Search Results - "BUDHU, Richard J"

Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties by Kim, Dooseop, Wang, Liping, Hale, Jeffrey J., Lynch, Christopher L., Budhu, Richard J., MacCoss, Malcolm, Mills, Sander G., Malkowitz, Lorraine, Gould, Sandra L., DeMartino, Julie A., Springer, Martin S., Hazuda, Daria, Miller, Michael, Kessler, Joseph, Hrin, Renee C., Carver, Gwen, Carella, Anthony, Henry, Karen, Lineberger, Janet, Schleif, William A., Emini, Emilio A.

“…[Display omitted] A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the…”
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Biomimetic synthesis of enantiomerically pure D-myo-inositol derivatives by Bender, Steven L, Budhu, Richard J

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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 by DORN, Conrad P, FINKE, Paul E, DEMARTINO, Julie A, SICILIANO, Salvatore J, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael, OATES, Bryan, SCHLEIF, William A, EMINI, Emilio A, BUDHU, Richard J, MILLS, Sander G, MACCOSS, Malcolm, MALKOWITZ, Lorraine, SPRINGER, Martin S, DAUGHERTY, Bruce L, GOULD, Sandra L

“…Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded…”
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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs by Hale, Jeffrey J, Mills, Sander G, MacCoss, Malcolm, Dorn, Conrad P, Finke, Paul E, Budhu, Richard J, Reamer, Robert A, Huskey, Su-Er W, Luffer-Atlas, Debra, Dean, Brian J, McGowan, Erin M, Feeney, William P, Chiu, Shuet-Hing Lee, Cascieri, Margaret A, Chicchi, Gary G, Kurtz, Marc M, Sadowski, Sharon, Ber, Elzbieta, Tattersall, F. David, Rupniak, Nadia M. J, Williams, Angela R, Rycroft, Wayne, Hargreaves, Richard, Metzger, Joseph M, MacIntyre, D. Euan

“…The regioselective dibenzylphosphorylation of 2 followed by catalytic reduction in the presence of N-methyl-d-glucamine afforded…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements by Hale, Jeffrey J., Budhu, Richard J., Mills, Sander G., MacCoss, Malcolm, Malkowitz, Lorraine, Siciliano, Salvatore, Gould, Sandra L., DeMartino, Julie A., Springer, Martin S.

“…A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains by Lynch, Christopher L., Willoughby, Christopher A., Hale, Jeffrey J., Holson, Edward J., Budhu, Richard J., Gentry, Amy L., Rosauer, Keith G., Caldwell, Charles G., Chen, Ping, Mills, Sander G., MacCoss, Malcolm, Berk, Scott, Chen, Liya, Chapman, Kevin T., Malkowitz, Lorraine, Springer, Martin S., Gould, Sandra L., DeMartino, Julie A., Siciliano, Salvatore J., Cascieri, Margaret A., Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A., Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio A.

“…The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent Anti-HIV activity by Hale, Jeffrey J., Budhu, Richard J., Holson, Edward B., Finke, Paul E., Oates, Bryan, Mills, Sander G., MacCoss, Malcolm, Gould, Sandra L., DeMartino, Julie A., Springer, Martin S., Siciliano, Salvatore, Malkowitz, Lorraine, Schleif, William A., Hazuda, Daria, Miller, Michael, Kessler, Joseph, Danzeisen, Renee, Holmes, Karen, Lineberger, Janet, Carella, Anthony, Carver, Gwen, Emini, Emilio

“…Investigations of the structure–activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV by LYNCH, Christopher L, HALE, Jeffrey J, DEMARTINO, Julie A, SICILIANO, Salvatore J, CASCIERI, Margaret A, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, SCHLEIF, William A, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, BUDHU, Richard J, LINEBERGER, Janet, MILLER, Michael, EMINI, Emilio A, GENTRY, Amy L, MILLS, Sander G, CHAPMAN, Kevin T, MACCOSS, Malcolm, MALKOWITZ, Lorraine, SPRINGER, Martin S, GOULD, Sandra L

“…A series of alpha-(pyrrolidin-1-yl)acetic acids is presented as selective and potent antivirals against HIV. Several of the pyrrolidine zwitterions…”
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1,3,4 trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains by Willoughby, Christopher A, Rosauer, Keith G, Hale, Jeffery J, Budhu, Richard J, Mills, Sander G, Chapman, Kevin T, MacCoss, Malcolm, Malkowitz, Lorraine, Springer, Martin S, Gould, Sandra L, DeMartino, Julie A, Siciliano, Salvatore J, Cascieri, Margaret A, Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A, Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio A

“…A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity by HALE, Jeffrey J, BUDHU, Richard J, HAZUDA, Daria, MILLER, Michael, KESSLER, Joseph, DANZEISEN, Renee, HOLMES, Karen, LINEBERGER, Janet, CARELLA, Anthony, CARVER, Gwen, EMINI, Emilio A, MILLS, Sander G, MACCOSS, Malcolm, GOULD, Sandra L, DEMARTINO, Julie A, SPRINGER, Martin S, SICILIANO, Salvatore J, MALKOWITZ, Lorraine, SCHLEIF, William A

“…Incorporation of acidic functional groups into a lead CCR5 antagonist identified from a targeted combinatorial library resulted in compounds with enhanced…”
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CCR5 Antagonists:  3-(Pyrrolidin-1-yl)propionic Acid Analogues with Potent Anti-HIV Activity by Lynch, Christopher L, Hale, Jeffrey J, Budhu, Richard J, Gentry, Amy L, Finke, Paul E, Caldwell, Charles G, Mills, Sander G, MacCoss, Malcolm, Shen, Dong-Ming, Chapman, Kevin T, Malkowitz, Lorraine, Springer, Martin S, Gould, Sandra L, DeMartino, Julie A, Siciliano, Salvatore J, Cascieri, Margaret A, Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A, Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio

“…A novel approach to α,α-disubstituted-β-amino acids (β2,2-amino acids) was employed in the synthesis of a series of 3-(pyrrolidin-1-yl)propionic acids…”
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1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists by Mills, Sander G., MacCoss, Malcolm, Underwood, Dennis, Shah, Shrenik K., Finke, Paul E., Miller, Daniel J., Budhu, Richard J., Cascieri, Margaret A., Sadowski, Sharon, Strader, Catherine D.

“…A stereocontrolled synthesis of 1-benzyloxy-2-phenylcyclohexane derivatives containing polar substituents at C3 is described. These compounds, designed to test…”
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