Enhanced dissolution of poorly soluble antiviral drugs from nanoparticles of cellulose acetate based solid dispersion matrices

Polysaccharide-based polymers were used to produce nanoparticles of poorly soluble antiviral drugs using a rapid precipitation process. The structure-property relationships of four novel cellulose acetate-based polymers were studied for their solubility enhancement of poorly soluble drugs. Particles were purified by dialysis, and dried powders were recovered after freeze-drying. The particle diameters were 150–200 nm. The target drug loading in the particles was 25 wt%, and the drug loading efficiencies were 80–96%. The effects of the formulation process and nanoparticle properties on drug solubility were investigated. All nanoparticles afforded increased solubility and faster release compared to pure drugs. Drug release was a function of the relative hydrophobicity (or solubility parameters) of the polymers

An appraisal of pancreatic cyst fluid molecular markers

Pancreatic malignancy is the third leading cause of cancer related death in the United States with limited viable screening options. By the end of this decade, cancers are poised to become the leading cause of death with pancreatic cancer projected to be the second leading cause of cancer related mortality. Pancreatic cystic lesions (PCLs) are found in approximately 5%–14% of patients due to the increased utilization of cross-sectional imaging, with approximately 8%–10% of pancreatic cancers originating as PCLs. Current screening guidelines have shown discrepancies between morphologic characteristics of PCLs and identifying advanced pancreatic disease. Molecular analysis has emerged as a novel technology to aid in adequate diagnosis and management decisions of PCLs. Mucinous cysts including intraductal papillary mucinous neoplasms (IPMNs) or mucinous cystic neoplasms have similar oncogenic mutations including KRAS, TP53, SMAD4, PIK3CA, PTEN, or CKDN2A, while GNAS and RNF43 mutations are specific only to IPMNs. Serous cystadenomas have been associated with a loss of tumor suppressor gene VHL, while solid-psuedopapillary neoplasms have an oncogenic mutation CTNNB1. A specific molecular marker to diagnose existing high-grade dysplasia or impending malignant transformation is yet to be identified. Moving forward it is important to advance technology in isolating and identifying high-risk molecular markers from cyst fluid while considering their increased utilization in the evaluation of PCLs

Synthesis of 3-(3-(Phenacyl/Alkyl/Benzylthio)-[1,2,4]Triazolo[3,4-B][1,3,4]Thiadiazol-6-Yl)-2<i>H</i>-Chromen-2-Ones

<div><p></p><p>Reaction of coumarin-3-carboxylic acid with 3,5-di mercapto-4-amino-s-triazole in POCl₃to generate 3-(3-mercapto-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)-2H-chromen-2-one (<b>3</b>). Reaction of <b>3</b> with different substituted phenacyl/benzyl/allyl bromides in anhydrous ethanol gave corresponding 3-(3-(phenacyl/alkyl/benzylthio)-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazol-6-yl)-2H-chromen-2-ones <b>5</b>. The structures of newly prepared compounds were confirmed by their analytic and spectral data.</p> </div

One-pot synthesis of bis (phenylimino dihydro thiazolyl-2<i>H</i>-chromene) derivatives

<p>A novel series of bis (phenylimino dihydro thiazolyl-2<i>H</i>-chromene) derivatives have been synthesized through an efficient one-pot multicomponent approach involving different substituted of 3-(2-bromoacetyl)-2<i>H</i>-chromen-2-ones, phenyl isothiocyanates and <i>para</i>-phenylenediamine in presence of dimethylformamide solvent. The target compounds were obtained in a shorter reaction time through simple reaction work up with good yields. All the synthesized products were characterized by their spectral and analytical data like IR, ¹H NMR, ¹³C NMR, Roesy, and mass spectral data.</p

Novel multicomponent synthesis of 2-OXO-1, 2-diphenylethylidene hydrazinyl thiadiazinyl-2<i>H</i>-chromen-2-one derivatives

<p></p> <p>A series of novel 2-oxo-1,2-diphenylethylidene hydrazinyl thiadiazinyl-2<i>H</i>-chromen-2-ones (shown in <a href="#c0001" target="_blank">Scheme 1</a>) have been synthesized via multicomponent approach by the reaction of equimolar amount of benzil (1), thiocarobohydrazide (2), and substituted of 3-(2-bromoacetyl)-2<i>H</i>-chromen-2-ones (3a-i) in a shorter reaction time with good yields. All these compounds were characterized by their spectral and analytical data like IR, ¹H NMR, ¹³C NMR, and mass spectra.</p

Bis coumarinyl bis triazolothiadiazinyl ethane derivatives: Synthesis, antiviral activity evaluation, and molecular docking studies

© 2018 Taylor & Francis. A series of novel 3,3′-(3,3′-(dihydroxy/hydroxyethane-1,2-diyl)bis(7H-[1,2,4]triazolo[3,4-b]triazolo[3,4-b[1,3,4]thiadiazine-6,3-diyl))bis(2H-chromen-2-ones) were prepared by the condensation of thiocarbohydrazide with tartaric acid or malic acid followed by various 3-(2-bromoacetyl)-2H-chromen-2-ones in two steps with good yields. All the synthesized compounds were characterized by analytical and spectral (IR, 1H NMR, 13C NMR, and mass) data. These synthesized bis(triazolothiadiazinyl coumarin) compounds were evaluated for broad spectrum of antiviral activity. Among all the tested compounds, compound 5f exhibited antiviral activity against H1N1 virus. The molecular docking studies of these compounds against H1N1 neuraminidase enzyme were performed. The binding affinity and binding values were compared with standard drugs.status: publishe

Bis coumarinyl bis triazolothiadiazinyl ethane derivatives: Synthesis, antiviral activity evaluation, and molecular docking studies

<p>A series of novel 3,3′-(3,3′-(dihydroxy/hydroxyethane-1,2-diyl)bis(7<i>H</i>-[1,2,4]triazolo[3,4-<i>b</i>][1,3,4]thiadiazine-6,3-diyl))bis(2<i>H</i>-chromen-2-ones) were prepared by the condensation of thiocarbohydrazide with tartaric acid or malic acid followed by various 3-(2-bromoacetyl)-2<i>H</i>-chromen-2-ones in two steps with good yields. All the synthesized compounds were characterized by analytical and spectral (IR, ¹H NMR, ¹³C NMR, and mass) data. These synthesized bis(triazolothiadiazinyl coumarin) compounds were evaluated for broad spectrum of antiviral activity. Among all the tested compounds, compound <b>5f</b> exhibited antiviral activity against H1N1 virus. The molecular docking studies of these compounds against H1N1 neuraminidase enzyme were performed. The binding affinity and binding values were compared with standard drugs.</p