Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides

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Abstract

A series of benzo-fused lactams were incorporated as conformationally restricted dipeptide mimetics of Ala-Pro in dual-acting ACE/NEP inhibitors 1 and 2. The result of this modification led to compounds possessing excellent inhibitory potency versus ACE and NEP both in vitro and in vivo.

A series of benzo-fused lactams were incorporated as conformationally restricted dipeptide mimetics of Ala-Pro in angiotensin converting (ACE)/neutral endopeptidase (NEP) inhibitors.

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