Novel coumarin amino acid derivatives were synthesized. The structure of synthesized compounds has established on basis of different spectral data. The optimization geometry, frontier molecular orbitals (FMOs), thermodynamic parameters and chemical reactivity, were discussed using DFT\B3LYP by 6...
The molecular structure of Cu(II) complexes, obtained using direct and electrochemical synthesis, with 4-oxo-4H-chromene-2-carboxylic acid, 2-oxo-2H-chromene-3-carboxylic acid and (7-hydroxy-2-oxo-2H-chromen-4-yl)acetic acid have been studied. Due to difficulties in obtaining complexes as monocr...
A natural compound plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) was isolated from the leaves of Plumbago auriculata and found to inhibit the enzyme, 8-amino-7-oxononanoate synthase (AONS, also known as 7-keto-8-aminopelargonate synthase, KAPAS) an IC50 of 2.1 μM in vitro. Biotin supplement...
The chemical validation of a potential herbicide target was investigated with 8-amino-7-oxononanoate synthase (AONS, also known as 7-keto-8-aminopelargonate synthase, KAPAS) and triazolyl phenyl disulfide derivatives in vitro and in vivo. AONS activity was completely inhibited by these synthesiz...
The highly enantioselective synthesis of (2S)-α-(hydroxymethyl)-glutamic acid 2, a potent metabotropic receptor ligand, was accomplished using the improved Schöllkopf methodology for the construction of quaternary α-amino acids and β-lactams. This was converted to a derivative suitably protec...
Kinetic, thermodynamic and spectral data are reported for the formation of low spin d5 pentacyanoferrate(III) complexes of the type Fe(CN)5L starting from Fe(CN)5H2O2− for L=cytosine, cytidine and cytidine-5′-monophosphate. The complexes exhibit strong ligand-to-metal charge-transfer bands in t...
Formation of molecular complexes as a result of non-covalent interactions between adenosine 5′-monophosphate (AMP) or cytidine 5′-monophosphate (CMP) and polyamines, 1,5-diamino-3-azapentane (dien) or 1,6-diamino-3-azahexane (2,3-tri), has been studied in metal-free systems. Based on the acid–...
Uridine 5′-monophosphate (5′-UMP) and cytidine 5′-monophosphate (5′-CMP) were biosynthesized by recombinant uridine–cytidine kinase (UCK) and acetate kinase (ACK). The ack and uck genes from Escherichia coli K12 and the uck1, uck2 and ack genes from Lactobacillus bulgaricus ATCC 11842 were ...
The chemical interaction between DNA macromolecules and hard tissues in vertebrate is of foremost importance in paleogenetics, as bones and teeth represent a major substrate for the genetic material after cell death. Recently, the empirical hypothesis of DNA “protection” over time thanks to it...
Photoprotection of the RNA nucleotides adenosine 5′-monophosphate and cytidine 5′-monophosphate, and the nucleobase cytosine was studied using UV pump, IR probe femtosecond transient absorption spectroscopy. The excitation energy is contained in the aromatic ring system, protecting the RNA bac...
In vitro culture of H9 human lymphoid cells in the presence of 5.0 μM dideoxycytidine (ddC), for about 40–45 days, selected cells (H9-ddC cells), which were resistant to the drug and cross-resistant to AZT (zidovudine) and 5-fluoro-2′-deoxyuridine (FdUR). The major mechanism of cross-resistan...
Cell lines derived from different species show striking differences in their sensitivity to the cytostatic and anti-retrovirus activity, as well as the intracellular metabolism, of 3'-azido-2',3'-dideoxythymidine (AzddThd) and2',3'-dideoxycytidine (ddCyd). AzddThd and dd...
Peripheral neuropathy induced by 2′,3′-dideoxycytidine (ddC) could result from the previously shown inhibition of mtDNA replication by the action of ddC on the mitochondrial enzyme DNA polymerase γ. Such inhibition would be expected to impair oxidative phosphorylation, and this was demonstrat...
2′,3′-Dideoxycytidine (ddCyd) is one of the most potent antiviral nucleosides for killing the human immunodeficiency virus (HIV). ddCyd is currently used in the treatment of severe HIV infections but due to its rapid clearance it must be administered to patients every 4 h reaching concentratio...
The incidence of acquired immunodeficiency syndrome and the number of people infected with the human immunodeficiency virus (HIV) is likely to increase into the 1990s and perhaps beyond. Zidovudine, a 2′,3′-dideoxynucleoside approved for the treatment of acquired immunodeficiency syndrome, pro...
The effect of 2′,3′-dideoxycytidine, a potent antiviral agent, which, following anabolic phosphorylation, inhibits the reverse transcriptase of the human immunodeficiency virus in vitro, was assessed in 16 Pekin ducks chronically infected with the duck hepatitis B virus. Nine ducks were given ...
The nucleoside analog 2′,3′-dideoxycytidine (ddC) has been used for treatment of human immunodeficiency virus (HIV) infections. ddC causes delayed toxicity when cells are exposed to the drug at low concentration for prolonged periods of time. The delayed toxicity is due to inhibition of mitoch...
The 5′ → 5′ dinucleoside methylphosphonates of 3′-azido-3′-deoxythymidine (AZT) and 2′,3′-dideoxycytidine (DDC) were prepared and evaluated for their inhibitory properties against different viruses, including human immunodeficiency virus (HIV). The synthesis of the compounds was achieved ...
Both 2′,3′-dideoxycytidine (ddC) and 2′,3′-dideoxycytidine 5′-triphosphate (ddCTP) inhibit the synthesis of the major phospholipids phosphatidylcholine (PC) and phosphatidylethanolamine (PE) in permeabilized rat hepatocytes. For PC, this appears to be based on competitive inhibition of chol...
The Pd catalyzed reductive enyne cyclization provides an approach to control 1,3- diastereoselectivity and thereby provides a five step synthesis of β-necrodol, a key substituent of the defensive secretion of the red-lined carrion beetle.
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