The design, synthesis, and biological evaluation of phosphoramide derivatives as urease inhibitors to reduce the loss of ammonia has been carried out. Forty phosphorus derivatives were synthesized and their inhibitory activities evaluated against that of jack bean urease. In addition, in vivo assays have been carried out. All of the compounds were characterized by IR, (1)H NMR, MS, and elemental microanalysis. In some cases, detailed molecular modeling studies were carried out, and these highlighted the interaction between the enzyme active center and the compounds and also the characteristics related to their activity as urease inhibitors. According to the IC(50) values for in vitro inhibitory activity, 12 compounds showed values below 1 microM and 8 of them represent improvements of activity in comparison to the commercial urease inhibitor N-n-butylthiophosphorictriamide (NBPT) (100 nM) (AGROTAIN). On the basis of the activity results and the conclusions of the molecular modeling study, a structural model for new potential inhibitors has been defined.

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Cardiac contusion following blunt chest trauma is not rare, and the works in the literature report incidence rates between 5 and 50%. Traffic accidents are the most frequent cause of cardiac contusion followed by violent fall impacts, aggressions and the practice of risky sports. The spectrum of post-traumatic cardiac lesions varies greatly, ranging from no symptoms to decrease in cardiac function. Cardiogenic shock is a rarely encountered manifestation of blunt cardiac contusion. We review our experience of cardiac contusion after blunt chest trauma, and we describe two very severe cases that manifested as cardiogenic shock. We emphasize an early diagnosis by continuous electrocardiographic monitoring, serial electrocardiograms, echocardiography, serum determination of biochemical cardiac markers, radionuclide imaging and coronary angiography. The treatment includes continuous monitoring of cardiac rhythm, use of inotropic drugs, insertion of a catheter in the pulmonary artery for continuous assessment of cardiac output and, in extreme cases, the insertion of a contrapulsation balloon to maintain haemodynamics until improvement of cardiac function.

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