C. Fotsch

发表

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

N. Chen, J. Treanor, C. Dominguez, 2007, Journal of medicinal chemistry.

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

N. Chen, J. Treanor, V. Viswanadhan, 2007, Journal of medicinal chemistry.

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

J. Treanor, C. Dominguez, C. Fotsch, 2006, Journal of medicinal chemistry.

Systematic Study of the Glutathione (GSH) Reactivity of N-Phenylacrylamides: 2. Effects of Acrylamide Substitution.

J. McCarter, T. Arvedson, M. Bartberger, 2020, Journal of medicinal chemistry.

Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).

Jiandong Zhang, R. Syed, R. Hungate, 2010, Journal of medicinal chemistry.

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

N. Chen, Z. Chen, V. Santora, 2000, Journal of medicinal chemistry.

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

N. Chen, C. Fotsch, M. Norman, 2001, Journal of medicinal chemistry.

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

Minghan Wang, C. Fotsch, 2006, Chemistry & biology.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Kristin L. Andrews, Jiandong Zhang, S. Chmait, 2015, Journal of medicinal chemistry.

Discovery of a Calcimimetic with Differential Effects on Parathyroid Hormone and Calcitonin Secretion

S. Morony, W. Richards, J. Reagan, 2011, Journal of Pharmacology and Experimental Therapeutics.

Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution.

J. McCarter, T. Arvedson, A. Tasker, 2015, Journal of medicinal chemistry.

Facile Modulation of Antibody Fucosylation with Small Molecule Fucostatin Inhibitors and Cocrystal Structure with GDP-Mannose 4,6-Dehydratase.

J. B. Jordan, J. McCarter, M. Mujacic, 2016, ACS chemical biology.

11β-Hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases

C. Fotsch, J. Chen, B. Askew, 2005 .

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.

Jiandong Zhang, R. Hungate, M. Véniant, 2008, Journal of medicinal chemistry.

Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.

Matthew R. Lee, Shiwen Zhang, J. Lofgren, 2011, Bioorganic & medicinal chemistry letters.

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

Daniel J. Freeman, Q. Zeng, Guomin Yao, 2010, Bioorganic & medicinal chemistry letters.

Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase.

M. Fielden, M. Véniant, Minghan Wang, 2013, Journal of medicinal chemistry.

The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.

S. Morony, J. Reagan, David A. Martin, 2010, Bioorganic & medicinal chemistry letters.

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

N. Chen, C. Fotsch, A. Bannon, 2005, Bioorganic & medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.

S. Chmait, M. Bartberger, S. Jordan, 2014, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

R. Kunz, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Enzyme-catalyzed organic synthesis: practical routes to aza sugars and their analogs for use as glycoprocessing inhibitors

Chi‐Huey Wong, G. Look, C. Fotsch, 1993 .

The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.

T. Bush, M. Rong, K. Sham, 2013, Bioorganic & medicinal chemistry letters.

Time of the day for 11β‐HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice

M. Véniant, C. Fotsch, R. Komorowski, 2009, Diabetes, obesity & metabolism.

Structural Characterization and Pharmacodynamic Effects of an Orally Active 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor

Zhulun Wang, Haoda Xu, Xiaoshan Min, 2007, Chemical biology & drug design.

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

Jiandong Zhang, R. Hungate, Meredith Williams, 2007, Bioorganic & medicinal chemistry letters.

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

Meredith Williams, C. Fotsch, V. M. Castro, 2007, Bioorganic & medicinal chemistry letters.

Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.

Matthew R. Lee, A. Tasker, K. Sham, 2012, ACS medicinal chemistry letters.

Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.

Matthew R. Lee, A. Tasker, M. Horner, 2012, Bioorganic & medicinal chemistry letters.

4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.

Matthew R. Lee, M. Horner, K. Sham, 2011, ACS medicinal chemistry letters.

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.

Jiandong Zhang, E. Homan, Meredith Williams, 2008, Journal of medicinal chemistry.

