Novel Series of [ddN]-[TSAO-T] Heterodimers as Potential Bi-Functional Inhibitors of HIV-1 RT. Studies in the Linker and ddN Region

Abstract

Novel series of [ddN]-(CH₂)_n-[TSAO-T] heterodimers have been prepared and tested for their anti-HIV-1 and HIV-2 activity. The most active compound of this series was the [d4T]-(CH₂)₃-[TSAO-T] heterodimer (EC₅₀ = 0.018 ± 0.03 μM).     

A New Synthesis of 2′,3′-Didehydro-3′-deoxy-3-Alkylthymidine

Abstract

The preparation of 3-alkyl D4T derivatives has been carried out starting from the corresponding 5′-O-t-butyldimethylsilyl-3′-O-methanesulfonylthymidine 2 by way of deprotection-elimination and succesive alkylation reactions.     

Synthesis and Biological Activity of Some 2-Aminopurine Carbonucleosides

Abstract

A series of new o ne t wo subtituted c arbonucleoside analogues (OTC) of purine was synthesized and evaluated against cytomegalovims and varicella-zoster virus in human embryonic lung (HEL) cells.     

Synthesis and Cytostatic Activity of Halomethylthiazole C-Nucleosides and Analogues1

Abstract

The synthesis of 2-(β-D-ribofuranosyl)-and 2-(tetrahydropyran-2-yl)-4-halomethylthiazoles from 2, 5-anhydro-D-allonthioamide and tetrahydropyran-2-thiocarboxamide is described. Bromination of 2-(β-D-ribofuranosyl)- and 2-tetrahydropyran-2-yl)-4-methylthiazole with NBS is studied. Cytostatic activity against HeLa cells of all the compounds is reported.     

Free radical scavenging activity,total phenolic content,total antioxidant status,and total oxidant status of endemic Thermopsis turcica

Thermopsis turcica, endemic to Turkey, is in danger of extinction. Studies on this species are very few due to the fact that it was only discovered in 1983 and grows in a small circumscribed area in Turkey. In this study, free radical scavenging activity, total phenolic content, total oxidant status (TOS), and total antioxidant status (TAS) of methanol (TTM) and acetone (TTA) extracts of T. turcica were measured spectroscopically. Free radical scavenging activity was determined according to the elimination of DPPH radicals and total phenol content was determined by the Folin–Ciocalteu reaction. Total oxidant status (TOS) and total antioxidant status (TAS) were measured with commercially available kits. Methanol and acetone extracts of T. turcica were found to have a specific radical scavenging effect. This effect was found to be related to the total phenolic content of the extracts. Since the TTA had a higher phenolic content than the methanol extract, it had a stronger radical scavenging effect. In addition, the total antioxidant capacity of the methanol extract was observed to be higher than that of its acetone counterpart. As a result, due to its antioxidative properties, T. turcica is thought to be a natural source of antioxidants.     

A?new species of the genus Duvalius sg. Neoduvalius from Montenegro with taxonomical remarks on the genus Duvalius (Coleoptera,Carabidae, Trechini)

Duvalius (sg. Neoduvalius) gejzadunayi sp. n. from Pećina u Dubokom potoku cave ( Donje Biševo village near Rožaje, Montenegro), the first known representative of this subgenus from the territory of Montenegro is described, illustrated and compared with the related species of the subgenus Neoduvalius Müller, 1913. This new species is characterised by depigmented, medium sized body, totally reduced eyes, deep and complete frontal furrows, 3–4 pairs of discal setae in third elytral stria, as well as by the shape of aedeagus. Data on the distribution and the ecology of this remarkable species, as well as a check-list of the subgenus Neoduvalius are also provided. Recently described genera Serboduvalius Ćurčić, S. B. Pavićević & Ćurčić, B.P.M., 2001, Rascioduvalius Ćurčić, S. B. Brajković, Mitić & Ćurčić, B.P.M., 2003, Javorella Ćurčić, S. B. Brajković, Ćurčić, B.P.M. & Mitić, 2003 and Curcicia Ćurčić, S. B. & Brajković, 2003 are regarded as junior synonyms of the genus Duvalius Delarouzée.     

De Novo Assembly and Functional Annotation of the Olive (Olea europaea) Transcriptome

Olive breeding programmes are focused on selecting for traits as short juvenile period, plant architecture suited for mechanical harvest, or oil characteristics, including fatty acid composition, phenolic, and volatile compounds to suit new markets. Understanding the molecular basis of these characteristics and improving the efficiency of such breeding programmes require the development of genomic information and tools. However, despite its economic relevance, genomic information on olive or closely related species is still scarce. We have applied Sanger and 454 pyrosequencing technologies to generate close to 2 million reads from 12 cDNA libraries obtained from the Picual, Arbequina, and Lechin de Sevilla cultivars and seedlings from a segregating progeny of a Picual × Arbequina cross. The libraries include fruit mesocarp and seeds at three relevant developmental stages, young stems and leaves, active juvenile and adult buds as well as dormant buds, and juvenile and adult roots. The reads were assembled by library or tissue and then assembled together into 81 020 unigenes with an average size of 496 bases. Here, we report their assembly and their functional annotation.     

Genetic characterization of the invasive mosquitofish (Gambusia spp.) introduced to Europe: population structure and colonization routes

Biological invasions are considered one of the main anthropogenic factors that reduce the abundance of native species. Understanding the patterns of population structure and behavior of introduced species is important to determine invasion sources and pathways, in addition to improving the protective management of native species. Thus, we set out to advance our knowledge about the mosquitofish Gambusia spp., which is an invasive species that was introduced to southern Europe in 1921 to control mosquito populations. We assessed the genetic diversity and population structure of this species at 13 European locations, by screening variation at six microsatellite loci. We also evaluated six American samples (four of G. holbrooki and two of G. affinis) to identify the most likely source of the populations that established in Europe, and to determine whether G. affinis is also present. The results showed that, while there was evidence of recent bottleneck events in a few isolated locations, most introduced populations harbored a considerable amount of gene diversity, probably because of multiple introductions and secondary contacts. Populations displayed strong genetic differentiation that was mainly associated with geographical distance. At least two main routes of colonization of G. holbrooki seem to have occurred in Europe. The first, and more ancient colonization, was consistent with historical records, with the species invading the Iberian Peninsula. A second and more recent colonization probably occurred in Greece and, from there, France. The presence of G. affinis was not detected in any of the European samples.