… enzyme inhibitors: new orally active 1, 4-thiazepine-2, 5-diones, 1, 4-thiazine-2, 5-diones, and 1, 4-benzothiazepine-2, 5-diones possessing antihypertensive activity

…, PR Menard, JN Barton, B Loev, H Jones…

Index: Skiles; Suh; Williams; Menard; Barton; Loev; Jones; Neiss; Schwab; Mann Journal of Medicinal Chemistry, 1986 , vol. 29, # 5 p. 784 - 796

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Citation Number: 50

Abstract

The preparation of a series of 1, 4-thiazepine-2, 5-diones, 14-thiazine-2, 5-diones, and 1, 4- benzothiazepine-2, 5-diones and their ability in inhibiting the activity of angiotensin- converting enzyme (ACE) in vitro and in vivo were examined. These compounds are assumed to act as prodrugs since they undergo rapid ring-opening reactions to give the corresponding biologically active free SH compounds when incubated with rat plasma or ...