Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 56

1.

Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].

Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014. doi: 10.1016/j.bmcl.2018.07.022. Epub 2018 Jul 31. No abstract available.

PMID:
30076050
2.

Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.

Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW.

J Med Chem. 2018 Apr 26;61(8):3491-3502. doi: 10.1021/acs.jmedchem.7b01716. Epub 2018 Apr 10.

PMID:
29617572
3.

The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity.

Cardarelli RA, Jones K, Pisella LI, Wobst HJ, McWilliams LJ, Sharpe PM, Burnham MP, Baker DJ, Chudotvorova I, Guyot J, Silayeva L, Morrow DH, Dekker N, Zicha S, Davies PA, Holenz J, Duggan ME, Dunlop J, Mather RJ, Wang Q, Medina I, Brandon NJ, Deeb TZ, Moss SJ.

Nat Med. 2017 Dec 7;23(12):1394-1396. doi: 10.1038/nm.4442. No abstract available.

PMID:
29216042
4.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5179-5184. doi: 10.1016/j.bmcl.2017.10.053. Epub 2017 Oct 24. Erratum in: Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014.

5.

Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154.

Gould RW, Grannan MD, Gunter BW, Ball J, Bubser M, Bridges TM, Wess J, Wood MW, Brandon NJ, Duggan ME, Niswender CM, Lindsley CW, Conn PJ, Jones CK.

Neuropharmacology. 2018 Jan;128:492-502. doi: 10.1016/j.neuropharm.2017.07.013. Epub 2017 Jul 17.

PMID:
28729220
6.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995. doi: 10.1016/j.bmcl.2017.05.014. Epub 2017 May 6.

7.

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.

Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Wu D, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2296-2301. doi: 10.1016/j.bmcl.2017.04.043. Epub 2017 Apr 13.

8.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Wood MR, Noetzel MJ, Melancon BJ, Poslusney MS, Nance KD, Hurtado MA, Luscombe VB, Weiner RL, Rodriguez AL, Lamsal A, Chang S, Bubser M, Blobaum AL, Engers DW, Niswender CM, Jones CK, Brandon NJ, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

ACS Med Chem Lett. 2016 Dec 16;8(2):233-238. doi: 10.1021/acsmedchemlett.6b00461. eCollection 2017 Feb 9.

9.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jan 15;27(2):171-175. doi: 10.1016/j.bmcl.2016.11.086. Epub 2016 Nov 30.

10.

Identification of a Chrysanthemic Ester as an Apolipoprotein E Inducer in Astrocytes.

Fan J, Zareyan S, Zhao W, Shimizu Y, Pfeifer TA, Tak JH, Isman MB, Van den Hoven B, Duggan ME, Wood MW, Wellington CL, Kulic I.

PLoS One. 2016 Sep 6;11(9):e0162384. doi: 10.1371/journal.pone.0162384. eCollection 2016.

11.

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

Wood MR, Noetzel MJ, Tarr JC, Rodriguez AL, Lamsal A, Chang S, Foster JJ, Smith E, Chase P, Hodder PS, Engers DW, Niswender CM, Brandon NJ, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4282-6. doi: 10.1016/j.bmcl.2016.07.042. Epub 2016 Jul 21.

12.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3029-3033. doi: 10.1016/j.bmcl.2016.05.010. Epub 2016 May 5.

13.

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects.

Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, Lindsley CW, Conn PJ, Jones CK.

Neuropharmacology. 2016 Mar;102:244-53. doi: 10.1016/j.neuropharm.2015.11.016. Epub 2015 Nov 23.

14.

Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.

Sivakumaran S, Cardarelli RA, Maguire J, Kelley MR, Silayeva L, Morrow DH, Mukherjee J, Moore YE, Mather RJ, Duggan ME, Brandon NJ, Dunlop J, Zicha S, Moss SJ, Deeb TZ.

J Neurosci. 2015 May 27;35(21):8291-6. doi: 10.1523/JNEUROSCI.5205-14.2015.

15.

Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.

Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK.

ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19.

16.

Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.

Schmidt A, Kimmel DB, Bai C, Scafonas A, Rutledge S, Vogel RL, McElwee-Witmer S, Chen F, Nantermet PV, Kasparcova V, Leu CT, Zhang HZ, Duggan ME, Gentile MA, Hodor P, Pennypacker B, Masarachia P, Opas EE, Adamski SA, Cusick TE, Wang J, Mitchell HJ, Kim Y, Prueksaritanont T, Perkins JJ, Meissner RS, Hartman GD, Freedman LP, Harada S, Ray WJ.

