Reaction of 3-nitrotyrosine with HOCl in aqueous phosphate buffer (pH 7.4) leads to a mixture of extractable products, including 3,5-di(4-hydroxy-3-nitrophenyl)pyridine (15% isolated yield) and 3,5-di(4-hydroxy-3-nitrophenyl)-2-(4-hydroxy-3-nitrophenylmethyl)pyridine (3%) arising by a Chichibabi...
The electrochemical properties of valacyclovir, an antiviral drug, were investigated in pH range 1.8–12.0 by cyclic, differential pulse and square-wave voltammetry. The drug was irreversibly oxidized at a glassy carbon electrode in one or two oxidation steps, which are pH-dependent. For analyti...
Objective: To document the frequency of genital herpes recurrences in men and women with histories of recurrent genital herpes during 1 year of continuous, suppressive therapy with valacyclovir hydrochloride (HCl).Methods: In an open-label clinical trial conducted at 11 centers, 127 subjects (46...
l-Valacyclovir, a prodrug of acyclovir, is a substrate for the peptide transporter (PepT1) in the intestinal mucosa, which accounts for its higher than expected oral bioavailability. The substrate activity of l-valacyclovir for PepT1 is surprising, particularly when one considers that the molecu...
A simple, sensitive and high throughput liquid chromatography/positive-ion electrospray ionization mass spectrometry (LC–ESI-MS/MS) method has been developed for the simultaneous determination of valacyclovir and acyclovir in human plasma using fluconazole as internal standard (IS). The method ...
The present study investigated the binding interaction between an antiviral drug, valacyclovir and calf thymus DNA (CT-DNA) using emission, absorption, circular dichroism, viscosity and DNA melting studies. In fluorimetric studies, thermodynamic enhancement constant (KD) and bimolecular enhancem...
A new simple, sensitive and precise liquid chromatography–tandem mass spectrometry method has been developed and validated for the determination of valacyclovir-HCl and acyclovir in tsetse flies (Glossina pallipides). Tsetse flies were extracted by ultrasonication with acidified methanol/aceton...
Electrochemically treated nanoporous TiO2 was employed as a novel electrode to assist in the photoelectrochemical degradation of acetaminophen and valacyclovir. The prepared electrode was characterized by scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS). Cyclic voltamm...
A series of novel nicotinohydrazide derivatives 6a–g and 1,3,4-oxadiazole functionalized pyridine derivatives 7a–k and 8a–d were prepared in series of steps. All the compounds were screened for cytotoxicity against HeLa (cervical), DU145 (prostate), HepG2 (liver) and MBA-MB-231 (breast) human...
The anti-HIV drug abacavir is associated with idiosyncratic hypersensitivity reactions and cardiotoxicity. Although the mechanism underlying abacavir-toxicity is not fully understood, drug bioactivation to reactive metabolites may be involved. This work was aimed at identifying abacavir–protein...
Abacavir is as a frequent part of combination antiretroviral therapy used in pregnant women. The aim of this study was to investigate, using in vitro, in situ and ex vivo experimental approaches, whether the transplacental pharmacokinetics of abacavir is affected by ATP-binding cassette (ABC) ef...
Most HIV-infected subjects will receive a treatment regimen including abacavir or tenofovir. Therefore, clarifying if there is an increased risk of acute myocardial infarction (AMI) among those exposed to abacavir is of the utmost importance. Due to the low frequency of AMI in this young populat...
Abacavir (ABC) is a nucleoside HIV-1 reverse transcriptase inhibitor, approved for clinical use in 1998. It is part of the recommended first-line therapy for treating HIV-1 infected children and adolescents. Resistance is determined by the M184V mutation, but additional substitutions are needed ...
IntroductionThe metabolic pathways of dolutegravir suggest a potential predator effect of nevirapine on dolutegravir pharmacokinetics and switching from a nevirapine- to a dolutegravir-containing regimen could lead to a lower and suboptimal exposure to dolutegravir several weeks after the switch...
ObjectivesAbacavir's potential to cause cardiovascular disease (CVD) among people living with HIV (PLWH) is debated. We conduct a systematic review and meta-analyses to assess CVD risk from recent and cumulative abacavir exposure.
Abacavir-induced liver toxicity is a rare event almost exclusively occurring in HLA B*5701-positive patients. Herein, we report one case of abnormal liver function tests occurring in a young HLA B*5701-negative woman on a stable nevirapine-based regimen with no history of liver problems or alcoh...
Electrochemical degradation of antiviral drug abacavir was investigated by using a penetration flux porous Ti/SnO2–Sb anode prepared by sol-gel method. The effects of applied current density, initial pH, and inorganic anions on the degradation kinetics were systematically studied. Degradation e...
Abacavir can cause a multi-systemic hypersensitivity reaction (HSR) in 5–8% of the patients, which is related to HLA-B*57-01 allele. In Brazil, the HLA-B*57-01 screening test became available only in March 2018, several years after abacavir was in use. In this retrospective study we reviewed me...
Human serum albumin (SA) is best known for its extraordinary ligand-binding capacity. Here, kinetics of peroxynitrite-mediated oxidation of SA–heme(II)–NO is reported. Peroxynitrite reacts with SA–heme(II)–NO leading to SA–heme(III) and NO by way of the transient SA–heme(III)–NO species. ...
Human serum albumin (HSA) participates to heme scavenging, in turn HSA–heme binds gaseous diatomic ligands at the heme–Fe-atom. Here, the effect of abacavir and warfarin on denitrosylation kinetics of HSA–heme–Fe(II)–NO (i.e., koff) is reported. In the absence of drugs, the value of koff is...
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