A number of new substituted 1,2,4-triazole {[(1,2,4-triazolyl)ethyl]tetrazolyl} derivatives, their sugar hydrazones, and their acyclic C-nucleoside analogues were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees...

Examples of organometallic compounds as nucleoside analogues are rare within the field of medicinal bioorganometallic chemistry. We report on the synthesis and properties of two chiral ferrocene derivatives containing a nucleobase and a hydroxyalkyl group. These so-called ferronucleosides show promising anticancer activity, with cytostatic studies on five different cancer cell lines indicating ...

BACKGROUND Adherence to medication is an important aspect of preventing drug resistance and treatment failure in patients receiving nucleos(t)ide analogues for chronic hepatitis B. AIMS To assess adherence to nucleoside/nucleotide analogues in chronic hepatitis B treatment and to determine factors associated with non-adherence. STUDY DESIGN Cross-sectional study. METHODS The study enrolle...

Actinic keratosis and cutaneous squamous cell carcinoma are of increasing importance with aging and increased ultraviolet light exposure in Western societies. Efficient and well-tolerated therapy is still a matter of concern. As with tumours of other organs, new target sites and innovative drugs selectively addressing them are widely looked for. Due to the relevance for DNA synthesis and thus c...

In an effort to study the effects of flexibility on enzyme recognition and activity, we have developed several different series of flexible nucleoside analogues in which the purine base is split into its respective imidazole and pyrimidine components. The focus of this particular study was to synthesize the truncated neplanocin A fleximers to investigate their potential anti-protozoan activitie...

The purine metabolism of several genera of parasitic protozoa, is of interest partly due to their sensitivity to purine analogues, and to differences in the enzymes of purine metabolism compared to mammalian systems [l-6]. Trichomonas vaginalis, the causative agent of trichomonal vaginitis, a mild, but very common, sexually-transmitted disease, has not been studied in this respect; there is a g...

The first copper-catalysed diastereoselective synthesis of P-chiral phosphoramidate prodrugs (ProTides) is reported. This procedure allows the synthesis of diastereomeric-enriched mixtures of ProTides. Application of this methodology to the asymmetric phosphorylation of purine and pyrimidine nucleoside analogues is presented.

Mainly driven by the needs of antisense research, a large number of oligonucleotide analogues have been prepared and evaluated over the last 15 years. Besides minor structural modifications of the building blocks of DNA and RNA itself, a considerable effort has been devoted to the de novo design of nucleoside analogues with improved binding properties. A particularly successful concept turned o...

Lactic acidosis is a rare but often fatal complication reported in some human immunodeficiency virus (HIV)-infected patients treated with nucleoside-analogue reverse-transcriptase inhibitors. We report a series of 12 patients with HIV infection treated with nucleoside analogues who developed unexplained metabolic acidosis. We have also reviewed 60 additional published cases. The aim of the pres...

The chemistry of natural nucleosides and their analogues has been widely studied due to their potential as fungicidal, antitumor, and antiviral agents. 1 Consequently, extensive modifications have been made to both the heterocyclic base and the sugar moiety in order to avoid the drawbacks shown by nucleosides or analogues in certain applications. For organic chemists, enzymatic-catalyzed reacti...