A5043422211- Inflammatory mediators and NSAID effects
- Eicosanoids and Hypertension Pharmacology
- Synthesis of β-Lactam Compounds
- Catalytic C–H Functionalization Methods
- Cardiovascular Function and Risk Factors
- Chemical Synthesis and Analysis
- Cancer Immunotherapy and Biomarkers
- Chemical synthesis and alkaloids
- Receptor Mechanisms and Signaling
- Asymmetric Synthesis and Catalysis
- Peroxisome Proliferator-Activated Receptors
- Radiopharmaceutical Chemistry and Applications
- Polysaccharides and Plant Cell Walls
- French Literature and Critical Theory
- Catalytic Cross-Coupling Reactions
- Polysaccharides Composition and Applications
- Synthesis and Catalytic Reactions
- Cyclopropane Reaction Mechanisms
- Down syndrome and intellectual disability research
- Cancer, Lipids, and Metabolism
- Cholesterol and Lipid Metabolism
- Synthetic Organic Chemistry Methods
- Sulfur-Based Synthesis Techniques
- Biomedical Research and Pathophysiology
- Kidney Stones and Urolithiasis Treatments
University of Kentucky
2008-2021
Merck & Co., Inc., Rahway, NJ, USA (United States)
2011-2021
United States Military Academy
2012-2020
Hofstra University
1996-2019
Merck Canada Inc. (Canada)
2006-2017
Alder Hey Children's Hospital
2014
University of Liverpool
2014
University of Toronto
2001-2012
Merck (Japan)
2007-2012
TransCanada (Canada)
2011
N-Heterocyclic carbenes can catalyze β-alkylations of a range α,β-unsaturated esters, amides, and nitriles that bear pendant leaving groups to form variety ring sizes. In this process, the nucleophilic catalyst transiently transforms normally electrophilic β carbon into site through an unanticipated addition−tautomerization sequence.
Antigenic recognition of four anti-bovine parathyroid hormone antisera was characterized by their reactivity with bovine hormonal fragments (1-34, 1-13, 14-34, 19-34, 53-84) and human extracted from adenomas. All were found to have antibody populations which recognized more than one antigenic determinant all differed in specificity for the hormone. By modification two antisera, GP-1 GP-133, preincubation excess concentrations 1-34 or 53-84 fragments, restricted defined regions sequence.
A metal-catalyzed cross-coupling of organosilicon compounds with alkyl halides has been developed. Noteworthy attributes the method are its scope (secondary electrophiles), high functional-group compatibility, and air stability catalyst components.
The first catalyst that achieves Stille cross-couplings of secondary (as well as primary) alkyl halides has been developed. method employs easily handled and inexpensive components (NiCl2 2,2'-bipyridine) and, through the use monoorganotin reagents, avoids formation toxic difficult-to-remove triorganotin side products.
A copper-catalyzed amidation of allylic and benzylic C−H bonds with both primary secondary sulfonamides is described. The reaction applicable to the coupling a diverse set hydrocarbon species aryl, heteroaryl, alkyl tolerant variety functional groups. Mechanistic insight has been gained through isolation acetate intermediate, which was demonstrated undergo facile conversion substituted sulfonamide product under copper catalysis.
The potential use of SCD inhibitors for the chronic treatment diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition in skin eye tissues. To establish a therapeutic window, we embarked on designing liver-targeted utilizing molecular recognition liver-specific organic anion transporting polypeptides (OATPs). In doing so, set out to target inhibitor organ believed be responsible efficacy (liver) while minimizing its exposure tissues mechanism-based...
A concise synthesis of the guanidine alkaloids, (±)-martinelline and (±)-martinellic acid, using a protic acid catalyzed 2:1 hetero Diels−Alder coupling reaction between N-Cbz 2-pyrroline methyl 4-aminobenzoate, is described. Protic catalysis, rather than Lewis was necessary to achieve desired sense diastereocontrol in reaction.
A room-temperature, copper-catalyzed amination of primary benzylic C−H bonds with and secondary sulfonamides is described. The reaction applicable to the coupling a range hydrocarbons diverse set tolerant substitution on both partners. Factors which influence selectivity functionalization between sites are examined.
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTCopper-Catalyzed Oxidative Coupling of Benzylic C−H Bonds with 1,3-Dicarbonyl CompoundsNadine Borduas and David A. Powell*View Author Information Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec H9H 3L1, Canada[email protected]Cite this: J. Org. Chem. 2008, 73, 19, 7822–7825Publication Date (Web):September 4, 2008Publication History Received19 June 2008Published online4 September inissue 3 October...
Membranes of Micrococcus lysodeikticus, flavus and sodonensis contain acidic lipomannans. Lipoteichoic acids could not be detected in these organisms, the suggestion that they are substituted for by lipomannans is strengthened chemical physical resemblances between two polymers. The mannans glycerol, ester-linked fatty mono-esterified succinic acid residues, giving them both hydrophobic charged properties. M. lysodeikticus mannan has a chain about 60 hexose units with branch points, joined...
Background: Primary hyperoxalurias 1-3 (PH1-3) are genetic diseases defined by elevated hepatic oxalate production and increased incidence of calcium kidney stones potentially failure. There two approved agents available for PH1, no therapies PH2 or PH3. Lactate dehydrogenase A (LDHA) catalyzes the final step in synthesis represents a potential therapeutic target PH other forms hyperoxaluria associated with production. Methods: Potent selective LDH inhibitors liver-targeted tissue...
To determine if proton magnetic resonance spectroscopy (1H-MRS) detect differences in dementia status adults with Down syndrome (DS), we used 1H-MRS to measure neuronal and glial metabolites the posterior cingulate cortex 22 DS 15 age- gender-matched healthy controls. We evaluated associations between results cognition among participants. Neuronal biomarkers, including N-acetylaspartate (NAA) glutamate-glutamine complex (Glx), were significantly lower patients Alzheimer's should probably be...
While the role of prostaglandin E2 (PGE2) in promoting malignant progression is well established, how to optimally block activity PGE2 signaling remains be demonstrated. Clinical trials with pathway targeted agents have shown but without sufficient significance or dose-limiting toxicities that prevented approval. signals through four receptors (EP1–4) modulate tumor progression. EP2 and EP4 exacerbates pathology immunosuppressive potentiating cAMP production. EP1 EP3 has opposite effect...
CD14 is a glycosylphosphatidylinositol (GPI)-anchored protein on the surfaces of monocytes and polymorphonuclear leukocytes (PMN) that binds initiates cellular responses to bacterial LPS. PMN also contain an intracellular pool can be deployed rapidly cell surface in response stimulation with variety agonists. To determine which well-characterized subcellular compartments contains CD14, cells were cavitated fractionated Percoll gradients. The gradient fractions assayed for by ELISA Western...
An operationally straightforward and efficient method for the alkylation of carbamate-protected guanidines with various alkyl halides mesylates is described. This protocol proceeds via deprotonation acidic N-carbamate hydrogen guanidine under biphasic conditions using a catalytic amount tetrabutylammonium salt as phase-transfer catalyst. In this manner, highly functionalized can be obtained. The reaction tolerant wide range functional groups on both halide component. addition, sufficiently...
We reviewed the immunoreactivity of sera binding to epidermal side basement membrane split skin from 13 adults and 8 children with IgA alone, 9 IgG 7 ocular pemphigoid. Immunoblots were done against previously described 45-, 97-, 180- 230-kD antigens, reactivity was confirmed by elution antibody nitrocellulose membrane. Ten reacted 97-kD antigen. Sera both in varying patterns on occasion more than 1 All patients cicatricial pemphigoid uniquely a 45-kD