1,721,026 research outputs found

    Recent advances in urea- And thiourea-containing compounds: focus on innovative approaches in medicinal chemistry and organic synthesis

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    Urea and thiourea represent privileged structures in medicinal chemistry. Indeed, these moieties constitute a common framework of a variety of drugs and bioactive compounds endowed with a broad range of therapeutic and pharmacological properties. Herein, we provide an overview of the state-of-the-art of urea and thiourea-containing pharmaceuticals. We also review the diverse approaches pursued for (thio)urea bioisosteric replacements in medicinal chemistry applications. Finally, representative examples of recent advances in the synthesis of urea- and thiourea-based compounds by enabling chemical tools are discussed

    Inhibitory effects of 1-deazaadenosine analogs of HIV replication and adenosine deaminase

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    A series of 2',3'-dideoxy-N6-(cyclo)alkyl-1-deazaadenosine derivs. were synthesized starting from 2,6-dichloro-1-deazapurine. The new nucleosides proved to be good inhibitors of HIV-1 replication, the most active being 2',3'-dideoxy-2-chloro-N6-cycloctyl-1-deazaadenosine (ED50 = 0.4 μM)

    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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