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

G. Biddlecome, C. Fotsch, Kevin C Yang, 2006, Bioorganic & medicinal chemistry letters.

Stereochemical control in reactions of nucleophiles with oxocarbenium ions formed by intramolecular opening of activated epoxides by neighboring carbonyl groups

C. Fotsch, A. Chamberlin, 1991 .

Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.

S. Chmait, M. Bartberger, S. Jordan, 2015, Journal of medicinal chemistry.

Mitigating heterocycle metabolism in drug discovery.

C. Fotsch, David J St Jean, Christopher Fotsch, 2012, Journal of medicinal chemistry.

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

Y. Lu, C. Fotsch, M. Norman, 2000, The Journal of organic chemistry.

Synthesis of a guanidino-sugar as a glycosyl cation mimic

Chi‐Huey Wong, C. Fotsch, 1994 .

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

Ming Huang, Hong Sun, Eileen Johnson, 2007, Journal of medicinal chemistry.

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

J. Treanor, R. Hungate, E. Doherty, 2005, Bioorganic & medicinal chemistry letters.

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

R. Hungate, M. Véniant, Minghan Wang, 2007, Journal of medicinal chemistry.

Vinyllithium cyclizations with unactivated alkenes as internal electrophiles: stereoselective formation of substituted methylenecyclopentanes

C. Fotsch, A. Chamberlin, L. Cervini, 1988 .

Stereochemical Control in Reactions of Nucleophiles with Oxocarbenium Ions Formed by Intramolecular Opening of Activated Epoxides by Neighboring Carbonyl Groups.

C. Fotsch, A. Chamberlin, 1991 .

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).

Michael G Kelly, J. Cheetham, M. Jarosinski, 2003, Bioorganic & medicinal chemistry letters.

Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism.

S. Morony, K. Pattabiraman, J. Reagan, 2013, Bioorganic & medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.

R. Kunz, S. Chmait, M. Bartberger, 2014, Journal of medicinal chemistry.

Calcium sensing receptor activators: calcimimetics.

C. Fotsch, Christopher Fotsch, Paul E Harrington, 2007, Current medicinal chemistry.

Solid-phase total synthesis of polymyxin B1.

K. Bair, C. Fotsch, N. Chandramouli, 1999, The journal of peptide research : official journal of the American Peptide Society.

Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.

L. Arik, R. Hungate, G. Biddlecome, 2010, Bioorganic & medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.

R. Wahl, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

R. Wahl, Jiandong Zhang, S. Chmait, 2013, Nature.

On-resin macrocyclization of peptides via intramolecular SnAr reactions.

N. Nirmala, R. Petter, C. Fotsch, 1999, Bioorganic & medicinal chemistry letters.

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

L. Arik, E. Laird, V. Viswanadhan, 2007, Journal of medicinal chemistry.

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

N. Chen, J. Treanor, P. Chakrabarti, 2005, Journal of medicinal chemistry.

Synthesis of Nitrocyclitols Based on Enzymic Aldol Reaction and Intramolecular Nitroaldol Reaction

Chi‐Huey Wong, C. Fotsch, Wen-Chi Chou, 1995 .

Synthesis of Nitrocyclitols Based on Enzymatic Aldol Reaction and Intramolecular Nitroaldol Reaction.

Chi‐Huey Wong, C. Fotsch, Wen-Chi Chou, 1995 .

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

Minghan Wang, C. Fotsch, 2008, Journal of medicinal chemistry.

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

C. Fotsch, Markian M Stec, N. Xi, 2004, Bioorganic & medicinal chemistry letters.

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]‐NH2.

C. Fotsch, 2003 .

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

J. Cheetham, K. Stark, C. Fotsch, 2003, Journal of medicinal chemistry.

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.

Q. Zeng, G. E. Wohlhieter, Guomin Yao, 2010, Chemical research in toxicology.

Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.

M. Véniant, R. Subramanian, M. Emery, 2011, ACS medicinal chemistry letters.

Blockade of Glucocorticoid Excess at the Tissue Level: Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 as a Therapy for Type 2 Diabetes

Minghan Wang, C. Fotsch, 2008 .

Mitigating heterocycle metabolism in drug discovery.

C. Fotsch, D. J. St Jean, 2012, Journal of medicinal chemistry.