Search Results - "Neubert, Alan D"
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Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans
Published in Journal of medicinal chemistry (08-06-2017)“…Modification of a gut restricted class of benzimidazole DGAT1 inhibitor 1 led to 9 with good oral bioavailability. The key structural changes to 1 include…”
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Design and Synthesis of Potent, Selective Inhibitors of Endothelin-Converting Enzyme
Published in Journal of medicinal chemistry (23-04-1998)“…Endothelin-1 is the most potent peptidic vasoconstrictor discovered to date. The final step of posttranslational processing of this peptide is the conversion…”
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Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides
Published in ACS medicinal chemistry letters (10-05-2012)“…High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which…”
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Perhydroquinolylbenzamides as Novel Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1
Published in Journal of medicinal chemistry (20-10-2005)“…High-throughput screening identified 5 as a weak inhibitor of 11β-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with…”
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Synthesis and Structure-Activity Relationships of Oxamic Acid and Acetic Acid Derivatives Related to L-Thyronine
Published in Journal of medicinal chemistry (01-02-1995)“…Aryloxamic acids 7 and 23, (arylamino)acetic acids 29, arylpropionic acids 33, arylthioacetic acids 37, and (aryloxy)acetic acid 41 related to…”
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Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Published in Journal of medicinal chemistry (20-10-2005)“…High-throughput screening identified 5 as a weak inhibitor of 11beta-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some…”
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2-Arylpyrazolo[4,3-c]quinolin-3-ones: a novel agonist, a partial agonist and an antagonist of benzodiazepines
Published in Journal of medicinal chemistry (01-04-1982)Get full text
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2-arylpyrazolo(4,3-c)quinolin-3-ones: Novel agonist, partial agonist, and antagonist of benzodiazepines
Published in Journal of medicinal chemistry (01-01-1982)“…The authors wish to report on three novel 2-arylpyrazolo(4,3-c)quinolin-3-ones, all of which possess extremely high affinity for the benzodiazepine receptors,…”
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