Search Results - "Klabe, R M"

Inhibition of Clinically Relevant Mutant Variants of HIV-1 by Quinazolinone Non-Nucleoside Reverse Transcriptase Inhibitors by Corbett, Jeffrey W, Ko, Soo S, Rodgers, James D, Gearhart, Lisa A, Magnus, Nicholas A, Bacheler, Lee T, Diamond, Sharon, Jeffrey, Susan, Klabe, Ronald M, Cordova, Beverly C, Garber, Sena, Logue, Kelly, Trainor, George L, Anderson, Paul S, Erickson-Viitanen, Susan K

“…A series of 4-alkenyl and 4-alkynyl-3,4-dihydro-4-(trifluoromethyl)-2-(1H)-quinazolinones were found to be potent non-nucleoside reverse transcriptase…”
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Expanded-Spectrum Nonnucleoside Reverse Transcriptase Inhibitors Inhibit Clinically Relevant Mutant Variants of Human Immunodeficiency Virus Type 1 by Corbett, J W, Ko, S S, Rodgers, J D, Jeffrey, S, Bacheler, L T, Klabe, R M, Diamond, S, Lai, C M, Rabel, S R, Saye, J A, Adams, S P, Trainor, G L, Anderson, P S, Erickson-Viitanen, S K

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Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors by Patel, Mona, McHugh, Robert J, Cordova, Beverly C, Klabe, Ronald M, Erickson-Viitanen, Susan, Trainor, George L, Rodgers, James D

“…A series of 3,3-disubstituted quinoxalinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The N-allyl ( 6b and 6f),…”
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Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA TM) by Patel, Mona, McHugh, Robert J., Cordova, Beverly C., Klabe, Ronald M., Erickson-Viitanen, Susan, Trainor, George L., Ko, Soo S.

“…Two series of benzoxazinones differing in the aromatic substitution pattern were prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The 5-fluoro…”
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Synthesis and evaluation of analogs of Efavirenz (SUSTIVA TM) as HIV-1 reverse transcriptase inhibitors by Patel, Mona, Ko, Soo S., McHugh, Robert J., Markwalder, Jay A., Srivastava, Anurag S., Cordova, Beverly C., Klabe, Ronald M., Erickson-Viitanen, Susan, Trainor, George L., Seitz, Steven.P.

“…Efavirenz (SUSTIVA TM) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse…”
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Thermodynamic linkage between the binding of protons and inhibitors to HIV-1 protease by TRYLSKA, JOANNA, ANTOSIEWICZ, JAN, GELLER, MACIEJ, HODGE, C. NICHOLAS, KLABE, RONALD M., HEAD, MARTHA S., GILSON, MICHAEL K.

“…The aspartyl dyad of free HIV-1 protease has apparent pKas of ∼3 and ∼6, but recent NMR studies indicate that the aspartyl dyad is fixed in the doubly…”
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Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: Novel biaryl indazoles as P2/P2′ substituents by Patel, Mona, Rodgers, James D., McHugh, Robert J., Johnson, Barry L., Cordova, Beverly C., Klabe, Ronald M., Bacheler, Lee T., Erickson-Viitanen, Susan, Ko, Soo S.

“…The preparation of unsymmetrical cyclic ureas bearing novel biaryl indazoles as P2/P2′ substituents was undertaken, utilizing a Suzuki coupling reaction as the…”
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Preparation and Structure−Activity Relationship of Novel P1/P1‘-Substituted Cyclic Urea-Based Human Immunodeficiency Virus Type-1 Protease Inhibitors by Nugiel, David A, Jacobs, Kim, Worley, Tabitha, Patel, Mona, Kaltenbach, Robert F, Meyer, Dayton T, Jadhav, Prabhakar K, De Lucca, George V, Smyser, Thomas E, Klabe, Ronald M, Bacheler, Lee T, Rayner, Marlene M, Seitz, Steven P

“…A series of novel P1/P1‘-substituted cyclic urea-based HIV-1 protease inhibitors was prepared. Three different synthetic schemes were used to assemble these…”
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Potency and selectivity of inhibition of human immunodeficiency virus protease by a small nonpeptide cyclic urea, DMP 323 by ERICKSON-VIITANEN, S, KLABE, R. M, CAWOOD, P. G, O'NEAL, P. L, MEEK, J. L

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Stereoisomers of Cyclic Urea HIV-1 Protease Inhibitors:  Synthesis and Binding Affinities by Kaltenbach, Robert F, Nugiel, David A, Lam, Patrick Y. S, Klabe, Ronald M, Seitz, Steven P

