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Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373
- L. Stokes, L. Jiang, +10 authors A. Surprenant
- Biology, Medicine
- British journal of pharmacology
- 1 December 2006
The ATP‐gated P2X7 receptor has been shown to play a role in several inflammatory processes, making it an attractive target for anti‐inflammatory drug discovery. We have recently identified a novel… Expand
The Discovery of MMP7 Inhibitors Exploiting a Novel Selectivity Trigger
Matrilysin or matrix metalloproteinase 7 (MMP7) is a member of a class of zinc-dependent endopeptidases (MMPs) capable of degrading extracellular matrix proteins and thought to play an important role… Expand
Discovery of Potent and Selective Adamantane-Based Small-Molecule P2X7 Receptor Antagonists/Interleukin-1β Inhibitors
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful… Expand
Novel P2X7 receptor antagonists.
- L. Alcaraz, A. Baxter, +12 authors M. Robertson
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 17 November 2003
The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution… Expand
Identification of Antheridiogens in Lygodium circinnatum and Lygodium flexuosum
Antheridiogens in two species of Schizaeaceous ferns, Lygodium circinnatum and Lygodium flexuosum, were analyzed by gas chromatography-mass spectrometry. In L. circinnatum, gibberellin A73 (GA73)… Expand
Structure of an antheridiogen from the fern Anemia mexicana
Abstract A new antheridiogen isolated from gametophytes of the fern Anemia mexicana has been determined to have the structure ent -1α,10β-dihydroxy-9α,15α-cyclo-20-norgibberell-16-ene-7,19-dioic acid… Expand
Antagonists of the P2X(7) receptor. From lead identification to drug development.
A Palladium‐Catalyzed Synthesis of Amidines from Aryl Halides
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
- M. Furber, A. Tidén, +22 authors K. Edman
- Chemistry, Medicine
- Journal of medicinal chemistry
- 14 March 2014
A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were… Expand
Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides
Abstract Palladium-catalysed coupling between aryl- or heteroaryl-bromides, alkoxides, aryloxides or thioalkoxides, and isocyanides gives aryl-imidates and -thioimidates in high yield. Amidines can… Expand