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Items: 1 to 50 of 57

1.

In vivo kinetics of Wolbachia depletion by ABBV-4083 in L. sigmodontis adult worms and microfilariae.

Hübner MP, Koschel M, Struever D, Nikolov V, Frohberger SJ, Ehrens A, Fendler M, Johannes I, von Geldern TW, Marsh K, Turner JD, Taylor MJ, Ward SA, Pfarr K, Kempf DJ, Hoerauf A.

PLoS Negl Trop Dis. 2019 Aug 5;13(8):e0007636. doi: 10.1371/journal.pntd.0007636. eCollection 2019 Aug.

2.

Preclinical development of an oral anti-Wolbachia macrolide drug for the treatment of lymphatic filariasis and onchocerciasis.

Taylor MJ, von Geldern TW, Ford L, Hübner MP, Marsh K, Johnston KL, Sjoberg HT, Specht S, Pionnier N, Tyrer HE, Clare RH, Cook DAN, Murphy E, Steven A, Archer J, Bloemker D, Lenz F, Koschel M, Ehrens A, Metuge HM, Chunda VC, Ndongmo Chounna PW, Njouendou AJ, Fombad FF, Carr R, Morton HE, Aljayyoussi G, Hoerauf A, Wanji S, Kempf DJ, Turner JD, Ward SA.

Sci Transl Med. 2019 Mar 13;11(483). pii: eaau2086. doi: 10.1126/scitranslmed.aau2086.

PMID:
30867321
3.

Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity.

von Geldern TW, Morton HE, Clark RF, Brown BS, Johnston KL, Ford L, Specht S, Carr RA, Stolarik DF, Ma J, Rieser MJ, Struever D, Frohberger SJ, Koschel M, Ehrens A, Turner JD, Hübner MP, Hoerauf A, Taylor MJ, Ward SA, Marsh K, Kempf DJ.

PLoS Negl Trop Dis. 2019 Feb 28;13(2):e0007159. doi: 10.1371/journal.pntd.0007159. eCollection 2019 Feb.

4.

Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.

Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA.

J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4.

5.

Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

Keenan M, Alexander PW, Chaplin JH, Abbott MJ, Diao H, Wang Z, Best WM, Perez CJ, Cornwall SM, Keatley SK, Thompson RC, Charman SA, White KL, Ryan E, Chen G, Ioset JR, von Geldern TW, Chatelain E.

Future Med Chem. 2013 Oct;5(15):1733-52. doi: 10.4155/fmc.13.139.

6.

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

Keenan M, Alexander PW, Diao H, Best WM, Khong A, Kerfoot M, Thompson RC, White KL, Shackleford DM, Ryan E, Gregg AD, Charman SA, von Geldern TW, Scandale I, Chatelain E.

Bioorg Med Chem. 2013 Apr 1;21(7):1756-63. doi: 10.1016/j.bmc.2013.01.050. Epub 2013 Jan 31.

PMID:
23462713
7.

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.

Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL.

J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27.

PMID:
22536986
8.

Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy of enzymes associated with bradykinin-mediated angioedema.

Fryer RM, Segreti J, Banfor PN, Widomski DL, Backes BJ, Lin CW, Ballaron SJ, Cox BF, Trevillyan JM, Reinhart GA, von Geldern TW.

Br J Pharmacol. 2008 Mar;153(5):947-55. Epub 2007 Dec 17.

9.

Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2007 Apr 19;50(8):1983-7. Epub 2007 Mar 17.

PMID:
17367123
10.

Liver-selective glucocorticoid receptor antagonism decreases glucose production and increases glucose disposal, ameliorating insulin resistance.

Zinker B, Mika A, Nguyen P, Wilcox D, Ohman L, von Geldern TW, Opgenorth T, Jacobson P.

Metabolism. 2007 Mar;56(3):380-7.

PMID:
17292727
11.

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.

PMID:
17276063
12.

Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.

Backes BJ, Hamilton GL, Nguyen P, Wilcox D, Fung S, Wang J, Grynfarb M, Goos-Nilsson A, Jacobson PB, von Geldern TW.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):40-4. Epub 2006 Oct 5.

PMID:
17070047
13.

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2006 Nov 2;49(22):6439-42.

PMID:
17064063
14.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM.

J Med Chem. 2006 Oct 19;49(21):6416-20.

PMID:
17034148
15.

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW.

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. Epub 2006 Sep 28.

PMID:
17010607
16.

Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.

Richards SJ, von Geldern TW, Jacobson P, Wilcox D, Nguyen P, Ohman L, Osterlund M, Gelius B, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Kalmanovich M.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. Epub 2006 Sep 20.

PMID:
16987661
17.

Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.

Longenecker KL, Stewart KD, Madar DJ, Jakob CG, Fry EH, Wilk S, Lin CW, Ballaron SJ, Stashko MA, Lubben TH, Yong H, Pireh D, Pei Z, Basha F, Wiedeman PE, von Geldern TW, Trevillyan JM, Stoll VS.

Biochemistry. 2006 Jun 20;45(24):7474-82.

PMID:
16768443
18.

Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3520-35. Erratum in: J Med Chem. 2006 Aug 24;49(17):5387.

PMID:
16759095
19.

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.

Lai C, Gum RJ, Daly M, Fry EH, Hutchins C, Abad-Zapatero C, von Geldern TW.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1807-10. Epub 2006 Jan 30.

