Search Results - "McElroy, Andrew B."
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Synthesis of Macrocyclic, Potential Protease Inhibitors Using a Generic Scaffold
Published in Journal of organic chemistry (12-07-2002)“…A generic macrocyclic peptide structure 2 was designed as a potential inhibitor of a range of proteinases, by using as a basis for the design the known…”
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Discovery of Potent & Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor for the Treatment of Thrombosis
Published in Journal of medicinal chemistry (29-11-2007)“…Thrombin-activatable fibrinolysis inhibitor (TAFI) has emerged as a key link between the coagulation and fibrinolysis cascades and represents a promising new…”
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Regulation of tumour necrosis factor-α processing by a metalloproteinase inhibitor
Published in Nature (London) (18-08-1994)“…Tumour necrosis factor-alpha (TNF-alpha) is a potent pro-inflammatory agent produced primarily by activated monocytes and macrophages. TNF-alpha is synthesized…”
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Structure of the Catalytic Domain of Fibroblast Collagenase Complexed with an Inhibitor
Published in Science (American Association for the Advancement of Science) (21-01-1994)“…Collagenase is a zinc-dependent endoproteinase and is a member of the matrix metalloproteinase (MMP) family of enzymes. The MMPs participate in connective…”
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Conformationally constrained tachykinin analogs: potent and highly selective neurokinin NK-2 receptor agonists
Published in Journal of medicinal chemistry (01-10-1992)“…The design and synthesis of potent and selective neurokinin NK-2 receptor agonists 12 (GR64349) and 31 are described, together with structure-activity…”
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New .kappa.-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus
Published in Journal of medicinal chemistry (01-02-1992)“…The syntheses of some 1-[(3,4-dichlorophenyl)acetyl]-2- [(alkylamino)methyl]piperidines and their activities as kappa-opioid receptor agonists are described…”
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Design of Selective Thrombin Inhibitors Based on the (R)-Phe-Pro-Arg Sequence
Published in Journal of medicinal chemistry (06-06-2002)“…Potent and selective inhibitors of thrombin were sought based on the (R)-Phe-Pro-Arg sequence. The objective was to generate similar binding interactions to…”
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Matrix Metalloproteinase Inhibitors Containing a [(Carboxyalkyl)amino]zinc Ligand: Modification of the P1 and P2' Residues
Published in Journal of medicinal chemistry (01-03-1994)Get full text
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Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor
Published in Journal of medicinal chemistry (01-07-1992)“…Incorporation of D-Pro9 into substance P related peptides is known to enhance neurokinin NK-2 receptor agonist potency and selectivity with respect to other…”
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New Spiropiperidines as Potent and Selective Non-Peptide Tachykinin NK2 Receptor Antagonists
Published in Journal of medicinal chemistry (01-09-1995)“…The synthesis of a series of 2-(5-fluoro-1H-indol-3-yl)ethyl spiropiperidines is described together with their tachykinin NK2 receptor affinities measured in a…”
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Synthesis, antinociceptive activity and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols
Published in Journal of medicinal chemistry (01-01-1992)“…A series of trans-3-(6- and 7-substituted-decahydro-4a-isoquinolinyl)phenols and trans-3-(octahydro-4a-isoquinolinyl)phenols have been synthesized as potential…”
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Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand : modification of the P1 and P2' residues
Published in Journal of medicinal chemistry (04-03-1994)“…Systematic modification of the presumed P1 side chain in a series of (carboxyalkyl)amino-based inhibitors of matrix metalloproteinases enabled identification…”
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14
Regulation of tumour necrosis factor- alpha processing by a metallproteinase inhibitor
Published in Nature (London) (01-01-1994)“…Tumour necrosis factor- alpha (TNF- alpha ) is potent pro-inflammatory agent produced primarily by activated monocytes and macrophages. TNF- alpha is…”
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