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Items: 33

1.

Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.

Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29.

PMID:
26195137
2.

Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1.

Barrow JC, Rittle KE, Ngo PL, Selnick HG, Graham SL, Pitzenberger SM, McGaughey GB, Colussi D, Lai MT, Huang Q, Tugusheva K, Espeseth AS, Simon AJ, Munshi SK, Vacca JP.

ChemMedChem. 2007 Jul;2(7):995-9. No abstract available.

PMID:
17458843
3.

Mechanism of the solution oxidation of rofecoxib under alkaline conditions.

Harmon PA, Biffar S, Pitzenberger SM, Reed RA.

Pharm Res. 2005 Oct;22(10):1716-26. Epub 2005 Sep 22.

PMID:
16180130
4.

Identification and quantitation of extractables from cellulose acetate butyrate (CAB) and estimation of their in vivo exposure levels.

Ma D, Wasylaschuk WR, Beasley C, Zhao ZZ, Harmon PA, Ballard JM, Pitzenberger SM, Varga SL, Reed RA.

J Pharm Biomed Anal. 2004 Jun 29;35(4):779-88.

PMID:
15193722
5.

Bioactivation of the 3-amino-6-chloropyrazinone ring in a thrombin inhibitor leads to novel dihydro-imidazole and imidazolidine derivatives: structures and mechanism using 13C-labels, mass spectrometry, and NMR.

Subramanian R, Lin CC, Ho JZ, Pitzenberger SM, Silva-Elipe MV, Gibson CR, Braun MP, Yu X, Yergey JL, Singh R.

Drug Metab Dispos. 2003 Nov;31(11):1437-47.

PMID:
14570777
6.

Conformation of a novel tetrapeptide inhibitor NH2-D-Trp-D-Met-Phe(pCl)-Gla-NH2 bound to farnesyl-protein transferase.

Bogusky MJ, Culberson JC, Pitzenberger SM, Garsky VM, Wallace A, Pessi A, Koblan KS.

J Pept Res. 1999 Jul;54(1):66-73.

PMID:
10448971
7.

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.

Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ, et al.

J Med Chem. 1999 Jun 17;42(12):2180-90.

PMID:
10377223
8.

Antibacterial activity of lonchocarpol A.

Salvatore MJ, King AB, Graham AC, Onishi HR, Bartizal KF, Abruzzo GK, Gill CJ, Ramjit HG, Pitzenberger SM, Witherup KM.

J Nat Prod. 1998 May;61(5):640-2.

PMID:
9599265
9.

High fatty acid content in rabbit serum is responsible for the differentiation of osteoblasts into adipocyte-like cells.

Diascro DD Jr, Vogel RL, Johnson TE, Witherup KM, Pitzenberger SM, Rutledge SJ, Prescott DJ, Rodan GA, Schmidt A.

J Bone Miner Res. 1998 Jan;13(1):96-106.

10.

Characterization of a solid state reaction product from a lyophilized formulation of a cyclic heptapeptide. A novel example of an excipient-induced oxidation.

Dubost DC, Kaufman MJ, Zimmerman JA, Bogusky MJ, Coddington AB, Pitzenberger SM.

Pharm Res. 1996 Dec;13(12):1811-4.

PMID:
8987076
11.

Identification of fatty acid methyl ester as naturally occurring transcriptional regulators of the members of the peroxisome proliferator-activated receptor family.

Schmidt A, Vogel RL, Witherup KM, Rutledge SJ, Pitzenberger SM, Adam M, Rodan GA.

Lipids. 1996 Nov;31(11):1115-24.

PMID:
8934443
12.

Species differences in the metabolism of a potent HIV-1 reverse transcriptase inhibitor L-738,372. In vivo and in vitro studies in rats, dogs, monkeys, and human.

Prueksaritanont T, Balani SK, Dwyer LM, Ellis JD, Kauffman LR, Varga SL, Pitzenberger SM, Theoharides AD.

Drug Metab Dispos. 1995 Jul;23(7):688-95.

PMID:
7587955
13.

Solution structure of the cytoplasmic domain of phopholamban: phosphorylation leads to a local perturbation in secondary structure.

Mortishire-Smith RJ, Pitzenberger SM, Burke CJ, Middaugh CR, Garsky VM, Johnson RG.

Biochemistry. 1995 Jun 13;34(23):7603-13.

PMID:
7779806
14.

NMR studies of novel inhibitors bound to farnesyl-protein transferase.

Koblan KS, Culberson JC, Desolms SJ, Giuliani EA, Mosser SD, Omer CA, Pitzenberger SM, Bogusky MJ.

Protein Sci. 1995 Apr;4(4):681-8.

15.

Metabolism of L-689,502 by rat liver slices to potent HIV-1 protease inhibitors.

Balani SK, Pitzenberger SM, Schwartz MS, Ramjit HG, Thompson WJ.

Drug Metab Dispos. 1995 Feb;23(2):185-9.

PMID:
7736909
16.

Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites.

Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD.

Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8.

PMID:
7895608
17.

Transglutaminase inhibition by 2-[(2-oxopropyl)thio]imidazolium derivatives: mechanism of factor XIIIa inactivation.

Freund KF, Doshi KP, Gaul SL, Claremon DA, Remy DC, Baldwin JJ, Pitzenberger SM, Stern AM.

Biochemistry. 1994 Aug 23;33(33):10109-19.

PMID:
7914744
18.

Three-dimensional structure of echistatin and dynamics of the active site.

