A5041108407- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- Pharmacogenetics and Drug Metabolism
- Asymmetric Synthesis and Catalysis
- Click Chemistry and Applications
- Chemical Reactions and Isotopes
- Histone Deacetylase Inhibitors Research
- Coordination Chemistry and Organometallics
- Synthesis of heterocyclic compounds
- MicroRNA in disease regulation
- Advanced biosensing and bioanalysis techniques
- RNA Interference and Gene Delivery
- Glycosylation and Glycoproteins Research
- Chemical Reaction Mechanisms
- Cancer Treatment and Pharmacology
- Cancer, Hypoxia, and Metabolism
- Drug-Induced Hepatotoxicity and Protection
- Synthesis of Tetrazole Derivatives
- Organophosphorus compounds synthesis
- Epigenetics and DNA Methylation
- Metabolism, Diabetes, and Cancer
- Enzyme Catalysis and Immobilization
- Diet and metabolism studies
- Protein Degradation and Inhibitors
- Enzyme Structure and Function
AbbVie (United States)
2016-2021
United States Military Academy
2014
Merck & Co., Inc., Rahway, NJ, USA (United States)
2005-2014
Merck (Japan)
2007
Urbana University
2001
University of Illinois Urbana-Champaign
2000
University of Maryland, College Park
1999-2000
University of Pennsylvania
1999
Hypervalent azido- and cyanosilicate derivatives, prepared in situ by the reaction of trimethylsilyl azide or cyanide, respectively, with tetrabutylammonium fluoride, are effective sources nucleophilic cyanide. Primary secondary alkyl halides sulfonates undergo rapid efficient cyanide displacement absence phase transfer catalysts silicate derivatives. Application these reagents to stereoselective synthesis glycosyl derivatives is reported.
The application of small interfering (si)RNAs as potential therapeutic agents requires safe and effective methods for their delivery to the cytoplasm target cells tissues. Recent studies have shown significant progress in development targeting reagents that facilitate recognition of, siRNA to, specific cell types. Among recently reported approaches, polymers with amphipathic properties been used enable endosome escape cytosolic delivery. Here, we describe a linear poly(amido amine) polymer...
The disposition of vorinostat, an anticancer agent, was investigated in rats and dogs. Vorinostat possessed high serum clearance, a short elimination half-life low oral bioavailability both species. renal route played important role the drug-related material vorinostat eliminated primarily by metabolic biotransformation.
The 2,3-diaminopyridine (DAP) moiety was found to represent a core structure essential for the potency of new series human bradykinin B1 receptor antagonists. However, incubation 14C-labeled 2,3-DAP derivatives with rat and liver microsomes resulted in substantial irreversible binding radioactive material macromolecules by process that NADPH-dependent. Trapping reactive species GSH led significant reduction radioactivity, concomitant formation abundant adducts. One type thiol adducts...
(3<i>R</i>)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[<i>b</i>]indol-3-yl acetic acid (MK-0524) is a potent orally active human prostaglandin D<sub>2</sub> receptor 1 antagonist that currently under development for the prevention of niacin-induced flushing. The major in vitro and vivo metabolite MK-0524 acyl glucuronic conjugate parent compound, M2. To compare metabolism across preclinical species humans, studies were undertaken to determine kinetic...
[(3<i>R</i>)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopentaindol-3-yl]acetic acid (MK-0524) is a potent orally active human prostaglandin D<sub>2</sub> receptor 1 antagonist that currently under development for the prevention of niacin-induced flushing. The metabolism and excretion [<sup>14</sup>C]MK-0524 in humans were investigated six healthy volunteers following single p.o. dose 40 mg (202 μCi). was absorbed rapidly, with plasma <i>C</i><sub>max</sub> achieved...
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTAdvances in Glycosyl Azide Preparation via Hypervalent Silicates†Eric D. Soli and Philip DeShongView Author Information Department of Chemistry Biochemistry, The University Maryland, College Park, Maryland 20742 Cite this: J. Org. Chem. 1999, 64, 26, 9724–9726Publication Date (Web):November 24, 1999Publication History Received21 July 1999Published online24 November inissue 1 December...
Gonadotropin‐releasing hormone (GnRH) receptor antagonists are an important class of compounds designed to block the pituitary gland from synthesizing follicle‐stimulating and luteinizing for treatment sex dependent disorders. Elagolix (ABT‐620) is currently approved pain associated with endometriosis as a combination estradiol norethindrone acetate management heavy menstrual bleeding due uterine fibroids. In order support development elagolix, we prepared [ 3 H]elagolix preclinical...
In support of a program to develop treatment for advanced, refractory cutaneous T-cell lymphoma, two differentially [14C]-labeled forms vorinostat, histone deacetylase inhibitor, were synthesized use in metabolism studies. Copyright © 2006 John Wiley & Sons, Ltd.
Cholesteryl ester transfer protein inhibitors are an important class of compounds designed to treat hypocholesterolemia and prevent cardiovascular disease. Anacetrapib (MK-0859) is currently in phase III trials for the treatment elevated cholesterol levels prevention In order further support development anacetrapib, we prepared [M + 6]MK-0859, which was required absolute bioavailability study active pharmaceutical ingredient (API). Additional included synthesis internal standard 13] three...
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionORIGINAL ARTICLEThis notice is a correctionAzide and Cyanide Displacements via Hypervalent Silicate Intermediates.Eric D. Soli, Amy S. Manoso, Michael C. Patterson, Philip DeShong, David A. Favor, Ralph Hirschmann, Amos B. SmithCite this: J. Org. Chem. 1999, 64, 17, 6526Publication Date (Web):July 23, 1999Publication History Published online23 July 1999Published inissue 1 August...
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”