Search Results - "CASPER, Martin"
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1
Structure−Activity Relationships of Novel 2-Substituted Quinazoline Antibacterial Agents
Published in Journal of medicinal chemistry (04-11-1999)“…High-throughput screening of in-house compound libraries led to the discovery of a novel antibacterial agent, compound 1 (MIC: 12−25 μM against S. pyogenes)…”
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2
Discovery and Structure−Activity Relationship of 3-Methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Published in Journal of medicinal chemistry (10-06-2010)“…Serotonin, which is stored in platelets and is released during thrombosis, activates platelets via the 5-HT2A receptor. 5-HT2A receptor inverse agonists thus…”
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3
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluation
Published in Bioorganic & medicinal chemistry letters (01-11-2009)“…A series of pyrimidine analogues derived from ATC0175 were potent antagonists of human MCH-R1 in vitro with improved receptor selectivity. One example was…”
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4
Uniformly modified 2'-deoxy-2'-fluoro-phosphorothioate oligonucleotides as nuclease-resistant antisense compounds with high affinity and specificity for RNA targets
Published in Journal of medicinal chemistry (02-04-1993)“…"Uniformly" modified phosphodiester or phosphorothioate oligonucleotides incorporating 2'-deoxy-2'-fluoroadenosine, -guanosine, -uridine, and -cytidine,…”
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5
Allyl Group as a Protecting Group for Internucleotide Phosphate and Thiophosphate Linkages in Oligonucleotide Synthesis: Facile Oxidation and Deprotection Conditions
Published in Organic letters (10-02-2000)“…The allyl group, which serves as a protecting group for an internucleotide bond for both phosphates and phosphorothioates, can be easily removed by good…”
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6
Weaning From Mechanical Ventilation in Skilled Nursing Facility: A Multicenter Study
Published in Chest (01-04-2016)Get full text
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7
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (15-09-2009)Get full text
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8
Discovery and Structure−Activity Relationship of 3-Methoxy- N -(3-(1-methyl-1 H -pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine 2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Published in Journal of medicinal chemistry (10-06-2010)Get full text
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9
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1
Published in Bioorganic & medicinal chemistry letters (01-09-2005)“…The synthesis and SAR of 4-(dimethylamino)quinazolines as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists are reported, leading to the discovery…”
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10
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT sub(2A) inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…Potent 5-HT sub(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in…”
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11
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1
Published in Bioorganic & medicinal chemistry letters (16-05-2005)“…High-throughput screening of our in-house GPCR-directed library uncovered a series of 4-(dimethylamino)quinazolines as melanin-concentrating hormone receptor 1…”
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12
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT 2A inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (2009)“…Potent 5-HT 2A inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective…”
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13
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…Potent 5-HT(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective…”
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14
Synthesis, hybridization, and nuclease resistance properties of 2′-O-aminooxyethyl ( 2′-O-AOE) modified oligonucleotides
Published in Tetrahedron letters (22-01-1999)“…The novel RNA mimic 2′-O-AOE has been incorporated into antisense oligonucleotides. This 2′-O-modification significantly enhances hybridization against target…”
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