Search Results - "WIDEBURG, N"

Discovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy by Kempf, Dale J, Sham, Hing L, Marsh, Kennan C, Flentge, Charles A, Betebenner, David, Green, Brian E, McDonald, Edith, Vasavanonda, Sudthida, Saldivar, Ayda, Wideburg, Norman E, Kati, Warren M, Ruiz, Lisa, Zhao, Chen, Fino, LynnMarie, Patterson, Jean, Molla, Akhteruzzaman, Plattner, Jacob J, Norbeck, Daniel W

“…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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Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor by HO, D. D, TOYOSHIMA, T, HONGMEI MO, KEMPF, D. J, NORBECK, D, CHIH-MING CHEN, WIDEBURG, N. E, BURT, S. K, ERICKSON, J. W, SINGH, M. K

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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 by Kempf, Dale J, Codacovi, Lynnmarie, Wang, Xiu Chun, Kohlbrenner, William E, Wideburg, Norman E, Saldivar, Ayda, Vasavanonda, Sudthida, Marsh, Kennan C, Bryant, Pamela

“…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 by Sham, Hing L, Zhao, Chen, Stewart, Kent D, Betebenner, David A, Lin, Shuqun, Park, Chang H, Kong, Xiang-P, Rosenbrook, William, Herrin, Thomas, Madigan, Darold, Vasavanonda, Suthida, Lyons, Nicholas, Molla, Akhter, Saldivar, Ayda, Marsh, Kennan C, McDonald, Edith, Wideburg, Norman E, Denissen, Jon F, Robins, Terrel, Kempf, Dale J, Plattner, Jacob J, Norbeck, Daniel W

“…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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Induction of calf thymus topoisomerase II-mediated DNA breakage by the antibacterial isothiazoloquinolones A-65281 and A-65282 by KOHLBRENNER, W. E, WIDEBURG, N, WEIGL, D, SALDIVAR, A, CHU, D. T. W

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Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel p3 ligands by XIAOQI CHEN, KEMPF, D. J, MCDONALD, E, NORBECK, D. W, SHAM, H. L, GREEN, B. E, MOLLA, A, KORNEYEVA, M, VASAVANONDA, S, WIDEBURG, N. E, SALDIVAR, A, MARSH, K. C

“…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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Potent Inhibitors of the HIV-1 Protease with Good Oral Bioavailabilities by Sham, H.L., Zhao, C., Marsh, K.C., Betebenner, D.A., Lin, S.Q., Mcdonald, E., Vasavanonda, S., Wideburg, N., Saldivar, A., Robins, T., Kempf, D.J., Plattner, J.J., Norbeck, D.W.

“…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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ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease by SHAM, H. L, KEMPF, D. J, BETEBENNER, D, KORNEYEVA, M, VASAVANONDA, S, MCDONALD, E, SALDIVAR, A, WIDEBURG, N, XIAOOI CHEN, PING NIU, CHANG PARK, JAYANTI, V, MOLLA, A, GRABOWSKI, B, GRANNEMAN, G. R, SUN, E, JAPOUR, A. J, LEONARD, J. M, PLATTNER, J. J, NORBECK, D. W, MARSH, K. C, KUMAR, G. N, CHEN, C.-M, KATI, W, STEWART, K, LAL, R, HSU, A

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Potent HIV-1 protease inhibitors with antiviral activities in vitro by Sham, H L, Betebenner, D A, Wideburg, N E, Saldivar, A C, Kohlbrenner, W E, Vasavanonda, S, Kempf, D J, Norbeck, D W, Zhao, C, Clement, J J

“…A series of novel difluoroketones with low molecular weight (less than 600 m.u.) and which are potent inhibitors of the HIV-1 protease (IC50 = 1.0 to 21 nM)…”
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Novel Azacyclic Ureas That Are Potent Inhibitors of HIV-1 Protease by Sham, Hing L., Zhao, Chen, Marsh, Kennan C., Betebenner, David A., Lin, Shuqun, Jr, William Rosenbrook, Herrin, Thomas, Li, Leping, Madigan, Darold, Vasavanonda, Suthida, Molla, Akhter, Saldivar, Ayda, McDonald, Edith, Wideburg, Norman E., Kempf, Dale, Norbeck, Daniel W., Plattner, Jacob J.

