The preparation of 3-cyano-4,6-diaryl-pyridin-2(1H)-ones 4a-h, calcium entry blockers related to diltiazem, is described starting from 1,3-diaryl-2-propen-1-ones 5. On preliminary pharmacological tests all compounds are active and some of them show calcium antagonistic activity superior or comparable to diltiazem.
Manna, C., Bolasco, B., Botta, M., Tafi, A., Filippelli, R. (2000). Synthesis and Preliminary Biological Evaluation of 4,6-Disubstituted 3-Cyanopyridin-2(1H)-ones, a New Class of Calcium Entry Blockers. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 10(16), 1883-1885 [10.1016/S0960-894X(00)00361-9].
Synthesis and Preliminary Biological Evaluation of 4,6-Disubstituted 3-Cyanopyridin-2(1H)-ones, a New Class of Calcium Entry Blockers
BOTTA, MAURIZIO;TAFI, ANDREA;
2000-01-01
Abstract
The preparation of 3-cyano-4,6-diaryl-pyridin-2(1H)-ones 4a-h, calcium entry blockers related to diltiazem, is described starting from 1,3-diaryl-2-propen-1-ones 5. On preliminary pharmacological tests all compounds are active and some of them show calcium antagonistic activity superior or comparable to diltiazem.
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https://hdl.handle.net/11365/19321