Formamidines with antinociceptive and antiinflammatory activities

Pursuing our investigations on 7-amino-2,3-polymethyleneindole derivatives, a set of 7-(dimethylaminomethylene)-amino-2,3-polymethyleneindoles, together with some other aryl or cycloalkyl substituted formamidines, were prepared and tested for analgesic and antiinflammatory activities. Several compounds resulted endowed with one or both of these activities; the indole derivatives 1 and 2 exhibited a good degree of both of them

Amides and formamidines with antinociceptive activity: note II

Forty amides, formamidines and trifluoromethylsulfonylamides bearing on the nitrogen a cyclohexyl residue, eventually 2-substituted, were prepared and tested for analgesic activity against a chemical stimulus. Good activity was exhibited by amides 9, 11 and 28, by formamidine 34, as well as by triflyamide 40. Eleven additional compounds exhibited a moderate activity

Fungicidal activity of some o-nitrophenyl-hydrazones

The antimycotic activity of 16 o-nitrophenylhydrazones against strains of Hansenula anomala, Saccharomyces cerevisiae, Candida parapsyliosis, and Cryptococcus albidus was tested. All 16 compounds inhibited growth of the yeast strains. The inhibitory activity of the 4 methyl-derivatives substituted on the aromatic nucleus was particularly significant

Sintesi di nuovi singoli isomeri di -ciclodestrina neutri e carichi negativamente quali selettori chirali in elettroforesi capillare

In questo studio sono stati sintetizzati diversi derivati delle Ciclodestrine (CD) come singoli isomeri sia neutri che anionicamente derivatizzati utilizzando due diversi approcci sintetici uno di selettiva protezione e l'altra di selettiva attivazione dei gruppi funzionali presenti nella struttura CD

Variabilità dell'olio essenziale di <i>Helichrysum italicum</i> (Roth) G. Don

Per lo studio dell'olio essenziale di Helichrysum italicum, sono state prese in considerazione varie stazioni di E. italicum (Roth) G. Don subsp. microphyllum (Willd.) Nyman vegetante allo stato spontaneo sia nel Nord che nel Sud della Sardegna. Le analisi sono state condotte via Gas-massa e ci hanno permesso di identificare 69 costituenti per un totale compreso tra il 92.9% ed il 99.9% dei costituenti totali

Variabilità dell'olio essenziale di <i>Thymus herba-barona</i> Loisel e sue proprietà antibatteriche

La Famiglia delle Labiatae include 350 specie di cui 66 vivono spontanee in Europa in particolare in Sardegna è da annoverare la presenza di un endemismo Sardo-Corso, Thymus herbabarona Loisel. Di questa pianta è stata studiata la composizione dell'olio essenziale e la sua variabilità  prendendo in considerazione varie stazioni del nord Sardegna. Le analisi sono state effettuate sia via Gas-massa che NMR. Da un primo studio si nota che sono presenti fondamentalmente due chemotipi uno a carvacrolo e l'altro a timolo tra questi il più diffuso è il chemotipo a carvacrolo sostanza presente in una concentrazione superiore al 70% con solo tracce di timolo mentre il chemotipo a timolo (29%) presenta anche una buona percentuale di carvacrolo (26%)

Serial Ultrasound Assessment of Diaphragmatic Function and Clinical Outcome in Patients with Amyotrophic Lateral Sclerosis.

Background: Ultrasound (US) evaluation of the diaphragm may be a non-volitional useful tool in the clinical management of patients with ALS. Aim of the present study was then to evaluate the impact of serial assessment of ΔTmax index on clinical outcomes during the follow-up in these patients and to correlate non-volitional US indices and other volitional measures with these outcomes. Methods: A cohort of 39 consecutive patients with ALS was followed up to 24 months. At baseline and every 3-month spirometry (forced vital capacity-FVC), sniff inspiratory nasal pressure (SNIP), and US of the diaphragm (ΔTdi and ΔTmax) were recorded. These parameters were correlated with clinical outcomes (hypercapnia, nocturnal hypoventilation, NIV start in the following 6 month, and death within 1 year). Results: The occurrence of ΔTmax &gt;0.75 during follow-up increased the risk for NIV (HR=5.6, p=0.001) and death (HR=3.7, p=0.0001) compared with patients with stable lower values. The evidence of diaphragmatic dysfunction, i.e. ΔTmax &gt;0.75, occurs 3.2 month earlier than the onset of NIV. Moreover, ΔTmax &gt;0.75 correlated with onset of nocturnal hypoventilation, NIV initiation within 6 months, and death within 12 months, similarly to FVC &lt;50% predicted and better than other functional indices. Conclusions: Serial monitoring of diaphragmatic ΔTmax by US may be useful to predict initiation of NIV and death in patients with ALS. The occurrence of an abnormal ΔTmax value in the follow-up precedes the decision for starting NIV

Acute exacerbation of idiopathic pulmonary fibrosis: Lessons learned from acute respiratory distress syndrome?

Idiopathic pulmonary fibrosis (IPF) is a fibrotic lung disease characterized by progressive loss of lung function and poor prognosis. The so-called acute exacerbation of IPF (AE-IPF) may lead to severe hypoxemia requiring mechanical ventilation in the intensive care unit (ICU). AE-IPF shares several pathophysiological features with acute respiratory distress syndrome (ARDS), a very severe condition commonly treated in this setting. A review of the literature has been conducted to underline similarities and differences in the management of patients with AE-IPF and ARDS. During AE-IPF, diffuse alveolar damage and massive loss of aeration occurs, similar to what is observed in patients with ARDS. Differently from ARDS, no studies have yet concluded on the optimal ventilatory strategy and management in AE-IPF patients admitted to the ICU. Notwithstanding, a protective ventilation strategy with low tidal volume and low driving pressure could be recommended similarly to ARDS. The beneficial effect of high levels of positive end-expiratory pressure and prone positioning has still to be elucidated in AE-IPF patients, as well as the precise role of other types of respiratory assistance (e.g., extracorporeal membrane oxygenation) or innovative therapies (e.g., polymyxin-B direct hemoperfusion). The use of systemic drugs such as steroids or immunosuppressive agents in AE-IPF is controversial and potentially associated with an increased risk of serious adverse reactions. Common pathophysiological abnormalities and similar clinical needs suggest translating to AE-IPF the lessons learned from the management of ARDS patients. Studies focused on specific therapeutic strategies during AE-IPF are warranted

Nuovi derivati 1,2-difenil-imidazolici come potenti ed efficaci modulatori allosterici positivi del recettore GABA_A

Il complesso recettoriale GABAA è il più importante recettore inibitorio presente nel sistema nervoso centrale dei vertebrati. Il legame dell’acido γ-aminobutirrico (GABA) ai recettori GABAA induce l’apertura di un intrinseco canale al Cl- con conseguente iperpolarizzazione e inibizione della cellula. Recentemente presso i nostri laboratori abbiamo sviluppato una serie di 1,2-difenilimidazol-piperazine dotate di significativa affinità di legame per i recettori dopaminergici D2- simili, serotoninergici 5-HT1A e 5-HT2A. La nostra attenzione si è focalizzata sulla capacità di alcuni derivati di inibire in modo concentrazione-dipendente (0.1-300 µM) le correnti al Cl- evocate dal GABA su recettori GABAA umani espressi in oociti di Xenopus