The pseudo-symmetric n-benzyl hydroxyethylamine core in a new series of heteroarylcarboxyamide hiv-1 pr inhibitors: Synthesis, molecular modeling and biological evaluation

Here, we report the synthesis, enzyme inhibition and structure–activity relationship studies of a new potent class of HIV-1 protease inhibitors, which contain a pseudo-symmetric hydroxyethylamine core and heteroarylcarboxyamide moieties. The simple synthetic pathway furnished nine compounds in a few steps with high yields. The compounds were designed taking into account our previous results on other series of inhibitors with different substituents at P’ and P” and different ways of linking them to the inhibitor core. Potent inhibitory activity was obtained with nanomolar IC50 values measured with a standard fluorimetric test in 100 mM MES buffer, pH 5.5, containing 400 mM NaCl, 1 mM EDTA, 1 mM DTT and 1 mg/mL BSA. Compounds 9a–c, containing the indole ring in P1, exhibited an HIV-1 protease inhibitory activity more powerful than darunavir in the same assay. To obtain molecular insight into the binding properties of these compounds, docking analysis was performed, and their binding properties were also compare

A capillary zone electrophoretic method for size characterization of gold nanoparticles

The unusual size dependent chemical and physical properties make nanoparticles attractive for quite different fields of applications1. The characterization of size distribution of solution grown nanoparticles is usually performed by dynamic light scattering and transmission electron microscopy2 (TEM). A method here is proposed for the separation of gold colloid standards, with core diameters ranging from 5 to 20 nm, using free solution capillary zone electrophoresis. The size characterization was possible by adding to the buffer poly(sodium 4-styrenesulfonate) which infers an “electrosteric” stabilization3 to colloids, exalting the difference in their electrophoretic mobilities. Applying a potential step for separation, a significant improvement was provided in terms of resolution between different sized colloids whose migration time varied linearly with particle diameter. A comparison with the size distribution derived by TEM allowed to assess that the electrophoretic profile is representative of the effective heterogeneity in size of each colloid sample. The practical utility of the method was demonstrated by measuring the size distribution of a home synthesized gold colloid which was in good agreement with the profile derived by TEM. 1. Daniel, M.C.; Astruc, D. Chem. Rev. 2004, 104, 293-346. 2. Henglein, A. J. Phys. Chem. 1993, 97, 5457-5471. 3. Pugh, T.L.; Heller, W. J. Polym. Sci. 1960, 47, 219-227

Regio- and Diastereo-Selective Biomimetic Synthesis of (+/-)-ε-Viniferin by NIS and Resveratrol

In this work, we describe the synthesis of (±)-permethylated-ϵ-viniferin from resveratrol by successive iodination, methylation and dehalogenation reactions. Iodination reaction by N-iodosuccinimide (NIS) was studied to optimize and confirm a proposed radical mechanism. Switching to acetyl protecting group, a new straightforward regio- and diastereo-selective biomimetic synthesis of (±)-ϵ-viniferin was obtained. Permethylated and free ϵ-viniferin were isolated up to 20 %yield

Regio- and diastereoselective organo-zinc promoted arylation of trans 2,3-diaryloxiranes by arylboronic acids: stereoselective access to trans 2,3-diphenyl-2,3-dihydrobenzofuran

Ortho-oxo substituted trans 2,3-diaryloxiranes were regio and stereoselective arylated by aryl zinc reagents, obtained from the corresponding boronic acids by B-Zn exchange. The reaction was quite general, irrespective to the aryl nucleophile and roceeded via a ring opening at the -carbon with respect to the substituted aryl ring. The stereoselectivity was from high to complete toward the alcohol resulted from retention of configuration at the electrophilic carbon. The method allowed a direct and high yielding access to trans 2,3-diphenyl-2,3-dihydrobenzofuran, which is a key structural motif in resveratrol dimers as viniferins. The use of enantioenriched starting diaryloxiranes resulted in no loss of stereochemical integrity in the final trans 2,3-dihydrobenzofuran, which was characterized for the first time in enantioenriched form

Analisi dei modelli organizzativi di risposta al COVID-19 in Italia: evidenze da 2 anni di ISTANT REPORT Altems

all’anno 2020 la storia dell’umanità ha dovuto fare i conti con la diffusione del Sars-COV-2 che ha generato in Italia, come in molti Paesi del pianeta una emergenza, sanitaria, sociale ed economica. L’Alta Scuola di Economia e Management dei Sistemi Sani- tari della Facoltà di Economia dell’Università Cattolica del Sacro Cuore, in collaborazione con il Dipartimento di Scienze della Vita e Sanità Pubblica (Sezione di Igiene) della Facoltà di Medicina e Chirurgia “A. Gemelli”, Cerismas (Centro di Ricerca e Studi in Management Sanitario), il Gruppo di Organizzazione Aziendale del DiGES Diparti- mento di Giurisprudenza, Economia e Sociologia dell’Università della Magna Graecia di Catanzaro, e il Centro di Ricerca sulla Leadership in Medicina della Facoltà di Medicina e Chirurgia “A. Gemelli” dell’Università Cattolica del Sacro Cuore, ha settimanalmente pubblicato un Report per analizzare in modo sistematico e comparativo i modelli di risposta adottati dalle Regioni in risposta all’emergenza Covid-19, partendo dall’analisi epidemiologica dell’evoluzione della pandemia. A due anni dal primo paziente in Italia con COVID-19 di Codogno, ALTEMS ha voluto elaborare un report che sintetizzasse tutti gli elementi che hanno composto la risposta alla diffusione del virus soffermandosi sui modelli istituzionali ed organizzativi adottati dalle Regioni italiane. Questa serie settimanale, che aveva già visto una Edizione Speciale dell’Instant Report a fine anno 2020 in prossimità dell’avvio della campagna vaccinale, viene presentata in forma diversa rispetto agli 85 report precedenti. Il presente Report è stato strutturato per fornire una sintesi di quanto accaduto negli ultimi 24 mesi fornendo una lettura complessiva degli eventi e delle modalità di risposta adottate dalle Regioni