L-735,524 - THE DESIGN OF A POTENT AND ORALLY BIOAVAILABLE HIV PROTEASE INHIBITOR
DORSEY, BD, LEVIN, RB, MCDANIEL, SL, VACCA, JP, GUARE, JP, DARKE, PL, ZUGAY, JA, EMINI, EA, SCHLEIF, WA, QUINTERO, JC, LIN, JH, CHEN, IW, HOLLOWAY, MK, FITZGERALD, PMD, AXEL, MG, OSTOVIC, D, ANDERSON, PS, HUFF
Published in Journal of medicinal chemistry (14.10.1994)
Published in Journal of medicinal chemistry (14.10.1994)
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Journal Article
Nonpeptidal P-2 ligands for HIV protease inhibitors: Structure-based design, synthesis, and biological evaluation
Ghosh, AK, Kincaid, JF, Walters, DE, Chen, Y, Chaudhuri, NC, Thompson, WJ, Culberson, C, Fitzgerald, PMD, Lee, HY, McKee, SP, Munson, PM, Duong, TT, Darke, PL, Zugay, JA, Schleif, WA, Axel, MG, Lin, J, Huff
Published in Journal of medicinal chemistry (16.08.1996)
Published in Journal of medicinal chemistry (16.08.1996)
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Journal Article
L-735,524: The Design of a Potent and Orally Bioavailable HIV Protease Inhibitor
Dorsey, Bruce D, Levin, Rhonda B, McDaniel, Stacy L, Vacca, Joseph P, Guare, James P, Darke, Paul L, Zugay, Joan A, Emini, Emilio A, Schleif, William A
Published in Journal of medicinal chemistry (01.10.1994)
Published in Journal of medicinal chemistry (01.10.1994)
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Journal Article
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents : X-ray crystal structure assisted design
THOMPSON, W. J, FITZGERALD, P. M. D, SCHWERING, J. E, HOMMICK, C. F, NUNBERG, J, SPRINGER, J. P, HUFF, J. R, HOLLOWAY, M. K, EMINI, E. A, DARKE, P. L, MCKEEVER, B. M, SCHLEIF, W. A, QUINTERO, J. C, ZUGAY, J. A, TUCKER, T. J
Published in Journal of medicinal chemistry (15.05.1992)
Published in Journal of medicinal chemistry (15.05.1992)
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Journal Article
Dissociation and association of the HIV-1 protease dimer subunits: Equilibria and rates
Darke, Paul L, Hall, Dawn L, Jordan, Susan P, Zugay, Joan A, Shafer, Jules A, Kuo, Lawrence C
Published in Biochemistry (Easton) (11.01.1994)
Published in Biochemistry (Easton) (11.01.1994)
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THE DEVELOPMENT OF CYCLIC SULFOLANES AS NOVEL AND HIGH-AFFINITY P(2) LIGANDS FOR HIV-1 PROTEASE INHIBITORS
GHOSH, AK, LEE, HY, THOMPSON, WJ, CULBERSON, C, HOLLOWAY, MK, MCKEE, SP, MUNSON, PM, DUONG, TT, SMITH, AM, DARKE, PL, ZUGAY, JA, EMINI, EA, SCHLEIF, WA, HUFF, ANDERSON, PS
Published in Journal of medicinal chemistry (15.04.1994)
Published in Journal of medicinal chemistry (15.04.1994)
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Journal Article
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors
Ghosh, Arun K, Thompson, Wayne J, McKee, Sean P, Duong, Tien T, Lyle, Terry A, Chen, Jenny C, Darke, Paul L, Zugay, Joan A, Emini, Emilio A
Published in Journal of medicinal chemistry (1993)
Published in Journal of medicinal chemistry (1993)
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Journal Article
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors
Lyle, Terry A, Wiscount, Catherine M, Guare, James P, Thompson, Wayne J, Anderson, Paul S, Darke, Paul L, Zugay, Joan A, Emini, Emilio A, Schleif, William A
Published in Journal of medicinal chemistry (01.03.1991)
Published in Journal of medicinal chemistry (01.03.1991)
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Journal Article
CYCLIC SULFOLANES AS NOVEL AND HIGH-AFFINITY P-2 LIGANDS FOR HIV-1 PROTEASE INHIBITORS
GHOSH, AK, THOMPSON, WJ, LEE, HY, MCKEE, SP, MUNSON, PM, DUONG, TT, DARKE, PL, ZUGAY, JA, EMINI, EA, SCHLEIF, WA, HUFF, ANDERSON, PS
Published in Journal of medicinal chemistry (02.04.1993)
Published in Journal of medicinal chemistry (02.04.1993)
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Journal Article
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity
Tucker, Thomas J, Lumma, William C, Payne, Linda S, Wai, Jenny M, De Solms, S. Jane, Giuliani, Elizabeth A, Darke, Paul L, Heimbach, Jill C, Zugay, Joan A
Published in Journal of medicinal chemistry (01.07.1992)
Published in Journal of medicinal chemistry (01.07.1992)
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Journal Article
Cycloalkylpiperazines as HIV-1 protease inhibitors: enhanced oral absorption
Moon Kim, B., Evans, Ben E., Gilbert, Kevin F., Hanifin, Colleen M., Vacca, Joseph P., Michelson, Stuart R., Darke, Paul L., Zugay, Joan A., Emini, Emilio A., Schleif, William, Lin, Jiunn H., Chen, I.-W., Vastag, Kari, Anderson, Paul S., Huff, Joel R.
