A5040538626- Pharmacogenetics and Drug Metabolism
- Chemical synthesis and alkaloids
- Asymmetric Hydrogenation and Catalysis
- Asymmetric Synthesis and Catalysis
- Hormonal and reproductive studies
- Chemical Reactions and Isotopes
- Analytical Chemistry and Chromatography
- Cholinesterase and Neurodegenerative Diseases
- Biosimilars and Bioanalytical Methods
- Cholesterol and Lipid Metabolism
- Nicotinic Acetylcholine Receptors Study
- Antibiotics Pharmacokinetics and Efficacy
- Synthetic Organic Chemistry Methods
- Tryptophan and brain disorders
- Hepatitis C virus research
- Migraine and Headache Studies
- Microbial Natural Products and Biosynthesis
- Cancer Treatment and Pharmacology
- Medical Imaging Techniques and Applications
- Bacterial Identification and Susceptibility Testing
- Eicosanoids and Hypertension Pharmacology
- Metabolism and Genetic Disorders
- HIV/AIDS drug development and treatment
- Inflammatory mediators and NSAID effects
Bristol-Myers Squibb (United States)
2011-2022
Bristol-Myers Squibb (Germany)
2015
Eastern Michigan University
2007
It has recently been proposed that plasma levels of 4β-hydroxycholesterol (4βHC) may be indicative cytochrome P450 3A4 (P450 3A) activity and therefore could used to probe for 3A-mediated drug–drug interactions. With this in mind, we describe a highly sensitive precise liquid chromatography–electrospray ionization–tandem mass spectrometry method the measurement 4βHC human with lower limit quantification established at 2 ng/mL using 50 μL plasma. The entire sample preparation scheme including...
In previous studies, gemfibrozil acyl-β-glucuronide, but not gemfibrozil, was found to be a mechanism-based inhibitor of cytochrome P450 2C8. To better understand whether this inhibition is specific for acyl-β-glucuronide or other glucuronide conjugates are potential substrates enzyme, we evaluated several pharmaceutical compounds (as their acyl glucuronides) as direct-acting and metabolism-dependent inhibitors CYP2C8 in human liver microsomes. Of 11 that were conjugates, only exhibited...
Cytochrome P450 3A (CYP3A) enzymes are involved in the metabolism of over half today's prescription drugs. As a result, drugs metabolized by CYP3A have risk drug–drug interactions (DDIs). Recent studies shown potential to use 4 β ‐hydroxycholesterol as an endogenous biomarker activity and predictor DDIs. Bristol–Myers Squibb has developed liquid chromatography‐electron ionization‐tandem mass spectrometry method that accurately measures levels clinical plasma samples following treatment with...
The first microwave-assisted version of the tandem aza-Cope rearrangement-Mannich cyclization was developed. This sequence provides acylpyrrolidines in a single synthetic step while significantly reducing reaction times as compared to analogous reactions using conventional heating. Diastereoselectivity these may be improved by increasing size amine-protecting group, an observation which has not been reported previously for aza-Cope-Mannich leading monosubstituted acylpyrrolidines. Finally,...
Oral calcitonin gene-related peptide (CGRP) receptor antagonists have been shown to be effective in the acute and preventive treatment of migraine. CGRP offer safety advantages over triptans because they are not active vasoconstrictors, which reduces cardiovascular risks. Bristol Myers Squibb discovered a high affinity antagonist BMS-927711 for migraine now FDA approved as Nurtec® ODT (rimegepant). Dual-labeled [14 C]-BMS-927711 was prepared used human...
The stabilization of microtubules using epothilones represents a novel mechanism action to treat Alzheimer's disease. Epothilone D is one such microtubule-stabilizing drug that has been investigated by Bristol-Myers Squibb. An important step in the development process was synthesis stable isotope-labeled analog for use bioanalytical assays accurately quantify concentration biological samples. A synthetic route epothilone described. based on strategy degrade B and then key intermediate...
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 200 leading journals. To access Abstract, please click on HTML or PDF.