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Items: 17

1.

Orally efficacious NR2B-selective NMDA receptor antagonists.

Claiborne CF, McCauley JA, Libby BE, Curtis NR, Diggle HJ, Kulagowski JJ, Michelson SR, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):697-700.

PMID:
12639561
2.

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.

Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP Jr, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJ Jr, Michelson SR, Young SD.

J Med Chem. 2003 Feb 13;46(4):453-6.

PMID:
12570367
3.

Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.

Dorsey BD, McDonough C, McDaniel SL, Levin RB, Newton CL, Hoffman JM, Darke PL, Zugay-Murphy JA, Emini EA, Schleif WA, Olsen DB, Stahlhut MW, Rutkowski CA, Kuo LC, Lin JH, Chen IW, Michelson SR, Holloway MK, Huff JR, Vacca JP.

J Med Chem. 2000 Sep 7;43(18):3386-99.

PMID:
10978186
4.

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Salvatore C, Stauffer KJ, Woyden CJ.

Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6.

PMID:
10340620
5.

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.

Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP, Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS, Lis EV, Mathre DJ, Michelson SR, Pawluczyk JM, Pettibone DJ, Reiss DR, Vickers S, Williams PD, Woyden CJ.

J Med Chem. 1998 Jun 4;41(12):2146-63.

PMID:
9622556
6.

Time- and dose-dependent pharmacokinetics of L-754,394, an HIV protease inhibitor, in rats, dogs and monkeys.

Lin JH, Chiba M, Chen IW, Vastag KJ, Nishime JA, Dorsey BD, Michelson SR, McDaniel SL.

J Pharmacol Exp Ther. 1995 Jul;274(1):264-9.

PMID:
7616407
7.

3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors.

Hunt CA, Mallorga PJ, Michelson SR, Schwam H, Sondey JM, Smith RL, Sugrue MF, Shepard KL.

J Med Chem. 1994 Jan 21;37(2):240-7.

PMID:
8295211
8.

4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.

Hartman GD, Halczenko W, Smith RL, Sugŕue MF, Mallorga PJ, Michelson SR, Randall WC, Schwam H, Sondey JM.

J Med Chem. 1992 Oct 16;35(21):3822-31.

PMID:
1433194
9.

Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.

Hartman GD, Halczenko W, Prugh JD, Smith RL, Sugrue MF, Mallorga P, Michelson SR, Randall WC, Schwam H, Sondey JM.

J Med Chem. 1992 Aug 7;35(16):3027-33.

PMID:
1501230
10.

Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides.

Shepard KL, Graham SL, Hudcosky RJ, Michelson SR, Scholz TH, Schwam H, Smith AM, Sondey JM, Strohmaier KM, Smith RL, et al.

J Med Chem. 1991 Oct;34(10):3098-105.

PMID:
1920359
11.

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.

Prugh JD, Hartman GD, Mallorga PJ, McKeever BM, Michelson SR, Murcko MA, Schwam H, Smith RL, Sondey JM, Springer JP, et al.

J Med Chem. 1991 Jun;34(6):1805-18.

PMID:
2061922
12.

Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides.

Graham SL, Hoffman JM, Gautheron P, Michelson SR, Scholz TH, Schwam H, Shepard KL, Smith AM, Smith RL, Sondey JM, et al.

J Med Chem. 1990 Feb;33(2):749-54.

PMID:
2299640
13.

Affinity purification of the HIV-1 protease.

Heimbach JC, Garsky VM, Michelson SR, Dixon RA, Sigal IS, Darke PL.

Biochem Biophys Res Commun. 1989 Nov 15;164(3):955-60.

PMID:
2686642
14.

(Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes.

Alexander J, Cargill R, Michelson SR, Schwam H.

J Med Chem. 1988 Feb;31(2):318-22.

PMID:
2892933
15.

Inhibitors of glycolic acid oxidase. 4-substituted 2,4-dioxobutanoic acid derivatives.

Williams HW, Eichler E, Randall WC, Rooney CS, Cragoe EJ Jr, Streeter KB, Schwam H, Michelson SR, Patchett AA, Taub D.

J Med Chem. 1983 Aug;26(8):1196-200.

PMID:
6348285
16.

Inhibitors of glycolic acid oxidase. 4-Substituted 3-hydroxy-1H-pyrrole-2,5-dione derivatives.

Rooney CS, Randall WC, Streeter KB, Ziegler C, Cragoe EJ Jr, Schwam H, Michelson SR, Williams HW, Eichler E, Duggan DE, Ulm EH, Noll RM.

J Med Chem. 1983 May;26(5):700-14.

PMID:
6341589
17.

Quantitative structure-activity relationships involving the inhibition of glycolic acid oxidase by derivatives of glycolic and glyoxylic acids.

Randall WC, Streeter KB, Cresson EL, Schwam H, Michelson SR, Anderson PS, Cragoe EJ Jr, Williams HW, Eichler E, Rooney CS.

J Med Chem. 1979 Jun;22(6):608-14.

PMID:
458816

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