT, Lee MR, Zhang S, Lofgren JA, Freeman DJ, Yang S, Li C, Tominey E,

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Bioorganic & medicinal chemistry letters 20(5):1559-64, 2010 Mar 1 - Who cited this? | PubMed ID: 20137943 | Fulltext

Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.

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Poon SF, St Jean DJ, Harrington PE, Henley C, Davis J, Morony S, Lott FD, Reagan JD, Lu JY, Yang Y, and Fotsch C

Journal of medicinal chemistry 52(21):6535-8, 2009 Nov 12 - Who cited this? | PubMed ID: 19835382 | Fulltext

Time of the day for 11beta-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice.

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Véniant MM, Hale C, Komorowski R, Chen MM, St Jean DJ, Fotsch C, and Wang M

Diabetes, obesity & metabolism 11(2):109-17, 2009 Feb - Who cited this? | PubMed ID: 18479468 | Fulltext

Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.

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Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G,

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Journal of medicinal chemistry 51(24):7953-67, 2008 Dec 25 - Who cited this? | PubMed ID: 19053753 | Fulltext

Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.

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Fotsch C and Wang M

Journal of medicinal chemistry 51(16):4851-7, 2008 Aug 28 - Who cited this? | PubMed ID: 18652443 | Fulltext

2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.

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Johansson L, Fotsch C, Bartberger MD, Castro VM, Chen M, Emery M, Gustafsson S, Hale C, Hickman D, Homan E, Jordan SR, Komorowski R, Li A, McRae K, Moniz G, Matsumoto G,

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Journal of medicinal chemistry 51(10):2933, 2008 May 22 - Who cited this? | PubMed ID: 18419108 | Fulltext

Structural characterization and pharmacodynamic effects of an orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor.

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Hale C, Véniant M, Wang Z, Chen M, McCormick J, Cupples R, Hickman D, Min X, Sudom A, Xu H, Matsumoto G, Fotsch C, St Jean DJ, and Wang M

Chemical biology & drug design 71(1):36-44, 2008 Jan - Who cited this? | PubMed ID: 18069989 | Fulltext

Inhibitors of 11beta-HSD1: A Potential Treatment for the Metabolic Syndrome.

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St Jean DJ, Wang M, and Fotsch C

Current topics in medicinal chemistry 8(17):1508-23, 2008 - Who cited this? | PubMed ID: 19075762 | Fulltext

The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.

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Yuan C, St Jean DJ, Liu Q, Cai L, Li A, Han N, Moniz G, Askew B, Hungate RW, Johansson L, Tedenborg L, Pyring D, Williams M, Hale C, Chen M, Cupples R,

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Bioorganic & medicinal chemistry letters 17(22):6056-61, 2007 Nov 15 - Who cited this? | PubMed ID: 17919905 | Fulltext

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.

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Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R,

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Journal of medicinal chemistry 50(15):3515, 2007 Jul 26 - Who cited this? | PubMed ID: 17585750 | Fulltext

Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.

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Norman MH, Zhu J, Fotsch C, Bo Y, Chen N, Chakrabarti P, Doherty EM, Gavva NR, Nishimura N, Nixey T, Ognyanov VI, Rzasa RM, Stec M, Surapaneni S, Tamir R, Viswanadhan VN,

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Journal of medicinal chemistry 50(15):3497, 2007 Jul 26 - Who cited this? | PubMed ID: 17585749 | Fulltext

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

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

Bioorganic & medicinal chemistry letters 17(12):3421-5, 2007 Jun 15 - Who cited this? | PubMed ID: 17442567 | Fulltext

Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.

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Biswas K, Li A, Chen JJ, D'Amico DC, Fotsch C, Han N, Human J, Liu Q, Norman MH, Riahi B, Yuan C, Suzuki H, Mareska DA, Zhan J, Clarke DE, Toro A,

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Journal of medicinal chemistry 50(9):2200-12, 2007 May 3 - Who cited this? | PubMed ID: 17408249 | Fulltext

Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.

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D'Amico DC, Aya T, Human J, Fotsch C, Chen JJ, Biswas K, Riahi B, Norman MH, Willoughby CA, Hungate R, Reider PJ, Biddlecome G, Lester-Zeiner D, Staden CV, Johnson E, Kamassah A,

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Journal of medicinal chemistry 50(4):607-10, 2007 Feb 22 - Who cited this? | PubMed ID: 17243660 | Fulltext

2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.

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Jean DJ, Yuan C, Bercot EA, Cupples R, Chen M, Fretland J, Hale C, Hungate RW, Komorowski R, Veniant M, Wang M, Zhang X, and Fotsch C

Journal of medicinal chemistry 50(3):429-32, 2007 Feb 8 - Who cited this? | PubMed ID: 17266194 | Fulltext

Calcium sensing receptor activators: calcimimetics.

