In vitro evaluation of the antielastase activity of polycyclic β-lactams

A series of bi- and tricyclic β-lactam compounds was synthesized and evaluated as inhibitors of cleavage of synthetic substrates in vitro by the serine proteases Human Leukocyte Elastase (HLE), Human Leukocyte Proteinase 3 (HLPR3) and Porcine Pancreatic Elastase (PPE). The obtained results have permitted us to describe a homobenzocarbacephem compound as HLE and HLPR3 inhibitor, to observe the positive effect that the styryl group exerts on the HLE inhibitory activity in polycyclic β-lactam compounds and to conclude that the hydroxyl function decreases the HLE inhibitory activity or rules it out completely.

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► A series of bi- and tricyclic β-lactam compounds has been synthesized.
► They have been evaluated as inhibitors of Human Leukocyte and Porcine Pancreatic Elastases and Human Leukocyte Proteinase 3.
► A homobenzocarbacephem compound has been described as HLE and HLPR3 inhibitor.
► The styryl group exerts a positive effect on the HLE inhibitory activity.
► The hydroxyl function decreases or eliminates the HLE inhibitory activity.