A5049366197- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Asymmetric Synthesis and Catalysis
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthetic Organic Chemistry Methods
- Chemical Synthesis and Analysis
- Chemical Synthesis and Reactions
- Sulfur-Based Synthesis Techniques
- Catalytic Cross-Coupling Reactions
- Catalytic C–H Functionalization Methods
- Synthesis of heterocyclic compounds
- Wildlife-Road Interactions and Conservation
- Advanced Polymer Synthesis and Characterization
- Synthesis and biological activity
- Crystallography and molecular interactions
- Synthesis and Catalytic Reactions
- Cyclopropane Reaction Mechanisms
- Oxidative Organic Chemistry Reactions
- Coordination Chemistry and Organometallics
- Synthesis and Reactions of Organic Compounds
- Receptor Mechanisms and Signaling
- Land Use and Ecosystem Services
- Various Chemistry Research Topics
- Asymmetric Hydrogenation and Catalysis
- Peptidase Inhibition and Analysis
Pfizer (United States)
2016-2025
University of Liverpool
2021-2024
John Wiley & Sons (United States)
2016-2020
Ecological Society of America
2016-2020
IFC Research (United Kingdom)
2018-2019
Wyoming Game and Fish Department
2019
Centre for Process Innovation
2016
Foton Motors (China)
2014
University of Pennsylvania
2012
Clark University
2006
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTFluoride-Mediated Boronic Acid Coupling ReactionsStephen W. Wright, David L. Hageman, and Lester D. McClureCite this: J. Org. Chem. 1994, 59, 20, 6095–6097Publication Date (Print):October 1, 1994Publication History Published online1 May 2002Published inissue 1 October 1994https://pubs.acs.org/doi/10.1021/jo00099a049https://doi.org/10.1021/jo00099a049research-articleACS PublicationsRequest reuse permissionsArticle...
Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, micromolar hit identified from screen Pfizer fragment library was optimized to afford inhibitors with nanomolar potency cellular assays. The medicinal chemistry effort featured judicious placement lipophilicity, informed by co-crystal structures optimization ADME properties deliver clinical candidate PF-06650833 (compound 40). This compound...
In early 2020, severe acute respiratory syndrome coronavirus 2 (SARS CoV-2) infections leading to COVID-19 disease reached a global level the World Health Organization (WHO) declaration of pandemic. Scientists around globe rapidly responded try and discover novel therapeutics repurpose extant drugs treat disease. This work describes preclinical discovery efforts that led invention PF-07321332 (nirmatrelvir, 14), potent orally active inhibitor SARS CoV-2 main protease (Mpro) enzyme. At outset...
Heteroaromatic thiols may be oxidized to the sulfonyl chloride at low temperature (-25 degrees C) by using 3.3 equiv of aqueous sodium hypochlorite. The reaction is rapid, avoids use chlorine gas, and succeeds with substrates that have previously been found afford little or none sulfonamide product other procedures. method allows preparation fluorides, which are stable enough purified stored, making them potentially useful monomers in parallel chemistry efforts.
Tyrosine kinase 2 (TYK2) is a member of the JAK family that regulates signal transduction downstream receptors for IL-23/IL-12 pathways and type I interferon family, where it pairs with JAK2 or JAK1, respectively. On basis human genetic emerging clinical data, selective TYK2 inhibitor provides an opportunity to treat autoimmune diseases delivering potentially differentiated profile compared currently approved inhibitors. The discovery ATP-competitive pyrazolopyrazinyl series inhibitors was...
Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule antagonists have yet progressed into clinical trials. Investigation series linear peptide ligands to characterization their binding site has enabled the design novel macrocyclic are themselves potent antagonists.
The synthesis and in vitro structure-activity relationships (SAR) of a novel series anilinoquinazolines as allosteric inhibitors fructose-1,6-bisphosphatase (F16Bpase) are reported. compounds have different SAR F16Bpase than previously Selective inhibition can be attained through the addition appropriate polar functional groups at quinazoline 2-position, thus separating inhibitory activity from epidermal growth factor receptor tyrosine kinase observed with similar structures. been found to...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRationally designed, potent competitive inhibitors of leukotriene biosynthesisE. J. Corey, John R. Cashman, Steven S. Kantner, and Stephen W. WrightCite this: Am. Chem. Soc. 1984, 106, 5, 1503–1504Publication Date (Print):March 1, 1984Publication History Published online1 May 2002Published inissue 1 March 1984https://pubs.acs.org/doi/10.1021/ja00317a064https://doi.org/10.1021/ja00317a064research-articleACS PublicationsRequest reuse...
Lipoxygenases are non-heme iron dioxygenases that catalyze the oxygenation of polyunsaturated fatty acids. Using soybean lipoxygenase-1 as a model, we have shown two classes lipoxygenase inhibitors currently in development potential antiinflammatory agents obtain significant amount their potency by reducing active-site from active ferric state to inactive ferrous state. It is not surprising members first these classes, 2-benzyl-1-naphthols, agents. The second class, N-alkyl-hydroxamic acids,...
<s><s></s></s> Brepocitinib is an oral once-daily Janus kinase 1 and Tyrosine 2 selective inhibitor currently in development for the treatment of several autoimmune disorders. Mass balance metabolic profiles were determined using accelerator mass spectrometry six healthy male participants following a single 60 mg dose <sup>14</sup>C-brepocitinib (~300 nCi). The average recovery was 96.7% {plus minus} 6.3% with majority (88.0% 8.0%) recovered urine 8.7% 2.1% feces....
Inhibitors of the glucagon-like peptide-1 (GLP-1) degrading enzyme dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes in animal models and human subjects. A novel series cis-2,5-dicyanopyrrolidine alpha-amino amides were synthesized evaluated as inhibitors treatment diabetes. 1-({[1-(Hydroxymethyl)cyclopentyl]amino}acetyl)pyrrolidine-2,5-cis-dicarbonitrile (1c) is an achiral, slow-binding (time-dependent) inhibitor DPP-IV that selective over other...
We report that the stereochemical outcome of conjugate addition organocopper reagents to bicyclic α,β-unsaturated lactams derived from pyroglutaminol is determined by nature aminal group. Bicyclic in which a ketone have been found afford products syn addition. By contrast, an aldehyde anti These remarkably different results obtained very similar starting materials are unexpected.
The palladium - catalyzed aminocarbonylation of aryl tosylates with amines is reported. Suitable conditions were identified by high throughput reaction screening and then further optimized. substrate scope the respect to tosylate component amine are Competitive aminolysis afford toluenesulfonamides phenol was not observed.
We report that TLR7, IL-6, and the adaptive immune system are essential for autoimmunity glomerulonephritis but not liver pathology in mice expressing ubiquitin-binding–defective ABIN1[D485N] mutant. The blood organs of have exceptionally high numbers patrolling monocytes (pMo), which develop independently IL-6 system. They detectable months before organ seen may diagnostic potential. splenic pMo, inflammatory (iMo), neutrophils expressed levels mRNAs encoding proteins released during...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStereochemistry and mechanism of the biosynthesis leukotriene A4 from 5(S)-hydroperoxy-6(E),8,11,14(Z)-eicosatetraenoic acid. Evidence for an organoiron intermediateE. J. Corey, Stephen W. Wright, Seiichi P. T. MatsudaCite this: Am. Chem. Soc. 1989, 111, 4, 1452–1455Publication Date (Print):February 1, 1989Publication History Published online1 May 2002Published inissue 1 February...