The synthesis of a new series of abacavir prodrugs involving N2-substitution with various substituted benzaldehyde and ketone derivatives is described. The in vitro anti-HIV activities indicated that compound (3-(2-(4-methylaminobenzylideneamino)-6-(cyclopropylamino)-9H-purin-9-yl)cyclopentyl)me...
Abacavir has an antiretroviral activity against HIV and is oxidizable at the glassy carbon electrode. Cyclic voltammetry studies showed one well-defined oxidation wave or splitted two waves depending on pH. The oxidation was irreversible and exhibited diffusion controlled process depending on pH...
A sensitive and reproducible method has been developed and validated for the simultaneous quantification of the key antiretroviral drugs abacavir and tenofovir in hair using LC–MS/MS. The method was validated according to the US Food and Drug Administration (FDA) guidelines for the parameters: ...
Nucleoside reverse transcriptase inhibitors (NRTIs) require intracellular phosphorylation to active triphosphate (TP) nucleotide metabolites before they can inhibit the HIV reverse transcriptase. However, monitoring these pharmacologically active TP metabolites is challenging due to their instab...
In the present study the binding characteristics of abacavir (ABV), efavirenz (EFV) and emtricitabine (EMC) to bovine serum albumin (BSA) have been investigated via the use of spectroscopic tools and in silico docking studies. Those ligands were found to statically quench the intrinsic fluoresce...
Growth Hormone (GH) deficiency is frequent in HIV-infected patients treated with antiretroviral therapy. We treated GH3 cells with antiretrovirals (nevirapine, ritonavir or abacavir sulfate; 100 pM-1 mM range), after transfection with human growth hormone releasing hormone (GHRH) receptor cDNA. ...
A simple high-performance liquid chromatography (HPLC) method has been developed and validated for the simultaneous determination of abacavir and zidovudine (AZT) in rat plasma, amniotic fluid, fetal, and placental tissues. Extraction of abacavir, AZT, and the internal standard, azidouridine (AZ...
The study was designed to prepare and evaluate albumin nanoparticles containing antiviral drug abacavir sulphate. Various batches of albumin nanoparticles containing abacavir sulphate were prepared by desolvation method. The abacavir loaded particles were characterized for their yield, percentag...
The pharmacokinetics of a new, selective thromboxane synthase inhibitor, sodium 5-(3′-pyridinylmethyl)benzofuran-2-carboxylate were determined for single dose, bolus intravenous injections (1, 3, and 10 mg/kg); for continuous 24 hr infusions (10 and 30 μg/kg/min); and for oral doses of gelatin...
Fibronectins are a part of the repertoire of matrix molecules by the chondrocyte in order to assemble a functional cartilage matrix. They are encoded by a single gene, but significant protein heterogeneity results form alternatie RNA splicing. The population of fibronectin isoforms in adult cart...
Fibronectins are high molecular weight glycoproteins present in body fluids and tissues that facilitate cell-to-extracellular matrix adhesion. Fibronectins are integrally involved in cell growth, differentiation, and migration, and therefore, fibronectins play important roles in numerous biologi...
Fibronectin is present at the dermal-epidermal junction in normal skin and is increased in skin tissues in inflammatory diseases, skin cancers and wound repair. The present studies focused on further characterizing the interaction between fibronectin and keratinocytes, specifically addressing wh...
The region of fibronectin (FN) surrounding the two type II modules of FN binds type I collagen. However, little is known about interactions of this collagen binding domain with other collagen types or extracellular matrix molecules. Among several expressed recombinant (r) human FN fragments from...
Mesenchymal cell movement is normally constrained; however, fibronectin can provide a pathway for stromal cell migration during embryogenesis, morphogenesis, and wound healing. Cells can adhere to fibronectin via integrin and nonintegrin receptors, which bind multiple unique peptide sequences. S...
Interaction of exogenous fibronectin with the basement membrane-like PYS-2 cell matrix, lacking fibronectin and hyaluronic acid but containing heparan sulfate proteoglycan, was studied in vitro. Both human plasma fibronectin and fibronectin in fetal calf serum bound to PYS-2 matrix; also, fragme...
A better understanding of the mechanism of adhesion, spreading and proliferation of human endothelial cells (HEC) on polymeric surfaces may lead to the development of vascular prostheses which allow the formation of an endothelial lining on the luminal surface. In the present investigation the i...
Numerous studies have been made into the nature and importance of altered levels of plasma fibronectin seen in a range of clinical disorders. However, fibronectin is highly sensitive to the proteolytic degradation which may accompany some of these conditions. The influence of such degradation on...
This paper reports a new, mild procedure (“di-UPS”) for the solid phase synthesis of racemic α,α-disubstituted amino acids (1) and epimeric α,α-disubstituted terminal amino acid residues (2, R3=H) in a resin bound peptide. The synthetic route is compatible with most protected amino acid si...
Succinimidyl esters of various carboxylic acids are formed in high yield at ambient to slightly elevated temperature by the system chlorophosphate / hydroxysuccinimide / base.
Publisher SummaryThe chapter discusses intramolecular reversible addition reactions to the C═N group and other groups. The chapter offer an introduction to and general considerations of the ring-chain tautomeric process. Despite the lower reactivity of the azomethine group as compared with the ...
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