J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31.

17.

Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.

Schmidt A, Harada S, Kimmel DB, Bai C, Chen F, Rutledge SJ, Vogel RL, Scafonas A, Gentile MA, Nantermet PV, McElwee-Witmer S, Pennypacker B, Masarachia P, Sahoo SP, Kim Y, Meissner RS, Hartman GD, Duggan ME, Rodan GA, Towler DA, Ray WJ.

J Biol Chem. 2009 Dec 25;284(52):36367-76. doi: 10.1074/jbc.M109.049734. Epub 2009 Oct 21.

18.

Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Mitchell HJ, Dankulich WP, Hartman GD, Prueksaritanont T, Schmidt A, Vogel RL, Bai C, McElwee-Witmer S, Zhang HZ, Chen F, Leu CT, Kimmel DB, Ray WJ, Nantermet P, Gentile MA, Duggan ME, Meissner RS.

J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r.

PMID:
19606870
19.

Covalent modifiers: an orthogonal approach to drug design.

Potashman MH, Duggan ME.

J Med Chem. 2009 Mar 12;52(5):1231-46. doi: 10.1021/jm8008597. Review. No abstract available.

PMID:
19203292
20.

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.

Zhao Z, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huber HE, Duggan ME, Lindsley CW.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):49-53. Epub 2007 Nov 13.

PMID:
18054229
21.

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. Epub 2006 Dec 3.

PMID:
17210250
22.

Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides.

Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Tsou NN, Duggan ME, Conn PJ, Hartman GD.

ChemMedChem. 2006 Aug;1(8):807-11. No abstract available.

PMID:
16902933
23.

Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.

Zartman AE, Duong LT, Fernandez-Metzler C, Hartman GD, Leu CT, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME, Meissner RS.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1647-50.

PMID:
15745815
24.

Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.

DeFeo-Jones D, Barnett SF, Fu S, Hancock PJ, Haskell KM, Leander KR, McAvoy E, Robinson RG, Duggan ME, Lindsley CW, Zhao Z, Huber HE, Jones RE.

Mol Cancer Ther. 2005 Feb;4(2):271-9.

25.

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.

Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME, Lindsley CW.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):905-9.

PMID:
15686884
26.

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.

Lindsley CW, Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.

PMID:
15664853
27.

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. Epub 2004 Dec 17.

PMID:
15608073
28.

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR.

J Med Chem. 2004 Nov 18;47(24):5825-8.

PMID:
15537338
29.

Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.

Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA, Duong LT, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD, Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont T, Rodan GA, Wesolowski GA, Rodan SB, Duggan ME.

J Med Chem. 2004 Sep 23;47(20):4829-37.

PMID:
15369386
30.

Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.

Breslin MJ, Duggan ME, Halczenko W, Hartman GD, Duong LT, Fernandez-Metzler C, Gentile MA, Kimmel DB, Leu CT, Merkle K, Prueksaritanont T, Rodan GA, Rodan SB, Hutchinson JH.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4515-8.

PMID:
15357983
31.

Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.

Whitman DB, Askew BC, Duong LT, Fernandez-Metzler C, Halczenko W, Hartman GD, Hutchinson JH, Leu CT, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4411-5.

PMID:
15357963
32.

Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.

Wang J, Breslin MJ, Coleman PJ, Duggan ME, Hunt CA, Hutchinson JH, Leu CT, Rodan SB, Rodan GA, Duong LT, Hartman GD.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1049-52.

PMID:
15013021
33.

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.

O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2004 May;309(2):568-77. Epub 2004 Jan 27.

PMID:
14747613
34.

Disposition of a novel and potent alpha(v)beta3 antagonist in animals, and extrapolation to man.

Prueksaritanont T, Fernandez-Metzler C, Meng Y, Barrish A, Halczenko W, Rodan SB, Hutchinson JH, Duggan ME, Lin JH.

Xenobiotica. 2004 Jan;34(1):103-15.

PMID:
14742139
35.

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes.

Williams DL Jr, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ.

Ann N Y Acad Sci. 2003 Nov;1003:481-4. No abstract available.

PMID:
14684495
36.

Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.

Perkins JJ, Duong LT, Fernandez-Metzler C, Hartman GD, Kimmel DB, Leu CT, Lynch JJ, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME, Meissner RS.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4285-8.