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Harrington PE and Fotsch C

Current medicinal chemistry 14(28):3027-34, 2007 - Who cited this? | PubMed ID: 18220738 | Fulltext

Small-molecule compounds that modulate lipolysis in adipose tissue: targeting strategies and molecular classes.

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Wang M and Fotsch C

Chemistry & biology 13(10):1019-27, 2006 Oct - Who cited this? | PubMed ID: 17052606 | Fulltext

Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

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Ognyanov VI, Balan C, Bannon AW, Bo Y, Dominguez C, Fotsch C, Gore VK, Klionsky L, Ma VV, Qian YX, Tamir R, Wang X, Xi N, Xu S, Zhu D, Gavva NR,

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Journal of medicinal chemistry 49(12):3719-42, 2006 Jun 15 - Who cited this? | PubMed ID: 16759115 | Fulltext

A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.

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Fotsch C, Biddlecome G, Biswas K, Chen JJ, D'Amico DC, Groneberg RD, Han NB, Hsieh FY, Kamassah A, Kumar G, Lester-Zeiner D, Liu Q, Mareska DA, Riahi BB, Wang YJ, Yang K,

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Bioorganic & medicinal chemistry letters 16(8):2071-5, 2006 Apr 15 - Who cited this? | PubMed ID: 16464576 | Fulltext

Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.

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Xi N, Bo Y, Doherty EM, Fotsch C, Gavva NR, Han N, Hungate RW, Klionsky L, Liu Q, Tamir R, Xu S, Treanor JJ, and Norman MH

Bioorganic & medicinal chemistry letters 15(23):5211-7, 2005 Dec 1 - Who cited this? | PubMed ID: 16203144 | Fulltext

Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

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Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N,

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Bioorganic & medicinal chemistry letters 15(6):1623-7, 2005 Mar 15 - Who cited this? | PubMed ID: 15745810 | Fulltext

Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.

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Doherty EM, Fotsch C, Bo Y, Chakrabarti PP, Chen N, Gavva N, Han N, Kelly MG, Kincaid J, Klionsky L, Liu Q, Ognyanov VI, Tamir R, Wang X, Zhu J, Norman MH,

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Journal of medicinal chemistry 48(1):71-90, 2005 Jan 13 - Who cited this? | PubMed ID: 15634002 | Fulltext

Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

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Xi N, Hale C, Kelly MG, Norman MH, Stec M, Xu S, Baumgartner JW, and Fotsch C

Bioorganic & medicinal chemistry letters 14(2):377-81, 2004 Jan 19 - Who cited this? | PubMed ID: 14698163 | Fulltext

Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).

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Fotsch C, Smith DM, Adams JA, Cheetham J, Croghan M, Doherty EM, Hale C, Jarosinski MA, Kelly MG, Norman MH, Tamayo NA, Xi N, and Baumgartner JW

Bioorganic & medicinal chemistry letters 13(14):2337-40, 2003 Jul 21 - Who cited this? | PubMed ID: 12824029 | Fulltext

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.

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Arasasingham PN, Fotsch C, Ouyang X, Norman MH, Kelly MG, Stark KL, Karbon B, Hale C, Baumgartner JW, Zambrano M, Cheetham J, and Tamayo NA

Journal of medicinal chemistry 46(1):9-11, 2003 Jan 2 - Who cited this? | PubMed ID: 12502354 | Fulltext

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.

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Fotsch C, Sonnenberg JD, Chen N, Hale C, Karbon W, and Norman MH

Journal of medicinal chemistry 44(14):2344-56, 2001 Jul 5 - Who cited this? | PubMed ID: 11428928 | Fulltext

Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.

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Norman MH, Chen N, Chen Z, Fotsch C, Hale C, Han N, Hurt R, Jenkins T, Kincaid J, Liu L, Lu Y, Moreno O, Santora VJ, Sonnenberg JD, and Karbon W

Journal of medicinal chemistry 43(22):4288-312, 2000 Nov 2 - Who cited this? | PubMed ID: 11063624 | Fulltext

A short, facile synthesis of 5-substituted 3-amino-1H-pyrrole-2-carboxylates.

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Chen N, Lu Y, Gadamasetti K, Hurt CR, Norman MH, and Fotsch C

The Journal of organic chemistry 65(8):2603-5, 2000 Apr 21 - Who cited this? | PubMed ID: 10789484 | Fulltext

On-resin macrocyclization of peptides via intramolecular SnAr reactions.

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Fotsch C, Kumaravel G, Sharma SK, Wu AD, Gounarides JS, Nirmala NR, and Petter RC

Bioorganic & medicinal chemistry letters 9(15):2125-30, 1999 Aug 2 - Who cited this? | PubMed ID: 10465530 | Fulltext

Solid-phase total synthesis of polymyxin B1.

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Sharma SK, Wu AD, Chandramouli N, Fotsch C, Kardash G, and Bair KW

The journal of peptide research : official journal of the American Peptide Society 53(5):501-6, 1999 May - Who cited this? | PubMed ID: 10424344 | Fulltext

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