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Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
Bioorg Med Chem Lett
March 2010
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.
View Article and Find Full Text PDFMelanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Bioorg Med Chem Lett
October 2007
Department of Medicinal Chemistry, Merck & Co., Inc, PO Box, 2000, Rahway, NJ 07065, USA.
SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.
View Article and Find Full Text PDFHighly potent growth hormone secretagogues.
Bioorg Med Chem Lett
July 2007
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
During an effort to search for more potent growth hormone secretagogues, we discovered a class of compounds of which the best compound 8 was 7-fold more active in vitro than the best compound in the series we revealed before [Tata, J. R.; Lu, Z.
View Article and Find Full Text PDFAntidiabetic activity of a highly potent and selective nonpeptide somatostatin receptor subtype-2 agonist.
Endocrinology
October 2006
Medizinische Klinik m. S. Hepatologie, Gastroenterologie, Endokrinologie und Stoffwechsel, Charité-Universitätsmedizin Berlin, Campus Virchow-Klinikum, Augustenburger Platz 1, 13353 Berlin, Germany.
Article Synopsis
- Somatostatin inhibits both glucagon and insulin secretion, but its effect on controlling hyperglycemia in type 2 diabetes is limited because it also suppresses insulin secretion.
- A new study introduces an sst(2)-selective, nonpeptide agonist (compound 1) that effectively reduces glucagon secretion from pancreatic islets, leading to lowered glucose levels without affecting insulin concentration.
- In animal models of type 2 diabetes, compound 1 demonstrated significant glucose-lowering effects, particularly in the fasting state, showcasing its potential as an innovative oral treatment option for managing the disease.
Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.
Bioorg Med Chem Lett
March 2006
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.
Design and synthesis of potent MC4 selective agonists based on cyclohexylpiperidine derived cyclic urea, oxazolidinones, and sulfonamide based privileged structures are disclosed.
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