Published in Bioorganic & medicinal chemistry letters (16.11.1995)
Published in Bioorganic & medicinal chemistry letters (16.11.1995)
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Journal Article
Nonpeptidal P sub(2) ligands for HIV protease inhibitors: Structure-based design, synthesis, and biological evaluation
Ghosh, A K, Kincaid, J F, Walters, DE, Chen, Yan, Chaudhuri, N C, Thompson, W J, Culberson, C, Fitzgerald, PMD, Lee, Hee Yoon, McKee, S P, Munson, P M, Duong, T T, Darke, P L, Zugay, JA
Published in Journal of medicinal chemistry (01.01.1996)
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Published in Journal of medicinal chemistry (01.01.1996)
Journal Article
Synthesis and evaluation of pyridyl analogs of L-735,524: Potent HIV-1 protease inhibitors
Dorsey, Bruce D., McDaniel, Stacey L., Levin, Rhonda B., Vacca, Joseph P., Darke, Paul L., Zuga, Joan A., Emini, Emilio A., Schleif, William A., Lin, Jiunn H., Chen, I-W., Holloway, M.Katharine, Anderson, Paul S., Huff, Joel R.
Published in Bioorganic & medicinal chemistry letters (01.12.1994)
Published in Bioorganic & medicinal chemistry letters (01.12.1994)
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Journal Article
Thiophene derivatives as extremely high affinity P 3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors
Moon Kim, B., Guare, James P., Vacca, Joseph D., Michelson, Stuart R., Darke, Paul L., Zugay, Joan A., Emini, Emilio A., Schleif, William, Lin, Jiunn H., Chen, I.W., Vastag, Kari, Anderson, Paul S., Huff, Joel R.
Published in Bioorganic & medicinal chemistry letters (19.01.1995)
Published in Bioorganic & medicinal chemistry letters (19.01.1995)
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Journal Article
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679
DESOLMS, S. J, GIULIANI, E. A, EMINI, E. A, SCHLEIF, W. A, QUINTERO, J. C, ANDERSON, P. S, HUFF, J. R, GUARE, J. P, VACCA, J. P, SANDERS, W. M, GRAHAM, S. L, WIGGINS, J. M, DARKE, P. L, SIGAL, I. S, ZUGAY, J. A
Published in Journal of medicinal chemistry (01.09.1991)
Published in Journal of medicinal chemistry (01.09.1991)
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Journal Article
3-tetrahydrofuran and pyran urethanes as high-affinity P sub(2)-ligands for HIV-1 protease inhibitors
Ghosh, A K, Thompson, W J, McKee, S P, Duong, T T, Lyle, T A, Chen, J C, Darke, P L, Zugay, JA, Emini, E A
Published in Journal of medicinal chemistry (01.01.1993)
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Published in Journal of medicinal chemistry (01.01.1993)
Journal Article
Cyclic sulfolanes as novel and high affinity P sub(2) ligands for HIV-1 protease inhibitors
Ghosh, A K, Thompson, W J, Lee, Hee Yoon, McKee, S P, Munson, P M, Duong, Tien T, Darke, P L, Zugay, JA, Emini, E A
Published in Journal of medicinal chemistry (01.01.1993)
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Published in Journal of medicinal chemistry (01.01.1993)
Journal Article
A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability
Kim, B.Moon, Vacca, Joseph P., Guare, James P., Hanifin, Colleen M., Michelson, Stuart R., Darke, PaulL, Zugay, Joan A., Emini, Emilio A., Schleif, William, Lin, Jiunn H., Chen, I-Wu, Vastag, Kari, Ostovic, Drazen, Anderson, Paul S., Huff, Joel R.
Published in Bioorganic & medicinal chemistry letters (06.10.1994)
Published in Bioorganic & medicinal chemistry letters (06.10.1994)
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Journal Article
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P sub(1) or P sub(1)' phenyl substituents: X-ray crystal structure assisted design
Thompson, W J, Fitzgerald, PMD, Holloway, M K, Emini, E A, Darke, P L, McKeever, B M, Schleif, WA, Quintero, J C, Zugay, JA
Published in Journal of medicinal chemistry (01.01.1992)
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Published in Journal of medicinal chemistry (01.01.1992)
Journal Article
Substituted alkylpyridines as P 3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles
Moon Kim, B., Hanifin, Colleen M., Blair Zartman, C., Vacca, Joseph P., Michelson, Stuart R., Lin, Jiunn H., Chen, I.-W., Vastag, Kari, Darke, Paul L., Zugay, Joan A., Emini, Emilio A., Schleif, William, Anderson, Paul S., Huff, Joel R.
Published in Bioorganic & medicinal chemistry letters (05.10.1995)
Published in Bioorganic & medicinal chemistry letters (05.10.1995)
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Journal Article