A novel series of indazole-/indole-based glucagon receptor antagonists (original) (raw)

The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus

Mary Didiuk

Bioorganic & Medicinal Chemistry Letters, 2013

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Discovery of a Novel Glucagon Receptor Antagonist N-[(4-{(1S)-1-[3-(3, 5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the Treatment of Type II Diabetes

Mari Candelore

Journal of Medicinal Chemistry, 2012

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In Silico Identification of Novel Glucagon Receptor Antagonist for the Treatment of Type 2 Diabetes Mellitus

Pritish Kumar

Enzyme Engineering, 2015

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Anti-Diabetic Efficacy and Impact on Amino Acid Metabolism of GRA1, a Novel Small-Molecule Glucagon Receptor Antagonist

Mari Candelore

PLoS ONE, 2012

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Recent Progress in the Use of Glucagon and Glucagon Receptor Antago-nists in the Treatment of Diabetes Mellitus

Huba Kalasz

The open medicinal chemistry journal, 2014

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A Novel Glucagon Receptor Antagonist Inhibits Glucagon-Mediated Biological Effects

Guoqiang Jiang, Mari Candelore

Diabetes, 2004

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Glucagon and Glucagon-Like Peptide Receptors as Drug Targets

Jennifer Estall

Current Pharmaceutical Design, 2006

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Glucagon-like peptide-1 receptor agonists for the treatment of type 2 diabetes: Differences and similarities

Thazha Prakash

European Journal of Internal Medicine, 2014

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A Review of Practical Issues on the Use of Glucagon- Like Peptide-1 Receptor Agonists for the Management of Type 2 Diabetes

芳瑩 廖

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Glucagon-like peptide 1 receptor agonists and dipeptidyl peptidase IV inhibitors: new therapeutic agents for the treatment of type 2 diabetes

Owais Khan

Current Opinion in Endocrinology & Diabetes, 2005

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Comparison Review of Short-Acting and Long-Acting Glucagon-like Peptide-1 Receptor Agonists

Edoardo Mannucci

Diabetes Therapy, 2015

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Novel strategies for the pharmacological management of type 2 diabetes

Angela Bulotta

Trends in Pharmacological Sciences, 2004

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Preclinical exploration of combined glucagon inhibition and liver-preferential insulin for treatment of diabetes using in vitro assays and rat and mouse models

Andrew Bowler

Diabetologia, 2022

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Identification of a novel conformationally constrained glucagon receptor antagonist

Mary Didiuk

Bioorganic & Medicinal Chemistry Letters, 2014

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Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus

Xiaoxiong Wei

Diabetes, obesity & metabolism, 2016

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Glucagon like peptide 1 receptor agonists: a therapy for diabetes management

Johan Granados Vega

Ces Medicina, 2018

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Optimization of Alkylidene Hydrazide Based Human Glucagon Receptor Antagonists. Discovery of the Highly Potent and Orally Available 3-Cyano-4-hydroxybenzoic Acid [1-(2,3,5,6-Tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide

John May

Journal of Medicinal Chemistry, 2002

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Therapeutic molecules against type 2 diabetes: What we have and what are we expecting

Ashwini Kumar, SUDHANSHU BHARTI

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Discovery of potent, orally active benzimidazole glucagon receptor antagonists

Guoqiang Jiang, Mari Candelore

Bioorganic & Medicinal Chemistry Letters, 2008

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A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice

jiayu liao

Proceedings of the National Academy of Sciences, 2007

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Glucagon-like peptide-1 derivatives and dipeptidyl peptidase-IV inhibitors. New hope for the treatment of type-2 diabetes

Mohamed Al-omar

Saudi medical journal, 2005

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Overview of Glucagon-like Peptide-1 Receptor Agonists

Joan Grant

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Computational identification of novel natural inhibitors of glucagon receptor for checking type II diabetes mellitus

Sonam Grover

BMC bioinformatics, 2014

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Glucagon-like peptide-1 receptor agonist therapeutics for total diabetes management: Assessment of composite end-points.

Ryota Usui, Daisuke Yabe

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Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents

Kiran Shah

Bioorganic & Medicinal Chemistry Letters, 2012

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A 5-week study of the pharmacokinetics and pharmacodynamics of LY2189265, a novel, long-acting glucagon-like peptide-1 analogue, in patients with type 2 diabetes

Fabian Tibaldi

Diabetes, Obesity and Metabolism, 2011

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Dual-acting peptide with prolonged glucagon-like peptide-1 receptor agonist and glucagon receptor antagonist activity for the treatment of type 2 diabetes

Nicole Barucci, Kevin Clairmont

Journal of Endocrinology, 2007

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The Glucagon Receptor as a Drug Target - a Witches’ Brew of Eye of Newt (Peptides) and Toe of Frog (Receptors)

Derek Nunez

Diabetes, Obesity and Metabolism

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des His 1, des Phe 6, Glu 9]glucagon amide: A newly designed “pure” glucagon antagonist

Clinton David

Bioorganic & Medicinal Chemistry Letters, 1995

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