hERG optimization of MCHR1 antagonist benzofuro‐pyridine and pyrazino‐indole derivatives

József Huszár,Éva Bozó,Gyula Beke,Krisztina Katalin Szalai,Péter Kardos,András Boros,István Greiner,János Éles

ChemMedChem（2022）

引用 3|浏览1

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摘要

Healthier heart: Melanin concentrating hormone receptor 1 (MCHR1) antagonists containing benzofuro−pyridine or pyrazino−indole scaffolds have been identified. Fine-tuning the lipophilicity and amine basicity provided compounds 17 and 23 g with both decreased hERG inhibition and metabolic clearance.

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