Journal of Medicinal Chemistry p. 756 - 772 (1992)
Update date:2022-07-29
Topics:
Floyd
Kimball
Krapcho
Das
Turk
Moquin
Lago
Duff
Lee
White
Ridgewell
Moreland
Brittain
Normandin
Hedberg
Cucinotta
As part of a program to discover potent antihypertensive analogues of diltiazem (3a), we prepared 1-benzazepin-2-ones (4). Benzazepinones competitively displace radiolabeled diltiazem, and show the same absolute stereochemical preferences at the calcium channel receptor protein. Derivatives of 4 containing a trifluoromethyl substituent in the fused aromatic ring show potent and long-acting antihypertensive activity. Studies of the metabolism of 4 lead to the metabolically stable antihypertensive calcium channel blockers 5a and 5c. Benzazepinone 5a is a longer acting and more potent antihypertensive agent than the second generation diltiazem analogue TA-3090 (3e).
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