Search Results - "DORN, Conrad P"
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Orally active .beta.-lactam inhibitors of human leukocyte elastase-1. Activity of 3,3-diethyl-2-azetidinones
Published in Journal of medicinal chemistry (01-10-1992)“…A thorough analysis of the mechanism of inhibition of human leukocyte elastase (HLE) by a monocyclic beta-lactam and the mechanism of beta-lactam hydrolysis…”
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2
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes
Published in Bioorganic & medicinal chemistry letters (22-01-2001)“…Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded…”
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3
Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs
Published in Journal of medicinal chemistry (23-03-2000)“…The regioselective dibenzylphosphorylation of 2 followed by catalytic reduction in the presence of N-methyl-d-glucamine afforded…”
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4
Orally active .beta.-lactam inhibitors of human leukocyte elastase. 2. Effect of C-4 substitution
Published in Journal of medicinal chemistry (01-03-1993)“…The effect of changing the C-4 substituent of 3,3-diethyl-1-[(benzylamino)carbonyl]-2-azetidinone on inhibition of HLE and in a model of HLE-induced lung…”
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5
Expression and characterization of the chemokine receptor CCR2B from rhesus monkey
Published in Biochemical pharmacology (15-07-2003)“…Species selectivity of chemokine receptor antagonists is a potential deterrent to making preclinical assessments in vivo. To determine if rhesus monkey disease…”
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Cephalosporin antibiotics can be modified to inhibit human leukocyte elastase
Published in Nature (London) (10-07-1986)“…Several laboratories, including our own have reported the synthesis and activity of certain low relative molecular mass inhibitors of mammalian serine…”
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7
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters
Published in Journal of medicinal chemistry (01-09-1990)“…Time-dependent inhibitors of the enzyme human leukocyte elastase have been developed based on the cephem nucleus. A series of cephalosporin tert-butyl esters…”
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8
Synthesis and immunoadjuvant activities of 2-acetamido-5-O-acetyl-6-O-acyl-2-deoxy-3-O-[(R)-2-propionyl-L-alanyl-D-isoglutamine]-D-glucofuranoses as potential prodrug forms of 6-O-acyl derivatives of N-acetylmuramyl dipeptide
Published in Journal of medicinal chemistry (01-09-1982)“…2-Acetamido-5-O-acetyl-6-O-acyl-2-deoxy-3-O-[(R)-2-propionyl-L-alanyl-D- isoglutamine]-D-glucofuranoses, designed as prodrug forms of the corresponding…”
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9
Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b,e]dioxepinacetic acids
Published in Journal of medicinal chemistry (01-08-1986)“…A new class of tricyclic arylacetic acids was synthesized and evaluated as antiinflammatory/analgesic agents as well as inhibitors of prostaglandin synthetase…”
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Proteinase inhibitors. 1. Inhibitors of elastase
Published in Journal of medicinal chemistry (01-11-1977)Get full text
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11
Steroids. IX. Synthesis of some thiazolosteroids
Published in Journal of pharmaceutical sciences (01-05-1962)Get more information
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12
Chemical, Biochemical, Pharmacokinetic, and Biological Properties of L-680, 833: A Potent, Orally Active Monocyclic β-Lactam Inhibitor of Human Polymorphonuclear Leukocyte Elastase
Published in Proceedings of the National Academy of Sciences - PNAS (15-09-1993)“…A series of potent and highly selective time-dependent monocyclic β-lactam inhibitors of human polymorphonuclear leukocyte elastase (PMNE, EC 3.4.21.37) is…”
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13
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol
Published in Journal of medicinal chemistry (01-10-1992)“…Human leukocyte elastase (HLE) is a serine protease which has been implicated as a causative agent in several pulmonary diseases. The continued modification of…”
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14
Synthesis and acylation of 2‐nitro‐11 H ‐dibenzo[ b,e ][1,4]dioxepin
Published in Journal of heterocyclic chemistry (01-05-1986)“…A one‐pot synthesis of the 11 H ‐dibenzo[ b,e ]1,4]dioxepin ring system from catechol and an o ‐chlorobenzyl chloride is described. Friedel‐Crafts acylation…”
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15
Structure of Human Neutrophil Elastase in Complex with a Peptide Chloromethyl Ketone Inhibitor at 1.84- angstrom Resolution
Published in Proceedings of the National Academy of Sciences - PNAS (01-01-1989)“…Human neutrophil elastase (HNE) has been implicated as a major contributor to tissue destruction in various disease states, including emphysema. The structure…”
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16
Synthesis and acylation of 2-nitro-11H-dibenzo[b,e][1,4]dioxepin
Published in Journal of heterocyclic chemistry (01-05-1986)“…A one‐pot synthesis of the 11H‐dibenzo[b,e]1,4]dioxepin ring system from catechol and an o‐chlorobenzyl chloride is described. Friedel‐Crafts acylation occurs…”
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17
Synthesis of 24-dehydrocholecalciferol
Published in Steroids (01-03-1980)Get more information
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18
Steroids. VI. Thiazoloandrostanes
Published in Journal of pharmaceutical sciences (01-03-1961)Get more information
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