Synthesis and preliminary biological evaluation of 4, 6-disubstituted 3-cyanopyridin-2 (1H)-ones, a new class of calcium entry blockers

F Manna, F Chimenti, A Bolasco, B Bizzarri…

Index: Manna, Fedele; Chimenti, Franco; Bolasco, Adriana; Bizzarri, Bruna; Botta, Maurizio; Tafi, Andrea; Filippelli, Amelia; Rossi, Settimio Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 16 p. 1883 - 1885

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Citation Number: 8

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.