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Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373
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 novelExpand
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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 roleExpand
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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 usefulExpand
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Novel P2X7 receptor antagonists.
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 distributionExpand
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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
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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 acidExpand
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Antagonists of the P2X(7) receptor. From lead identification to drug development.
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Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
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 wereExpand
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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 canExpand
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