it is important to determine whether a candidate molecule is capable of penetrating the plasma-brain barrier indrug discovery and development. the aim of this paper is to establish a predictive model for plasma-brainbarrier penetration using simple descriptors the usefulness of the quantum chemical descriptors, calculated atthe level of the dft and he theories using 6-310* basis set for qsar st...

Understanding and optimization of the photophysics fluorescent nucleoside analogues are critical for their applications in probing structure dynamics nucleic acids, studying interactions with ligands biomolecules.

A new efficient method for the synthesis of carboacyclic nucleosides as biologically interesting compounds via aza-conjugate addition of pyrimidine nucleobases to a,β-unsaturated esters in the presence of catalytic amount of LiOH.H2O (1.2-4.8 mol%) under microwave irradiation is described. This method affords the title compounds in good to excellent yields and i...

In this study the uptake and metabolism of adenosine by mitochondria has been investigated. Incubation of CEM cells mitochondria preparation with [3H] -adenosine showed substantial uptake and metabolism of adenosine. Adenosine was both anabolized to AMP, ADP and ATP, and also catabolized to inosine. The highest concentration of metabolites in extracted mitochondria was due to AMP. The mito...

Introduction . Cytomegalovirus infection (CMVI) makes a significant contribution to the development of pregnancy pathologies, including dysfunction placenta. However, mechanism such an effect CMV has not been precisely established. For coordination biochemical reactions in placenta, optimal concentration substances, nucleotides, is required. Nucleoside diphosphatase enzyme that catalyzes hydrol...

Three diazoles namely 5-methyl-1,3,4-oxadiazole -2(3H)-thione, 5-methyl-1,3,4-thiadiazol-2(3H)-thione and 4-amino-5-methyl-2H-1,2,4-triazole-3-thiol were synthesized from acetic acid or ethyl acetate. Seco-acyclo-N-nucleoside analogous was by condensation of 1,3-benzylidine-glyceryl-2-tosylate with the three diazoles. Structural proof based upon IR, 1H-NMR, 13C-NMR spectroscopy MS measurements....

Concentrative nucleoside transporters (CNT; SLC28) and equilibrative nucleoside transporters (ENT; SLC29) mediate the uptake of natural nucleosides and a variety of nucleoside-derived drugs, mostly used in anticancer therapy. SLC28 and SLC29 families consist in three and four members, respectively, which differ in their substrate selectivity and their energy requirements. Tissue distribution of...

BACKGROUND AND OBJECTIVES Nucleoside transporters might play a relevant role in the intracellular targeting of many nucleoside analogs used in anticancer therapy. Two gene families (SLC28 and SLC29) encode the two types of human nucleoside transporters, concentrative nucleoside transporter (CNT) and equilibrative nucleoside transporter (ENT) proteins. Chronic lymphocytic leukemia (CLL) cells ex...

There is an extensive list of applications for nucleosides, nucleotides, and their analogues that spans from substrates inhibitors in enzymatic research to anticancer antiviral drugs. Nucleoside phosphates are often obtained by chemical phosphorylation reactions, although nucleoside a promising green alternative. In this work two kinases, D. melanogaster deoxynucleoside kinase B. subtilis deoxy...