1,720,993 research outputs found

    A long-term prospective follow-up study of incident RLS in the course of chronic DAergic therapy in newly diagnosed untreated patients with Parkinson's disease

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    It is currently controversial if and in which terms Parkinson's disease (PD) and restless legs syndrome (RLS) are linked in co-morbid association. In a cohort of 106 de novo PD patients (67 male and 39 female, aged 42-83 years), 15 of them developed RLS, which was prospectively assessed at 6-month intervals from the starting of dopamine(DA)ergic therapy. The incidence rate of total RLS was 47 per 1,000 case/person per year and 37 per 1,000 case/person per year after the exclusion of possible "secondary" forms of the disorder (n = 3). These figures are higher than those reported in an incidence study conducted in German general population (Study of Health in Pomerania), in which the method of ascertainment of RLS similar to ours has been used. An incidence rate of total RLS significantly higher than that reported in the above-mentioned study was found in the age ranges 55-64 years and in the age range 45-74 years standardized to European general population 2013 (70 and 53 per 1,000 case/person per year, respectively, p < 0.01). Ten out of 12 patients (83.3 %) developed RLS within 24 months from the starting of DAergic medication (median latency 7.5 months). These findings support the view that sustained DAergic therapy could represent the critical factor inducing an increased incidence of RLS in patients with PD and that the latter disease should be regarded as the condition predisposing to the occurrence of the former and not viceversa as previously hypothesized. The mechanism underlying the increased incidence of RLS remains unclear and deserves further investigation

    Labeling Deoxyadenosine for the Preparation of Functional Conjugated Oligonucleotides

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    Herein we present a versatile synthetic method for the 8-​thioalkylation of (deoxy)​adenosine with a short carbon linker having on the other side a variety of mols. (psoralen, acridine) and functional groups (alkyne)​. After conventional protections, the modified adenosine can be phosphytylated and inserted into an oligonucleotide without affecting the std. protocols for supported oligonucleotide synthesis. The hybridization properties of a generic oligonucleotide contg. the above conjugated moieties toward both DNA and RNA are evaluated both in the case of a perfectly complementary strand and in the case of a single mismatch. This methodol. is suitable for the prepn. of several types of derivs. and-​through the alkynyl moiety-​provides fast access to click-​chem. transformations

    Molecular Hybridization as a Strategy for Developing Artemisinin-Derived Anticancer Candidates

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    Artemisinin is a natural compound extracted from Artemisia species belonging to the Asteraceae family. Currently, artemisinin and its derivatives are considered among the most significant small-molecule antimalarial drugs. Artemisinin and its derivatives have also been shown to possess selective anticancer properties, however, there are several limitations and gaps in knowledge that retard their repurposing as effective anticancer agents. Hybridization resulting from a covalent combination of artemisinin with one or more active pharmacophores has emerged as a promising approach to overcome several issues. The variety of hybridization partners allows improvement in artemisinin activity by tuning the ability of conjugated artemisinin to interact with various molecule targets involved in multiple biological pathways. This review highlights the current scenario of artemisinin-derived hybrids with potential anticancer activity. The synthetic approaches to achieve the corresponding hybrids and the structure–activity relationships are discussed to facilitate further rational design of more effective candidates

    Bile Acid Conjugates with Anticancer Activity: Most Recent Research

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    The advantages of a treatment modality that combines two or more therapeutic agents in cancer therapy encourages the study of hybrid functional compounds for pharmacological applications. In light of this, we reviewed recent works on hybrid molecules based on bile acids. Due to their biological properties, as well as their different chemical/biochemical reactive moieties, bile acids can be considered very interesting starting molecules for conjugation with natural or synthetic bioactive molecules

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
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