Search Results - "Antrilli, Thomas M."
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Evaluation of PAI-039 [{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid], a novel plasminogen activator inhibitor-1 inhibitor, in a canine model of coronary artery thrombosis
Published in The Journal of pharmacology and experimental therapeutics (01-08-2005)“…We tested a novel, orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) in a canine model of electrolytic injury. Dogs received by oral gavage…”
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Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities
Published in Bioorganic & medicinal chemistry (01-05-2023)“…[Display omitted] GPR40 AgoPAMs are highly effective antidiabetic agents that have a dual mechanism of action, stimulating both glucose-dependent insulin and…”
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Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1
Published in Bioorganic & medicinal chemistry letters (01-08-2005)“…[Display omitted] We synthesized and evaluated a novel series of 2-carboxylic acid indole-based inhibitors of plasminogen activator inhibitor-1 (PAI-1)…”
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Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1
Published in Bioorganic & medicinal chemistry letters (05-07-2004)“…Graphic A novel series of PAI-1 inhibitors containing an oxadiazolidinedione moiety were identified by high through-put screening. Optimization of substituents…”
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Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2010)“…A series of biaryl amides containing an azabicyclo[3.2.1]octane amine headpiece were synthesized and evaluated as mixed arginine vasopressin (AVP) receptor…”
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WAY-140312 reduces plasma PAI-1 while maintaining normal platelet aggregation
Published in Biochemical and biophysical research communications (28-11-2003)“…Plasminogen activator inhibitor-1 (PAI-1) is the major physiological inhibitor of tissue plasminogen activator (tPA) and is elevated in diseases of vascular…”
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Release of PAI-1 by Human Preadipocytes and Adipocytes Independent of Insulin and IGF-1
Published in Biochemical and biophysical research communications (29-12-2000)“…The effect of insulin and insulin-like growth factor-1 (IGF-1) on plasminogen activator inhibitor-1 (PAI-1) release from primary cultures of human…”
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