“…We have synthesized stereoisomers of cyclic urea HIV-1 protease inhibitors to study the effect of varying configurations on binding affinities. Four different…”
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Design, Synthesis, and Evaluation of Tetrahydropyrimidinones as an Example of a General Approach to Nonpeptide HIV Protease Inhibitors by De Lucca, George V, Liang, Jing, Aldrich, Paul E, Calabrese, Joe, Cordova, Beverly, Klabe, Ronald M, Rayner, Marlene M, Chang, Chong-Hwan

“…Re-examination of the design of the cyclic urea class of HIV protease (HIVPR) inhibitors suggests a general approach to designing novel nonpeptide cyclic HIVPR…”
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Nonsymmetric P2/P2‘ Cyclic Urea HIV Protease Inhibitors. Structure−Activity Relationship, Bioavailability, and Resistance Profile of Monoindazole-Substituted P2 Analogues by De Lucca, George V, Kim, Ui T, Liang, Jing, Cordova, Beverly, Klabe, Ronald M, Garber, Sena, Bacheler, Lee T, Lam, Gilbert N, Wright, Matthew R, Logue, Kelly A, Erickson-Viitanen, Susan, Ko, Soo S, Trainor, George L

“…Using the structural information gathered from the X-ray structures of various cyclic urea/HIVPR complexes, we designed and synthesized many nonsymmetrical…”
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Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2′ groups by Rodgers, James D., Johnson, Barry L., Haisheng, Wang, Erickson-Viitanen, Susan, Klabe, Ronald M., Bacheler, Lee, Cordova, Beverly C., Chang, Chong-Hwan

“…Cyclic ureas containing 3-aminoindazole P2/P2′ groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a K i × 0.01 nM but…”
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Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors by CORBETT, J. W, GEARHART, L. A, KO, S. S, RODGERS, J. D, CORDOVA, B. C, KLABE, R. M, ERICKSON-VIITANEN, S. K

“…Benzothiadiazine non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV have been synthesized via a novel process to afford active inhibitors, with…”
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The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: Modifications of the P1/P1′ residues by Patel, Mona, Bacheler, Lee T., Rayner, Marlene M., Cordova, Beverly C., Klabe, Ronald M., Erickson-Viitanen, Susan, Seitz, Steven P.

“…Two series of cyclic ureas modified at the P1/P1′ residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds…”
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Does a diol cyclic urea inhibitor of HIV-1 protease bind tighter than its corresponding alcohol form? A study by free energy perturbation and continuum electrostatics calculations by Wang, L, Duan, Y, Stouten, P, De Lucca, G V, Klabe, R M, Kollman, P A

“…The cyclic urea inhibitors of HIV-1 protease generally have two hydroxyl groups on the seven-membered ring. In this study, free energy perturbation and…”
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Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1′ substituents by Kaltenbach, Robert F., Klabe, Ronald M., Cordova, Beverly C., Seitz, Steven P.

“…A series of alkyl substituted P1/P1′ analogs was prepared in an attempt to increase translation of the 3-aminoindazole class of HIV protease inhibitors…”
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The synthesis of symmetrical and unsymmetrical P1/P1′ cyclic ureas as HIV protease inhibitors by Patel, Mona, Kaltenbach, Robert F., Nugiel, David A., McHugh, Robert J., Jadhav, Prabhakar K., Bacheler, Lee T., Cordova, Beverly C., Klabe, Ronald M., Erickson-Viitanen, Susan, Garber, Sena, Reid, Carol, Seitz, Steven P.

“…Cyclic urea SD146, a potent HIV protease inhibitor bearing a flat resistance profile, possessed poor solubility and bioavailability, which precluded further…”
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Improved P1/P1‘ Substituents for Cyclic Urea Based HIV-1 Protease Inhibitors:  Synthesis, Structure−Activity Relationship, and X-ray Crystal Structure Analysis by Nugiel, David A, Jacobs, Kim, Cornelius, Lyndon, Chang, Chong-Hwan, Jadhav, Prabhakar K, Holler, Edward R, Klabe, Ronald M, Bacheler, Lee T, Cordova, Beverly, Garber, Sena, Reid, Carol, Logue, Kelly A, Gorey-Feret, Lorraine J, Lam, Gilbert N, Erickson-Viitanen, Susan, Seitz, Steven P

“…We present several novel P1/P1‘ substituents that can replace the characteristic benzyl P1/P1‘ moiety of the cyclic urea based HIV protease inhibitor series…”
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Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors by PATEL, Mona, MCHUGH, Robert J, CORDOVA, Beverly C, KLABE, Ronald M, BACHELER, Lee T, ERICKSON-VIITANEN, Susan, RODGERS, James D

“…A series of 4,4-disubstituted quinolinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The C-3 substituted compound 9h displayed…”
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