Search Results - "MICHELSON, S. R"

Time- and dose-dependent pharmacokinetics of L-754,394, an HIV protease inhibitor, in rats, dogs and monkeys by Lin, J H, Chiba, M, Chen, I W, Vastag, K J, Nishime, J A, Dorsey, B D, Michelson, S R, McDaniel, S L

“…L-754,394 is a potent and specific inhibitor of the HIV-1 encoded protease that is essential for the maturation of the infectious virus. The drug exhibited…”
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Affinity purification of the HIV-1 protease by Heimbach, J C, Garsky, V M, Michelson, S R, Dixon, R A, Sigal, I S, Darke, P L

“…An inhibitor of the HIV-1 protease has been employed in the generation of a resin which allows the rapid purification of this enzyme. A peptide substrate…”
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Identification of MK-944a:  A Second Clinical Candidate from the Hydroxylaminepentanamide Isostere Series of HIV Protease Inhibitors by Dorsey, Bruce D, McDonough, Colleen, McDaniel, Stacey L, Levin, Rhonda B, Newton, Christina L, Hoffman, Jacob M, Darke, Paul L, Zugay-Murphy, Joan A, Emini, Emilio A, Schleif, William A, Olsen, David B, Stahlhut, Mark W, Rutkowski, Carrie A, Kuo, Lawrence C, Lin, Jiunn H, Chen, I-W, Michelson, Stuart R, Holloway, M. Katharine, Huff, Joel R, Vacca, Joseph P

“…Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome…”
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4-Substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors by Hartman, George D, Halczenko, Wasyl, Smith, Robert L, Sugrue, Michael F, Mallorga, Pierre J, Michelson, Stuart R, Randall, William C, Schwam, Harvey, Sondey, John M

“…A series of 4-substituted thiophene- and furan-2-sulfonamides was prepared and was found to possess nanomolar-level potency for inhibition of human carbonic…”
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Inhibitors of glycolic acid oxidase. 4-Substituted 3-hydroxy-1H-pyrrole-2,5-dione derivatives by Rooney, C. S, Randall, W. C, Streeter, K. B, Ziegler, C, Cragoe, E. J, Schwam, H, Michelson, S. R, Williams, H. W. R, Eichler, E

“…An extensive series of novel 4-substituted 3-hydroxy-1H-pyrrole-2,5-dione derivatives has been prepared and studied as inhibitors of glycolic acid oxidase…”
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Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency by Williams, Peter D., Bock, Mark G., Evans, Ben E., Freidinger, Roger M., Gallicchio, Steven N., Guidotti, Maribeth T., Jacobson, Marlene A., Kuo, Michelle S., Levy, Michelle R., Lis, Edward V., Michelson, Stuart R., Pawluczyk, Joseph M., Perlow, Debra S., Pettibone, Douglas J., Quigley, Amy G., Reiss, Duane R., Salvatore, Christopher, Stauffer, Kenneth J., Woyden, Carla J.

“…Structure-activity studies on the oxytocin antagonist 1 (L-371,257; K i = 9.3 nM) have led to the identification of a related series of compounds containing an…”
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(Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes by Alexander, J, Cargill, R, Michelson, S R, Schwam, H

“…(Acyloxy)alkyl carbamates of the type R1R2N-CO-O-CHR3-OCO-R4 are described as novel bioreversible prodrugs for primary and secondary amines. These were…”
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Inhibitors of glycolic acid oxidase. 4-Substituted-2,4-dioxobutanoic acid derivatives by Williams, H. W. R., Eichler, E., Randall, W. C., Rooney, C. S., Cragoe, E. J., Streeter, K. B., Schwam, H., Michelson, S. R., Patchett, A. A., Taub, D.

“…Fourteen new 4-substituted 2,4-dioxobutanoic acids have been synthesized. These compounds, all of which contain lipophilic 4-substituents, are potent…”
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3-Substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors by Hunt, Cecilia A, Mallorga, Pierre J, Michelson, Stuart R, Schwam, Harvey, Sondey, John M, Smith, Robert L, Sugrue, Michael F, Shepard, Kenneth L

“…3-Aminoalkyl derivatives of thieno[2,3-b][1,4]thiazine-6-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. The compounds…”
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Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors by Hartman, George D, Halczenko, Wasyl, Prugh, John D, Smith, Robert L, Sugrue, Michael F, Mallorga, Pierre, Michelson, Stuart R, Randall, William C, Schwam, Harvey, Sondey, John M

