Design, Synthesis, and Evaluation of Probes for Spatially Resolved Imaging of Enantioselective Sulfoxide Reductases.

A novel concept of nonhydrolytic enzyme sensing based on aggregation-induced emission is described. As a proof of principle, fluorogenic probes for methionine sulfoxide reductases have been developed. Changes in the polarity and electronic nature upon reduction of sulfoxide to sulfide are translated to the aggregation potential of the probe.

Synthesis and Cytotoxic and Antiviral Profiling of Pyrrolo- and Furo-Fused 7-Deazapurine Ribonucleosides.

Three series of isomeric pyrrolo- and furo-fused 7-deazapurine ribonucleosides were synthesized and screened for cytostatic and antiviral activity. The synthesis was based on heterocyclizations of hetaryl-azidopyrimidines to form the tricyclic heterocyclic bases, followed by glycosylation and final derivatizations through cross-coupling reactions or nucleophilic substitutions. The pyrrolo[2',3':4,5]pyrrolo[2,3- d]pyrimidine and furo[2',3':4,5]pyrrolo[2,3- d]pyrimidine ribonucleosides were found to be potent cytostatics, whereas the isomeric pyrrolo[3',2',4,5]pyrrolo[2,3- d]pyrimidine nucleosides were inactive.

[REGRESSION OF LEFT VENTRICULAR HYPERTROPHY IN PATIENTS WITH ESSENTIAL HYPERTENSION AND LONG-TERM THERAPY WITH LOSARTAN].

In 106 patients with essential hypertension stage II losartan effectively lowers systolic and diastolic blood pressure during the day, thus contributing to the normalization of the circadian blood pressure profile in patients with initial breach, and does not affect the normal circadian rhythm. Long losartan promotes regression remodeling processes of cardiac muscle and reduce preload and afterload.