PMID:
14643310
37.

Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.

Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD, Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA, Zartman AE, Rodan SB, Duggan ME.

J Med Chem. 2003 Oct 23;46(22):4790-8.

PMID:
14561098
38.

Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.

Breslin MJ, Duggan ME, Halczenko W, Fernandez-Metzler C, Hunt CA, Leu CT, Merkle KM, Naylor-Olsen AM, Prueksaritanont T, Stump G, Wallace A, Rodan SB, Hutchinson JH.

Bioorg Med Chem Lett. 2003 May 19;13(10):1809-12.

PMID:
12729670
39.

Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.

Feuston BP, Culberson JC, Duggan ME, Hartman GD, Leu CT, Rodan SB.

J Med Chem. 2002 Dec 19;45(26):5640-8.

PMID:
12477347
40.

Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.

Brashear KM, Hunt CA, Kucer BT, Duggan ME, Hartman GD, Rodan GA, Rodan SB, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Barrish A, Homnick CF, Hutchinson JH, Coleman PJ.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3483-6.

PMID:
12419389
41.

Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.

Coleman PJ, Askew BC, Hutchinson JH, Whitman DB, Perkins JJ, Hartman GD, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Merkle KM, Lynch R, Lynch JJ, Rodan SB, Duggan ME.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2463-5.

PMID:
12161158
42.

Differences in the absorption, metabolism and biliary excretion of a diastereomeric pair of alphavbeta3-antagonists in rat: limited role of P-glycoprotein.

Prueksaritanont T, Meng Y, Ma B, Leppert P, Hochman J, Tang C, Perkins J, Zrada M, Meissner R, Duggan ME, Lin JH.

Xenobiotica. 2002 Mar;32(3):207-20.

PMID:
11958560
43.

Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.

Coleman PJ, Brashear KM, Hunt CA, Hoffman WF, Hutchinson JH, Breslin MJ, McVean CA, Askew BC, Hartman GD, Rodan SB, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Ma B, Libby LA, Merkle KM, Stump GL, Wallace AA, Lynch JJ, Lynch R, Duggan ME.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):31-4.

PMID:
11738567
44.

Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.

Meissner RS, Perkins JJ, Duong LT, Hartman GD, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Naylor-Olsen A, Rodan GA, Rodan SB, Whitman DB, Wesolowski GA, Duggan ME.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):25-9.

PMID:
11738566
45.

alpha(v)beta(3) Integrin antagonists as inhibitors of bone resorption.

Hartman GD, Duggan ME.

Expert Opin Investig Drugs. 2000 Jun;9(6):1281-91. Review.

PMID:
11060743
46.

Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.

Duggan ME, Duong LT, Fisher JE, Hamill TG, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Perkins JJ, Rodan SB, Wesolowski G, Whitman DB, Zartman AE, Rodan GA, Hartman GD.

J Med Chem. 2000 Oct 5;43(20):3736-45.

PMID:
11020288
47.

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.

PMID:
10987423
48.

Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.

Hartman GD, Duggan ME, Hoffman WF, Meissner RJ, Perkins JJ, Zartman AE, Naylor-Olsen AM, Cook JJ, Glass JD, Lynch RJ, Zhang G, Gould RJ.

Bioorg Med Chem Lett. 1999 Mar 22;9(6):863-8.

PMID:
10206551
49.

Species and organ differences in first-pass metabolism of the ester prodrug L-751,164 in dogs and monkeys. In vivo and in vitro studies.

Prueksaritanont T, Gorham LM, Ellis JD, Fernandez-Metzler C, Deluna P, Gehret JR, Strong KL, Hochman JH, Askew BC, Duggan ME, Gilbert JD, Lin JH, Vyas KP.

Drug Metab Dispos. 1996 Nov;24(11):1263-71.

PMID:
8937862
50.

Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217.

Cook JJ, Holahan MA, Lyle EA, Ramjit DR, Sitko GR, Stranieri MT, Stupienski RF 3rd, Wallace AA, Hand EL, Gehret JR, Kothstein T, Drag MD, McCormick GY, Perkins JJ, Ihle NC, Duggan ME, Hartman GD, Gould RJ, Lynch JJ Jr.

J Pharmacol Exp Ther. 1996 Jul;278(1):62-73.

PMID:
8764336

Supplemental Content

Loading ...
Support Center