“…Novel 5-[(alkylamino)methyl]thieno[2,3-b]furan-2-sulfonamides were prepared and evaluated in vitro for inhibition of human carbonic anhydrase II (CA II) and ex…”
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Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides by Graham, Samuel L, Hoffman, Jacob M, Gautheron, Pierre, Michelson, Stuart R, Scholz, Thomas H, Schwam, Harvey, Shepard, Kenneth L, Smith, Anthony M, Smith, Robert L

“…Derivatives of benzofuran- and indole-2-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. These compounds were found to…”
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Development of Orally Active Oxytocin Antagonists:  Studies on 1-(1-{4-[1-(2-Methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and Related Pyridines by Bell, Ian M, Erb, Jill M, Freidinger, Roger M, Gallicchio, Steven N, Guare, James P, Guidotti, Maribeth T, Halpin, Rita A, Hobbs, Doug W, Homnick, Carl F, Kuo, Michelle S, Lis, Edward V, Mathre, David J, Michelson, Stuart R, Pawluczyk, Joseph M, Pettibone, Douglas J, Reiss, Duane R, Vickers, Stanley, Williams, Peter D, Woyden, Carla J

“…The previously reported oxytocin antagonist L-371,257 (2) has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups…”
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New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides by Prugh, John D, Hartman, George D, Mallorga, Pierre J, McKeever, Brian M, Michelson, Stuart R, Murcko, Mark A, Schwam, Harvey, Smith, Robert L, Sondey, John M

“…A series of 5-substituted thieno[2,3-b]- and thieno[3,2-b)- and thieno[3,2-b)thiophene-2-sulfonamides was prepared and evaluated for topical ocular hypotensive…”
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Development of orally active oxytocin antagonists : Studies on 1-(1-{4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2-methoxybenzo yl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines by BELL, I. M, ERB, J. M, LIS, E. V, MATHRE, D. J, MICHELSON, S. R, PAWLUCZYK, J. M, PETTIBONE, D. J, REISS, D. R, VICKERS, S, WILLIAMS, P. D, WOYDEN, C. J, FREIDINGER, R. M, GALLICCHIO, S. N, GUARE, J. P, GUIDOTTI, M. T, HALPIN, R. A, HOBBS, D. W, HOMNICK, C. F, KUO, M. S

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Topically active carbonic anhydrase inhibitors. 1. O-Acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide by Woltersdorf, O. W., Schwam, H., Bicking, J. B., Brown, S. L., DeSolms, S. J., Fishman, D. R., Graham, S. L., Gautheron, P. D., Hoffman, J. M.

“…A series of O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide (4, L-643,799) was prepared and the potential utility of each series member as a…”
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Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides by Shepard, Kenneth L, Graham, Samuel L, Hudcosky, Ronald J, Michelson, Stuart R, Scholz, Thomas H, Schwam, Harvey, Smith, Anthony M, Sondey, John M, Strohmaier, Kim M

“…For several decades a tantalizing goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase…”
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(Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes by Alexander, Jose, Cargill, Robyn, Michelson, Stuart R, Schwam, Harvey

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Topically active carbonic anhydrase inhibitors. IV: [(hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides by SHEPARD, K. L, GRAHAM, S. L, SUGRUE, M. F, HUDCOSKY, R. J, MICHELSON, S. R, SCHOLZ, T. H, SCHWAM, H, SMITH, A. M, SONDEY, J. M, STROHMAIER, K. M, SMITH, R. L

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New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors : 5-substituted thieno [2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]tiophene-2-sulfonamides by PRUGH, J. D, HARTMAN, G. D, SUGRUE, M. F, MALLORGA, P. J, MCKEEVER, B. M, MICHELSON, S. R, MURCKO, M. A, SCHWAM, H, SMITH, R. L, SONDEY, J. M, SPRINGER, J. P

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Topically active carbonic anhydrase inhibitors. III: Benzofuran- and indole-2-sulfonamides by GRAHAM, S. L, HOFFMAN, J. M, SUGRUE, M. F, GAUTHERON, P, MICHELSON, S. R, SCHOLZ, T. H, SCHWAM, H, SHEPARD, K. L, SMITH, A. M, SMITH, R. L, SONDEY, J. M

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