Πλοήγηση ανά Θέμα "Chemistry, Medicinal"
Αποτελέσματα 1-20 από 58
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1-(3-Deoxy-3-fluoro-beta-D-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies
(2010)Design of inhibitors of glycogen phosphorylase (GP) with pharmaceutical applications in improving glycaemic control in type 2 diabetes is a promising therapeutic strategy. The catalytic site of muscle glycogen phosphorylase ... -
3 '-Axial CH2OH Substitution on Glucopyranose does not Increase Glycogen Phosphorylase Inhibitory Potency. QM/MM-PBSA Calculations Suggest Why
(2012)Glycogen phosphorylase is a molecular target for the design of potential hypoglycemic agents. Structure-based design pinpointed that the 3'-position of glucopyranose equipped with a suitable group has the potential to form ... -
Anti-cancer activity of a novel palladium(II) complex on human breast cancer cells in vitro and in vivo
(2011)Anti-cancer effects of a newly-synthesized palladium(II) complex, [Pd(sac)(terpy)](sac)center dot 4H(2)O (sac = saccharinate, and terpy = 2,2':6',2 ''-terpyridine), were tested against human breast cancer cell lines, MCF-7 ... -
Antibacterial Activity of Greek and Cypriot Honeys Against Staphylococcus aureus and Pseudomonas aeruginosa in Comparison to Manuka Honey
(2013)The antibacterial activity of 31 Greek and Cypriot honeys against Staphylococcus aureus and Pseudomonas aeruginosa was initially screened using an agar-well diffusion assay in comparison with manuka honey. The minimum ... -
The binding of beta-D-glucopyranosyl-thiosemicarbazone derivatives to glycogen phosphorylase: A new class of inhibitors
(2010)Glycogen phosphorylase (GP) is a promising target for the treatment of type 2 diabetes. In the process of structure based drug design for GP, a group of 15 aromatic aldehyde 4-(beta-D-glucopyranosyl) thiosemicarbazones ... -
The binding of C5-alkynyl and alkylfurano 2,3-d pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment
(2012)C5-alkynyl and allcylfurano[2,3-d]pyrimidine glucopyranonucleosides have been synthesized and studied as inhibitors of glycogen phosphorylase b (GPb). Kinetic experiments have shown that most of these compounds were low ... -
Biomarkers Obtained by Non-Invasive Methods in Patients with COPD: Where do we Stand, what do we Expect?
(2009)Recently, there has been widespread interest in the use of non-invasive methods for the assessment of airway inflammation in a variety of lung diseases including chronic obstructive pulmonary disease ( COPD). Sputum induction ... -
Branched-chain C-cyano pyranonucleosides: Synthesis of 3 '-C-cyano & 3 '-C-cyano-3 '-deoxy pyrimidine pyranonucleosides as novel cytotoxic agents
(2011)This report describes the total and facile synthesis of 3'-C-cyano & 3'-C-cyano-3'-deoxy pyrimidine pyranonucleosides. Reaction of 3-keto glucoside 1 with sodium cyanide gave the desired precursor 3-C-cyano-1,2:5,6-di-O- ... -
Catalytic Inhibition of Eukaryotic Topoisomerases I and II by Flavonol Glycosides Extracted from Vicia faba and Lotus edulis
(2011)Topoisomerases are essential enzymes involved in all processes of DNA metabolism, and their inhibitors have been identified as potential anticancer agents. The present study examined the effect of nine polyphenolic compounds ... -
Clindamycin binding to ribosomes revisited: foot printing and computational detection of two binding sites within the peptidyl transferase center
(2013)Clindamycin is a semi-synthetic lincosamide, active against most Gram-positive bacteria and some protozoa. It binds to the 50S ribosomal subunit and inhibits early peptide chain elongation. By kinetic analysis it has been ... -
Computation as a Tool for Glycogen Phosphorylase Inhibitor Design
(2010)Glycogen phosphorylase is an important therapeutic target for the potential treatment of type 2 diabetes. The importance of computation in the search for potent, selective and drug-like glycogen phosphorylase inhibitors ... -
Conformational analysis of two novel cytotoxic C2-substituted pyrrolo 2,3-f quinolines in aqueous media, organic solvents, membrane bilayers and at the putative active site
(2012)We have performed: (i) conformational analysis of two novel cytotoxic C2-substituted pyrrolo[2,3-f]quinolines Se and 5g in deuterated dimethylsulfoxide (DMSO-d(6)) utilizing NOE results from NMR spectroscopy; (ii) molecular ... -
Contribution of aldehyde oxidase, xanthine oxidase, and aldehyde dehydrogenase on the oxidation of aromatic aldehydes
(2004)Aliphatic aldehydes have a high affinity toward aldehyde dehydrogenase activity but are relatively poor substrates of aldehyde oxidase and xanthine oxidase. In addition, the oxidation of xenobiotic-derived aromatic aldehydes ... -
Curcumin analogues as possible anti-proliferative & anti-inflammatory agents
(2011)A series of novel curcumin analogues has been designed, synthesized and tested in vitro/in vivo as potential multi-target agents. Their anti-proliferative and anti-inflammatory activities were studied. Compounds 1b and 2b ... -
Dideoxy fluoro-ketopyranosyl nucleosides as potent antiviral agents: Synthesis and biological evaluation of 2,3-and 3,4-dideoxy-3-fluoro-4-and-2-keto-beta-D-glucopyranosyl derivatives of N-4-benzoyl cytosine
(2009)The synthesis of the dideoxy fluoro ketopyramonucleoside analogues, 1-(2,3-dideoxy-3-fluoro-6-O-trityl-beta-D-glycero-hexopyranosyl-4-ulose)-N-4-benzoyl cytosine (7a), 1-(3,4-dideoxy-3-fluoro-6-O-trityl-beta-D-glycero-he ... -
Effects of the active constituents of Crocus sativus L., crocins, in an animal model of anxiety
(2008)Crocus sativus L. is a plant cultivated in various parts of the world. Crocins are among the active components of Crocus sativus L. The present study was designed to investigate in the rat whether or not crocins possess ... -
An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents
(2007)1,2:5,6-Di-O-isopropylidene-alpha-D-glucofuranose by the sequence of mild oxidation, reduction, fluorination, periodate oxidation, borohydride reduction, and sulfonylation gave 3-deoxy-3-fluoro-1,2-O-isopropylidene-5-O-p ... -
Enzymes as Target Antigens of Liver-Specific Autoimmunity: The Case of Cytochromes P450s
(2008)Characterization of liver-specific autoantigens has given a fresh impetus to research in the pathogenesis of autoimmune liver diseases, viral-triggered and drug-induced autoimmunity affecting the liver. Intriguing is the ... -
Epigenetic Mechanisms and Kidney Diseases
(2011)In recent years, molecular research has brought to light a series of mechanisms involved in the regulation of gene function without altering the DNA sequence. These mechanisms are described with the term "epigenetics" and ...