Chen Y, Suri AK, Kominos D, Sanyal G, Naylor AM, Pitzenberger SM, Garsky VM, Levy RM, Baum J.

J Biomol NMR. 1994 May;4(3):307-24.

PMID:
8019139
19.

The solution conformation of Ac-Pen-Arg-Gly-Asp-Cys-OH, a potent fibrinogen receptor antagonist.

Bogusky MJ, Naylor AM, Mertzman ME, Pitzenberger SM, Nutt RF, Brady SF, Colton CD, Veber DF.

Biopolymers. 1993 Aug;33(8):1287-97.

PMID:
8364159
20.

Biotransformation of 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005) in rhesus monkeys and rat liver microsomes to a potent HIV-1 reverse transcriptase inhibitor.

Balani SK, Goldman ME, Kauffman LR, Varga SL, O'Brien JA, Smith SJ, Olah TV, Ramjit HG, Schorn TW, Pitzenberger SM, et al.

Drug Metab Dispos. 1993 Jul-Aug;21(4):598-604.

PMID:
7690697
21.

Structure of synthetic peptide analogues of an eggshell protein of Schistosoma mansoni.

Middaugh CR, Thomson JA, Burke CJ, Mach H, Naylor AM, Bogusky MJ, Ryan JA, Pitzenberger SM, Ji H, Cordingley JS.

Protein Sci. 1993 Jun;2(6):900-14.

22.

In vivo and in vitro metabolism studies on a class III antiarrhythmic agent.

Vickers S, Duncan CA, Kari PH, Homnick CF, Elliott JM, Pitzenberger SM, Hichens M, Vyas KP.

Drug Metab Dispos. 1993 May-Jun;21(3):467-73.

PMID:
8100503
23.

Metabolism of a new HIV-1 reverse transcriptase inhibitor, 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (L-696,229), in rat and liver slices.

Balani SK, Pitzenberger SM, Kauffman LR, Arison BH, Ramjit HG, Goldman ME, O'Brien JA, King JD, Hoffman JM, Rooney CS, et al.

Drug Metab Dispos. 1992 Nov-Dec;20(6):869-76.

PMID:
1283569
24.

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.

Hartman GD, Halczenko W, Duggan ME, Imagire JS, Smith RL, Pitzenberger SM, Fitzpatrick SL, Alberts AW, Bostedor R, Chao YS, et al.

J Med Chem. 1992 Oct 16;35(21):3813-21.

PMID:
1433193
25.

Physiological disposition and metabolism of L-365,260, a potent antagonist of brain cholecystokinin receptor, in laboratory animals.

Chen IW, Dorley JM, Ramjit HG, Pitzenberger SM, Lin JH.

Drug Metab Dispos. 1992 May-Jun;20(3):390-5.

PMID:
1355713
26.

NMR and molecular modeling characterization of RGD containing peptides.

Bogusky MJ, Naylor AM, Pitzenberger SM, Nutt RF, Brady SF, Colton CD, Sisko JT, Anderson PS, Veber DF.

Int J Pept Protein Res. 1992 Jan;39(1):63-76.

PMID:
1634331
27.

Proton NMR assignments and secondary structure of the snake venom protein echistatin.

Chen Y, Pitzenberger SM, Garsky VM, Lumma PK, Sanyal G, Baum J.

Biochemistry. 1991 Dec 17;30(50):11625-36.

PMID:
1661142
28.

Metabolism of antiparkinson agent dopazinol by rat liver microsomes.

Vyas KP, Kari PH, Ramjit HG, Pitzenberger SM, Hichens M.

Drug Metab Dispos. 1990 Nov-Dec;18(6):1025-30.

PMID:
1981508
29.

In vitro and in vivo biotransformation of simvastatin, an inhibitor of HMG CoA reductase.

Vickers S, Duncan CA, Vyas KP, Kari PH, Arison B, Prakash SR, Ramjit HG, Pitzenberger SM, Stokker G, Duggan DE.

Drug Metab Dispos. 1990 Jul-Aug;18(4):476-83.

PMID:
1976071
30.

Biotransformation of lovastatin. I. Structure elucidation of in vitro and in vivo metabolites in the rat and mouse.

Vyas KP, Kari PH, Pitzenberger SM, Halpin RA, Ramjit HG, Arison B, Murphy JS, Hoffman WF, Schwartz MS, Ulm EH, et al.

Drug Metab Dispos. 1990 Mar-Apr;18(2):203-11.

PMID:
1971574
31.

Regioselectivity and stereoselectivity in the metabolism of HMG-CoA reductase inhibitors.

Vyas KP, Kari PH, Pitzenberger SM.

Biochem Biophys Res Commun. 1990 Feb 14;166(3):1155-62.

PMID:
2306236
32.

Chemical synthesis of echistatin, a potent inhibitor of platelet aggregation from Echis carinatus: synthesis and biological activity of selected analogs.

Garsky VM, Lumma PK, Freidinger RM, Pitzenberger SM, Randall WC, Veber DF, Gould RJ, Friedman PA.

Proc Natl Acad Sci U S A. 1989 Jun;86(11):4022-6.

33.

Disposition and metabolism of sodium 4-[(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl]-gamma -oxobenzenebutanoate in rats and dogs.

Tocco DJ, deLuna FA, Duncan AE, Ramjit HG, Pitzenberger SM, Hsieh JY.

Drug Metab Dispos. 1988 Sep-Oct;16(5):690-6.

PMID:
2906591

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