“…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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Lack of stereospecificity in the binding of the P2 amino acid of ritonavir to HIV protease by Kempf, Dale J., Molla, Akhteruzzaman, Marsh, Kennan C., Park, Chang, Rodrigues, A.David, Korneyeva, Marina, Vasavanonda, Sudthida, McDonald, Edith, Flentge, Charles A., Muchmore, Steven, Wideburg, Norman E., Saldivar, Ayda, Cooper, Art, Kati, Warren M., Stewart, Kent D., Norbeck, Daniel W.

“…The biological and pharmacokinetic properties of the HIV protease inhibitor ritonavir and its D-valinyl diastereomer, A-117673, were found to be…”
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Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease by Erickson, J, Neidhart, D J, VanDrie, J, Kempf, D J, Wang, X C, Norbeck, D W, Plattner, J J, Rittenhouse, J W, Turon, M, Wideburg, N

“…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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Influence of stereochemistry on activity and binding modes for C2 symmetry-based diol inhibitors of HIV-1 protease by Hosur, Madhusoodan V, Bhat, T. Narayana, Kempf, Dale J, Baldwin, Eric T, Liu, Beishan, Gulnik, Sergei, Wideburg, Norman E, Norbeck, Daniel W, Appelt, Krzysztof, Erickson, John W

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Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores by Wang, Gary T, Li, Sam, Wideburg, Norman, Krafft, Grant A, Kempf, Dale J

“…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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Antiviral and pharmacokinetic properties of C2 symmetric inhibitors of the human immunodeficiency virus type 1 protease by Kempf, D J, Marsh, K C, Paul, D A, Knigge, M F, Norbeck, D W, Kohlbrenner, W E, Codacovi, L, Vasavanonda, S, Bryant, P, Wang, X C

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Design of orally bioavailable, symmetry-based inhibitors of HIV protease by Kempf, D J, Marsh, K C, Fino, L C, Bryant, P, Craig-Kennard, A, Sham, H L, Zhao, C, Vasavanonda, S, Kohlbrenner, W E, Wideburg, N E

“…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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ABT-538 is a Potent Inhibitor of Human Immunodeficiency Virus Protease and has High Oral Bioavailability in Humans by Kempf, Dale J., Marsh, Kennan C., Denissen, Jon F., McDonald, Edith, Vasavanonda, Sudthida, Flentge, Charles A., Green, Brian E., Fino, Lynnmarie, Park, Chang H., Kong, Xiang-Peng, Wideburg, Norman E., Saldivar, Ayda, Ruiz, Lisa, Kati, Warren M., Sham, Hing L., Robins, Terry, Stewart, Kent D., Hsu, Ann, Plattner, Jacob J., Leonard, John M., Norbeck, Daniel W.

“…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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Synthetic chemical diversity: Solid phase synthesis of libraries of C sub(2) symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores by Wang, G T, Li, S, Wideburg, N, Krafft, G A, Kempf, D J

“…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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Influence of stereochemistry on activity and binding modes for C sub(2) symmetry-based diol inhibitors of HIV-1 protease by Hosur, M V, Bhat, T N, Kempf, D J, Baldwin, E T, Liu, B, Gulnik, S, Wideburg, N E, Norbeck, D W, Appelt, K, Erickson, J W

“…The incorporation of C sub(2) symmetry has become a useful paradigm in the design of active site inhibitors for HIV-1 protease (HIV PR) and has led to the…”
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Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C sub(2)-symmetric protease inhibitor by Ho, D D, Toyoshima, T, Mo, Hongmei, Kempf, D J, Norbeck, D, Chen, Chih-Ming, Wideburg, N E, Burt, S K, Erickson, J W, Singh, M K

“…Inhibitors of the human immunodeficiency virus type 1 protease represent a promising class of antiviral drugs for the treatment of AIDS, and several are now in…”
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