Laura M. Monleón

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.

A bio-inspired enantioselective small-molecule artificial receptor for β adrenergic agonists and antagonists and its application for enantioselective extraction.

Administration of enantiomerically pure β-adrenergic agonists and antagonists increases their activity and reduces side effects. We report here a small-molecule artificial receptor (SMAR) that, by mimicking the β-adrenergic receptor, is able to enantioselectively extract commercial β-adrenergic interacting drugs. The selectivity is justified according to DFT calculations and X-ray diffraction experiments.

CCDC 973966: Experimental Crystal Structure Determination

Related Article: Victor Tena Perez, Angel L. Fuentes de Arriba, Laura M. Monleon, Luis Simon, Omayra H. Rubio, Francisca Sanz, and Joaquin R. Moran|2017|CSD Communication|||

Acyl Radicals from Nitriles Promoted by Cp2TiCl in β-Lactam Chemistry

In order to synthesize new tricyclic β-lactams we have studied the reactivity of 4-alkenylepoxy-N-(1-cyano-1-dimethylethyl)-2-azetidinones with Cp 2 TiCl. The desired trilactams were not formed at all but an unsaturated nitrile and an aldehyde were obtained instead. Under similar reaction conditions, the treatment of styrylnitrile with Cp 2 TiCl afforded the styrylaldehyde. The formation of aldehydes in these reactions suggest the generation of acyl radicals from nitriles mediated by Cp 2 TiCl.