Novel Lipophilic Acetohydroxamic Acid Derivatives Based on Conformationally Constrained Spiro Carbocyclic 2,6-Diketopiperazine Scaffolds with Potent Trypanocidal Activity

We describe novel acetohydroxamic acid derivatives with potent activity against cultured bloodstream-form Trypanosoma brucei and selectivity indices of >1000. These analogues were derived from conformationally constrained, lipophilic, spiro carbocyclic 2,6-diketopiperazine (2,6-DKP) scaffolds by attaching acetohydroxamic acid moieties to the imidic nitrogen. Optimal activity was achieved by placing benzyl groups adjacent to the basic nitrogen of the 2,6-DKP core. S-Enantiomer 7d was the most active derivative against T. brucei (IC(50) = 6.8 nM) and T. cruzi (IC(50) = 0.21 μM)

Novel Lipophilic Acetohydroxamic Acid Derivatives Based on Conformationally Constrained Spiro Carbocyclic 2,6-Diketopiperazine Scaffolds with Potent Trypanocidal Activity

We describe novel acetohydroxamic acid derivatives with potent activity against cultured bloodstream-form <i>Trypanosoma brucei</i> and selectivity indices of >1000. These analogues were derived from conformationally constrained, lipophilic, spiro carbocyclic 2,6-diketopiperazine (2,6-DKP) scaffolds by attaching acetohydroxamic acid moieties to the imidic nitrogen. Optimal activity was achieved by placing benzyl groups adjacent to the basic nitrogen of the 2,6-DKP core. <i>S</i>-Enantiomer <b>7d</b> was the most active derivative against <i>T. brucei</i> (IC₅₀ = 6.8 nM) and <i>T. cruzi</i> (IC₅₀ = 0.21 μM)

Indoor Air Quality Evaluation Using Mechanical Ventilation and Portable Air Purifiers in an Academic Dentistry Clinic during the COVID-19 Pandemic in Greece

The coronavirus disease 2019 (COVID-19), which is mainly transmitted through droplets without overlooking other sources of transmission, rendered attention on the air quality in indoor areas and more specifically in healthcare settings. The improvement of indoor air quality (IAQ) is ensured by frequent changes of the air that must be carried out in healthcare areas and with assistance from special devices that undertake the filtration of the air and its purification through special filters and lamps. In this research, the performance of air purifiers is assessed in terms of the limitation of PM2.5, PM10, VOCs and CO2 in a postgraduate clinic of the Dentistry School of the National and Kapodistrian University of Athens in parallel with mechanical ventilation. Our findings indicate that the use of mechanical ventilation plays a key role on the results, retaining good IAQ levels within the clinic and that air purifiers show a positive impact on IAQ by mainly reducing the levels of PM2.5 and secondly of TVOC