Search results for "Drugs"

Micelles of hyaluronic acid-hexadecylamine derivatives for ocular release of hydrophobic drugs

2016

Anti-adhesion agents against Gram-positive pathogens

2014

The rise of antibiotic-resistance as well as the deficiency of investments by pharmaceutical companies in the development of new antibiotics, have stimulated the investigation of alternative strategies to conventional antibiotics for counteracting the pathogens. A fundamental step of Gram positive pathogenesis is the bacterial adhesion to the host tissue involving a direct and a specific interaction between bacterial surface molecules and host ligands. Targeting the adhesion is a good strategy to design novel anti-infective drugs agents useful to interfere with the pathogenic process and with a virulence mechanism as biofilm formation. This review is focused on anti-virulence compounds whic…

Epidemiological cutoff values for fluconazole, itraconazole, posaconazole, and voriconazole for six Candida species as determined by the colorimetric…

2013

ABSTRACT In the absence of clinical breakpoints (CBP), epidemiological cutoff values (ECVs) are useful to separate wild-type (WT) isolates (without mechanisms of resistance) from non-WT isolates (those that can harbor some resistance mechanisms), which is the goal of susceptibility tests. Sensititre YeastOne (SYO) is a widely used method to determine susceptibility of Candida spp. to antifungal agents. The CLSI CBP have been established, but not for the SYO method. The ECVs for four azoles, obtained using MIC distributions determined by the SYO method, were calculated via five methods (three statistical methods and based on the MIC 50 and modal MIC). Respectively, the median ECVs (in mg/lit…

Documento de consenso sobre el tratamiento antimicrobiano de las infecciones bacterianas odontogénicas

2005

Las infecciones de la cavidad bucal son un problema de salud pública frecuente y motivo constante de prescripción antibiótica; el 10% de los antibióticos se emplean para tratar este problema. Sin embargo, hasta la fecha son pocos los estudios realizados para determinar su incidencia. Asímismo, su relación con ciertas enfermedades sistémicas (cardiacas, endocrinas, etc...) confiere a estas patologías una importancia vital. A pesar de la reconocida frecuencia e importancia de las infecciones odontogénicas, llama la atención la actual dispersión de criterio en varios aspectos referentes a su clasificación, terminología y recomendaciones terapéuticas. El objetivo principal de este documento, re…

Occurrence and transformation of illicit drugs in wastewater treatment plants.

2016

Illicit drugs (IDs) and their metabolites have been recently recognized as a new group of water emerging contaminants (ECs) with potent psychoactive properties and unknown effects to the aquatic environment (Pal et al., 2013). IDs are excreted via urine and feces and arrive at wastewater treatment plants (WWTPs) where can reach ppb levels (Castiglioni et al., 2006). Over the past few years, it has been demonstrated that conventional biological processes in WWTPs are not or scarcely able to remove IDs. Thus, they are discharged into water bodies through the treated effluent (Postigo et al., 2011). Therefore, monitoring the IDs concentration in WWTPs can have a twofold advantage: i. increase …

Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-…

2012

Abstract A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)-yl]ethan/propanamide derivatives was synthesized and characterized by 1H, 13C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N-(1,3-benzothiazol-2-yl)-2-[3,4-dihydroisoquinolin-2(1H)-yl]ethanamide is reported to determine its conformational feature. The investigated compounds were found to be active in psychotropic in vivo, anti-inflammatory in vivo and cytotoxicity in vitro screening. They possess marked sedative action, reveal high anti-inflammatory activity, have selective cytotoxic effects and NO-induction ability concerning tumour cell lines. Some of the compounds synthesi…

Polymeric prodrug for release of an antitumoral agent by specific enzymes.

2001

The clinical usefulness of antitumor chemotherapy has been strongly limited by the lack of specificity of most anticancer drugs, which act also against healthy cells. The aim of this work was to design, synthesize, and evaluate a macromolecular prodrug of Cytarabine, a known antitumor drug, which is a specific substrate for plasmin enzyme whose concentration is high in various kinds of tumor mass as a result of plasminogen activator secretion. alpha,beta-Poly(N-hydroxyethyl)-DL-aspartamide (PHEA), a known synthetic and biocompatible polyamino acid, was used as a drug carrier, and Cytarabine was linked to PHEA by D-Val-Leu-Lys spacer synthesized beginning from Cbz-D-Val-LeuOH dipeptide and N…

3-Aryl-2-[1H-benzotriazol-1-yl]acrylonitriles: a novel class of potent tubulin inhibitors.

2011

During a screening for compounds that could act against Mycobacterium tuberculosis, a series of new cellular antiproliferative agents was identified. The most cytotoxic molecules were evaluated against a panel of human cell lines derived from hematological and solid human tumors. In particular, (E)-2-(1H-benzo[d] [1,2,3]triazol-1-yl)-3-(4-methoxyphenyl)acrylonitrile (1) was found to be of a potency comparable to etoposide and greater than 6-mercaptopurine in all cell lines tested. Accordingly, a synthesis of a new series of (E)-2-(5,6-dichloro-1H-benzo[d] [1,2,3]triazol-1-yl)-3-(4-R-phenyl)acrylonitriles was conducted in order to extend the studies of structure-activity relationship (SAR) f…

Interleukin-6 and Soluble Interleukin-6 Receptor: Direct Stimulation of gp130 and Hematopoiesis

1998

T HE INTERLEUKIN-6 (IL-6) family of cytokines acts via receptor complexes that contain at least one subunit of the signal transducing protein gp130.[1][1] The family comprises IL-6, IL-11, ciliary neurotrophic factor (CNTF), cardiotrophin-1 (CT-1), leukemia inhibitory factor (LIF), and oncostatin M

Reaction of 3-Amino-1,2,4-Triazole with Diethyl Phosphite and Triethyl Orthoformate: Acid-Base Properties and Antiosteoporotic Activities of the Prod…

2017

The reaction of diethyl phosphite with triethyl orthoformate and a primary amine followed by hydrolysis is presented, and the reaction was suitable for the preparation of (aminomethylene)bisphosphonates. 3-Amino-1,2,4-triazole was chosen as an interesting substrate for this reaction because it possesses multiple groups that can serve as the amino component in the reaction-namely, the side-chain and triazole amines. This substrate readily forms 1,2,4-triazolyl-3-yl-aminomethylenebisphosphonic acid (compound 1) as a major product, along with N-ethylated bisphosphonates as side products. The in vitro antiproliferative effects of the synthesized aminomethylenebisphosphonic acids against J774E m…