I. Sebhat

发表

Molecular Profiling Reveals a Common Metabolic Signature of Tissue Fibrosis

Peter S. Kutchukian, A. Peier, Shirly Pinto, 2020, Cell reports. Medicine.

A role for the melanocortin 4 receptor in sexual function

Christopher P Austin, Ralph Stearns, G. Christ, 2002, Proceedings of the National Academy of Sciences of the United States of America.

Chapter 4. Melanocortin-4 receptor agonists and antagonists: Chemistry and potential therapeutic utilities

M. Bednarek, R. Nargund, T. Fong, 2003 .

Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula.

L. Gantert, D. Macintyre, L. V. D. van der Ploeg, 2002, European journal of pharmacology.

Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

L. V. D. van der Ploeg, A. Patchett, R. Nargund, 2007, Bioorganic & medicinal chemistry letters.

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.

Howard Y. Chen, R. Nargund, M. Wyvratt, 2010, Bioorganic & medicinal chemistry letters.

Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.

M. Reibarkh, Howard Y. Chen, R. Nargund, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.

D. Macintyre, Howard Y. Chen, R. Nargund, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.

J. Huber, F. Ujjainwalla, L. V. D. van der Ploeg, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

D. Macintyre, Howard Y. Chen, R. Nargund, 2010, Bioorganic & medicinal chemistry letters.

Synthesis of the Antitumor Alkaloid (+)-Pancratistatin Using the β-Azidonation Reaction via a Prochiral 4-Arylcyclohexanone Derivative

I. Sebhat, P. Magnus, 1998 .

Directed Lithiation in Arenetricarbonylchromium(0) Complexes: Assessment of Some Directing Group Specificities and of Electrophilic Quench Efficacies

David J. Williams, A. White, I. Sebhat, 2000 .

Application of the β-azidonation reaction to the synthesis of the antitumor alkaloid (+)-pancratistatin

I. Sebhat, P. Magnus, 1998 .

Asymmetric deprotonation—substitution of arenetricarbonylchromium(0) complexes: substituent controlled lithiation with the butyllithium–sparteine system

David J. Williams, A. White, I. Sebhat, 2000 .

Preparation of 2,3-dihydro-1H-spiro[isoquinoline-4,4′-piperidine] via an N-sulfonyl Pictet–Spengler reaction

R. Nargund, Jian Liu, I. Sebhat, 2006 .

Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 – present)

S. Gatti, S. Schann, Sylvain Celanire, 2015, Expert opinion on therapeutic patents.

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.

J. Metzger, D. Macintyre, L. V. D. van der Ploeg, 2005, Bioorganic & medicinal chemistry letters.

Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy

M. Erion, D. Kemp, S. Prahalada, 2017, Science.

AMPK activators – potential therapeutics for metabolic and other diseases

G. Zhou, B. Zhang, I. Sebhat, 2009, Acta physiologica.

Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver

M. Erion, D. Kemp, S. Souza, 2019, PloS one.

Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

M. Reitman, J. Metzger, Mark Hadden, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.

D. Macintyre, Howard Y. Chen, R. Nargund, 2011, Bioorganic & medicinal chemistry letters.

Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.

J. Metzger, L. V. D. van der Ploeg, C. Rosenblum, 2010, Bioorganic & medicinal chemistry letters.

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.

L. V. D. van der Ploeg, A. Patchett, R. Nargund, 2005, Bioorganic & medicinal chemistry letters.

Antiobesity Effect of MK-5046, a Novel Bombesin Receptor Subtype-3 Agonist

M. Reitman, J. Metzger, Liming Yang, 2011, Journal of Pharmacology and Experimental Therapeutics.

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.

M. Reitman, J. Metzger, Mark Hadden, 2010, Bioorganic & medicinal chemistry letters.

PAN-AMPK Activation Improves Renal Function in a Rat Model of Progressive Diabetic Nephropathy

Shirly Pinto, D. Kelley, E. Muise, 2019, The Journal of Pharmacology and Experimental Therapeutics.

Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

D. Kemp, Gaochao Zhou, F. A. Romero, 2018, ACS medicinal chemistry letters.

A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Michael E. Lassman, Shirly Pinto, J. Lisnock, 2012, Bioorganic & medicinal chemistry letters.

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.

D. Johnston, D. Macintyre, L. V. D. van der Ploeg, 2002, Journal of medicinal chemistry.

Small molecule ligands of the human melanocortin-4 receptor.

F. Ujjainwalla, I. Sebhat, 2007, Current topics in medicinal chemistry.

Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.

Margaret S. Wu, Q. Dang, D. Mackenna, 2017, Journal of medicinal chemistry.

Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.

M. Reitman, J. Metzger, O. Palyha, 2011, ACS medicinal chemistry letters.

1 TITLE

S. Souza, D. Kelley, Shirly Pinto, 2019 .

Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

M. Reitman, J. Metzger, Mark Hadden, 2010, Bioorganic & medicinal chemistry letters.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.

J. Metzger, D. Macintyre, L. V. D. van der Ploeg, 2005, Bioorganic & medicinal chemistry letters.

AMPK Activation in Health and Disease

R. Myers, I. Sebhat, 2012 .

PAN-AMPK ACTIVATION IMPROVES RENAL FUNCTION IN A RAT MODEL OF PROGRESSIVE DIABETIC NEPHROPATHY

D. Kelley, Shirly Pinto, E. Muise, 2019 .

Determination of brain and plasma drug concentrations by liquid chromatography/tandem mass spectrometry.

P. Griffin, J. Fenyk-Melody, C. Tamvakopoulos, 2000, Rapid communications in mass spectrometry : RCM.

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.

Howard Y. Chen, R. Nargund, M. Wyvratt, 2010, Bioorganic & Medicinal Chemistry Letters.