Search Results - "Wideburg, Norman"
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Discovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy
Published in Journal of medicinal chemistry (12-02-1998)“…The structure−activity studies leading to the potent and clinically efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately…”
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Synthesis and SAR studies of potent HIV protease inhibitors containing novel dimethylphenoxyl acetates as P2 ligands
Published in Bioorganic & medicinal chemistry letters (03-11-2003)“…Isopropyl substituted 4-thioazolyl valine side chains are highly optimized P(2)-P(3) ligands for C2 symmetry-based HIV protease inhibitors, as exemplified by…”
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3
Influence of stereochemistry on activity and binding modes for C2 symmetry-based diol inhibitors of HIV-1 protease
Published in Journal of the American Chemical Society (01-02-1994)Get full text
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Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol
Published in Journal of medicinal chemistry (01-02-1993)“…The structure-activity relationships in two series of novel, symmetry-based inhibitors of HIV protease, the enzyme responsible for maturation of the human…”
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A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease
Published in Journal of medicinal chemistry (19-01-1996)“…The design, synthesis, and molecular modeling studies of a novel series of azacyclic ureas, which are inhibitors of human immunodeficiency virus type 1 (HIV-1)…”
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6
Synthesis and SAR studies of potent HIV protease inhibitors containing novel dimethylphenoxyl acetates as P 2 ligands
Published in Bioorganic & medicinal chemistry letters (01-11-2003)Get full text
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7
ABT-538 is a Potent Inhibitor of Human Immunodeficiency Virus Protease and has High Oral Bioavailability in Humans
Published in Proceedings of the National Academy of Sciences - PNAS (28-03-1995)“…Examination of the structural basis for antiviral activity, oral pharmacokinetics, and hepatic metabolism among a series of symmetry-based inhibitors of the…”
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Structure-based, C2 symmetric inhibitors of HIV protease
Published in Journal of medicinal chemistry (01-10-1990)Get full text
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Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor
Published in Journal of Virology (01-03-1994)“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease
Published in Science (American Association for the Advancement of Science) (03-08-1990)“…A two-fold (C2) symmetric inhibitor of the protease of human immunodeficiency virus type-1 (HIV-1) has been designed on the basis of the three-dimensional…”
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11
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores
Published in Journal of medicinal chemistry (01-08-1995)“…Solid phase synthesis of non-oligomeric organic compounds has been pursued for high-efficiency generation of large numbers of structurally diverse compounds…”
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12
A new aminoglycoside antibiotic complex--the seldomycins. IV. The structure of seldomycin factor 5
Published in Journal of antibiotics (01-01-1977)Get more information
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13
Evaluation of furofuran as a P2 ligand for symmetry-based HIV protease inhibitors
Published in Bioorganic & medicinal chemistry letters (03-12-1996)Get full text
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14
Design of orally bioavailable, symmetry-based inhibitors of HIV protease
Published in Bioorganic & medicinal chemistry (01-09-1994)“…A series of novel inhibitors of HIV-1 protease with excellent oral bioavailability is described. Differential acylation of the two amino groups of…”
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15
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P 3 ligands
Published in Bioorganic & medicinal chemistry letters (15-12-1998)“…The 2-isopropyl thiazolyl group is a highly optimized P 3 ligand for C 2 symmetry-based HIV protease inhibitors, as exemplified in the drug ritonavir. Here we…”
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16
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel p3 ligands
Published in Bioorganic & medicinal chemistry letters (15-12-1998)“…The 2-isopropyl thiazolyl group is a highly optimized P3 ligand for C2 symmetry-based HIV protease inhibitors, as exemplified in the drug ritonavir. Here we…”
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17
Evaluation of substituted benzamides as P2 ligands for symmetry-based inhibitors of HIV protease
Published in Bioorganic & medicinal chemistry letters (16-11-1995)“…Substituted benzamides were evaluated as P2 ligands for symmetry-based HIV protease inhibitors. In contrast to previous reports, 2-methyl substitution provided…”
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18
Evaluation of furofuran as a P 2 ligand for symmetry-based HIV protease inhibitors
Published in Bioorganic & medicinal chemistry letters (03-12-1996)“…The hexahydrofurofuranyloxy group was evaluated as a conformationally constrained P 2 ligand for symmetry-based HIV protease inhibitors. A number of compounds…”
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Novel Azacyclic Ureas That Are Potent Inhibitors of HIV-1 Protease
Published in Biochemical and biophysical research communications (14-08-1996)“…A series of novel, azacyclic ureas which are highly potent inhibitors of the HIV-1 protease (IC50= 4.1 to <0.5 nM) were synthesized. Aqueous solubilities of…”
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Potent Inhibitors of the HIV-1 Protease with Good Oral Bioavailabilities
Published in Biochemical and biophysical research communications (06-06-1995)“…A series of novel pseudo-symmetrical and unsymmetrical inhibitors based on the backbone modification of a peptidomimetic were synthesized and found to be…”
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