Search results for "quinoline"

Molecular Classification of 5-Amino-2-Aroylquinolines and 4-Aroyl-6,7,8-Trimethoxyquinolines as Highly Potent Tubulin Polymerization Inhibitors

2013

Algorithms for classification and taxonomy are proposed based on criteria as information entropy and its production. It is classified a series of 5-amino-2-aroylquinolines (AAQs) and 4-aroyl-6,7,8-trimethoxyquinolines (TMQs) combretastatin analogues for anti-cancer activity. 5-Amino-6-methoxy-2-aroylquinoline AAQ showed anti-proliferative activity more potent as compared to combretastatin A-4 (CA4), against various human cancer cell lines and a multidrug resistance (MDR) cancer cell line. On the basis of AAQ/TMQ structure–activity relationship new derivatives are designed. The AAQs/TMQs are classified using nine characteristic chemical properties in molecules. Many classification algorithms…

Zinc(II) complexes of amide- and urea-substituted 8-hydroxyquinolines

2002

Abstract A series of amide- and urea-substituted 8-hydroxyquinoline ligands 1–6-H are used for the formation of zinc(II) complexes. Hereby in general 2:1 complexes are obtained and the X-ray structure of [(3)2Zn] reveals the presence of a coordination polymer in the solid state. Only the derivatives of 7-amino-8-hydroxyquinoline 4-H and 5-H form trinuclear hexa-helical 6:3 complexes which exhibit interesting structural and NMR and fluorescence spectroscopic properties.

A systematic comparison of kinetic modelling methods generating parametric maps for [11C]-(R)-PK11195

2006

[(11)C]-(R)-PK11195 is presently the most widely used radiotracer for the monitoring of microglia activity in the central nervous system (CNS). Microglia, the resident immune cells of the brain, play a critical role in acute and chronic diseases of the central nervous system and in host defence against neoplasia. The purpose of this investigation was to evaluate the reliability and sensitivity of five kinetic modelling methods for the formation of parametric maps from dynamic [(11)C]-(R)-PK11195 studies. The methods we tested were the simplified reference tissue model (SRTM), basis pursuit, a simple target-to-reference ratio, the Logan plot and a wavelet based Logan plot. For the reliabilit…

“Cysteinyl leukotriene-1 receptor activation in a human bronchial epithelial cell line leads to signal transducer and activator of transcription 1-me…

2008

Abstract We studied the effect of leukotriene D(4) (LTD(4)) on a human bronchial epithelial cell line (16HBE) overexpressing the cysteinyl leukotriene (CysLT) (1) receptor (HBECysLT(1)R), looking at the associated signal transduction mechanisms as well as at effects on inflammatory cell adhesion. The results obtained showed that LTD(4) increases the phosphorylation of extracellular signal-regulated protein kinase (ERK) 1/2 and of the signal transducer and activator of transcription 1 (STAT-1) in serine 727 (STAT-1Ser727), resulting in increased eosinophil adhesion to HBECysLT(1)R, associated with enhanced surface expression of intercellular adhesion molecule (ICAM) 1. Pretreatment with a Cy…

Randomized placebo-controlled trial comparing fluticasone aqueous nasal spray in mono-therapy, fluticasone plus cetirizine, fluticasone plus monteluk…

2004

BACKGROUND: Corticosteroids are considered to be particularly effective in reducing nasal congestion and are therefore recommended as first-line treatment in allergic rhinitis patients with moderate to severe and/or persistent symptoms. OBJECTIVE: We compared the clinical efficacy of fluticasone propionate aqueous nasal spray (FPANS) 200 microg given once daily, administered in mono-therapy or combined therapy with a H1 receptor antagonist (cetirizine, CTZ) or with a leukotriene antagonist (montelukast, MSK), and the combined therapy of CTZ plus MSK in the treatment of patients affected by allergic rhinitis to Parietaria during natural pollen exposure. In addition, we examined the effect of…

Safety and efficacy of montelukast as adjunctive therapy for treatment of asthma in elderly patients

2013

Asthma is a disease of all ages. This assumption has been challenged in the past, because of several cultural and scientific biases. A large body of evidence has accumulated in recent years to confirm that the prevalence of asthma in the most advanced ages is similar to that in younger ages. Asthma in the elderly may show similar functional and clinical characteristics to that occurring in young adults, although the frequent coexistence of comorbid conditions in older patients, together with age-associated changes in the human lung, may lead to more severe forms of the disease. Management of asthma in the elderly follows specific guidelines that apply to all ages, although most behaviors ar…

Effects of exercise training and montelukast in children with mild asthma

2008

Data from the general population suggest that habitual exercise decreases bronchial responsiveness, but the possible role of exercise in asthmatics is undefined. The leukotriene receptor antagonist montelukast decreases bronchial responsiveness and exercise-induced symptoms in asthmatic children. This randomized study in children with mild asthma evaluated the combined effects of aerobic training for 12 wk and montelukast or placebo on bronchial responsiveness (BHR) to methacholine, exercise-induced bronchoconstriction (EIB), inflammatory markers in exhaled breath condensate (EBC), and asthma exacerbations.Fifty children (mean age +/- SD: 10.2 +/- 2.4 yr) with mild stable asthma were random…

Can the response to Omalizumab be influenced by treatment duration? A real-life study

2017

Objective It is unknown whether Omalizumab effectiveness changes over the course of time. Our retrospective real-life study tried to analyze whether Omalizumab response may be influenced by treatment duration. Methods 340 severe asthmatics treated with Omalizumab for different periods of time were recruited. They were subdivided into 4 groups according to the Omalizumab treatment length: 60 months. Omalizumab treatment results (FEV1, exacerbations, ACT, SABA use, asthma control levels, medications used e and ICS doses) were compared. Results ACT, exacerbations, GINA control levels, ICS doses and SABA use were similar in all groups with different Omalizumab treatment durations. Using a linea…

Anti-inflammatory medications for the treatment of pediatric obstructive sleep apnea

2020

Efficacy, tolerability, and safety of montelukast versus finasteride for the treatment of moderate acne in women: A prospective, randomized, single-b…

2021

Background Acne is a chronic inflammatory skin disease which involves the pilosebaceous unit. Tissue inflammation isone of the crucial mechanisms, amongst others. Of the various cytokines, leukotriene B4 (LT-B4) is the most potentleucocyte chemotactic mediator. Montelukast is an antagonist of the LT-B4 receptor. Finasteride is an antiandrogen whichspecifically inhibits the 5α-reductase enzyme. Aims This study aimed at comparing the efficacy, tolerability and safety of montelukast versus finasteride in the treatmentof moderate acne in women. Patients/method This randomized, single-blinded, prospective trial over 12 weeks recruited 65 female subjects with moderate acne vulgaris (Global Acne G…