PMID:
16446092
20.

Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode.

von Geldern TW, Lai C, Gum RJ, Daly M, Sun C, Fry EH, Abad-Zapatero C.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1811-5. Epub 2006 Jan 25.

PMID:
16442285
21.

Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.

Link JT, Sorensen B, Patel J, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Wilcox D, Zinker B, Nguyen P, Hickman B, Schmidt JM, Swanson S, Tian Z, Reisch TJ, Rotert G, Du J, Lane B, von Geldern TW, Jacobson PB.

J Med Chem. 2005 Aug 11;48(16):5295-304.

PMID:
16078847
22.

Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.

Jacobson PB, von Geldern TW, Ohman L, Osterland M, Wang J, Zinker B, Wilcox D, Nguyen PT, Mika A, Fung S, Fey T, Goos-Nilsson A, Grynfarb M, Barkhem T, Marsh K, Beno DW, Nga-Nguyen B, Kym PR, Link JT, Tu N, Edgerton DS, Cherrington A, Efendic S, Lane BC, Opgenorth TJ.

J Pharmacol Exp Ther. 2005 Jul;314(1):191-200. Epub 2005 Mar 22.

PMID:
15784656
23.

Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.

Wang GT, Wang S, Gentles R, Sowin T, Leitza S, Reilly EB, von Geldern TW.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):195-201.

PMID:
15582439
24.

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.

von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB.

J Med Chem. 2004 Aug 12;47(17):4213-30. Erratum in: J Med Chem. 2005 Apr 7;48(7):2724.

PMID:
15293993
25.

Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.

Akritopoulou-Zanze I, Patel JR, Hartandi K, Brenneman J, Winn M, Pratt JK, Grynfarb M, Goos-Nisson A, Von Geldern TW, Kym PR.

Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82.

PMID:
15080982
26.

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies.

Wessale JL, Adler AL, Novosad EI, Calzadilla SV, Dayton BD, Marsh KC, Winn M, Jae HS, von Geldern TW, Opgenorth TJ, Wu-Wong JR.

Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S.

PMID:
12193067
27.

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies.

Wu-Wong JR, Dixon DB, Chiou WJ, Sorensen BK, Liu G, Jae HS, Tasker A, von Geldern TW, Winn M, Opgenorth TJ.

Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S.

PMID:
12193066
28.

New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models.

Szczepankiewicz BG, Liu G, Jae HS, Tasker AS, Gunawardana IW, von Geldern TW, Gwaltney SL 2nd, Wu-Wong JR, Gehrke L, Chiou WJ, Credo RB, Alder JD, Nukkala MA, Zielinski NA, Jarvis K, Mollison KW, Frost DJ, Bauch JL, Hui YH, Claiborne AK, Li Q, Rosenberg SH.

J Med Chem. 2001 Dec 6;44(25):4416-30.

PMID:
11728187
29.

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.

Winn M, Reilly EB, Liu G, Huth JR, Jae HS, Freeman J, Pei Z, Xin Z, Lynch J, Kester J, von Geldern TW, Leitza S, DeVries P, Dickinson R, Mussatto D, Okasinski GF.

J Med Chem. 2001 Dec 6;44(25):4393-403.

PMID:
11728185
30.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.

Jae HS, Winn M, von Geldern TW, Sorensen BK, Chiou WJ, Nguyen B, Marsh KC, Opgenorth TJ.

J Med Chem. 2001 Nov 8;44(23):3978-84.

PMID:
11689084
31.

Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.

Pei Z, Xin Z, Liu G, Li Y, Reilly EB, Lubbers NL, Huth JR, Link JT, von Geldern TW, Cox BF, Leitza S, Gao Y, Marsh KC, DeVries P, Okasinski GF.

J Med Chem. 2001 Aug 30;44(18):2913-20.

PMID:
11520199
32.

Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.

Liu G, Huth JR, Olejniczak ET, Mendoza R, DeVries P, Leitza S, Reilly EB, Okasinski GF, Fesik SW, von Geldern TW.

J Med Chem. 2001 Apr 12;44(8):1202-10.

PMID:
11312920
33.

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.

Liu G, Link JT, Pei Z, Reilly EB, Leitza S, Nguyen B, Marsh KC, Okasinski GF, von Geldern TW, Ormes M, Fowler K, Gallatin M.

J Med Chem. 2000 Oct 19;43(21):4025-40.

PMID:
11052808
34.

Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.

Liu G, Kozmina NS, Winn M, von Geldern TW, Chiou WJ, Dixon DB, Nguyen B, Marsh KC, Opgenorth TJ.

J Med Chem. 1999 Sep 9;42(18):3679-89.

PMID:
10479299
35.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.

von Geldern TW, Tasker AS, Sorensen BK, Winn M, Szczepankiewicz BG, Dixon DB, Chiou WJ, Wang L, Wessale JL, Adler A, Marsh KC, Nguyen B, Opgenorth TJ.

J Med Chem. 1999 Sep 9;42(18):3668-78.

PMID:
10479298
36.

Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET(A) receptor selectivity.

Boyd SA, Mantei RA, Tasker AS, Liu G, Sorensen BK, Henry KJ Jr, von Geldern TW, Winn M, Wu-Wong JR, Chiou WJ, Dixon DB, Hutchins CW, Marsh KC, Nguyen B, Opgenorth TJ.

Bioorg Med Chem. 1999 Jun;7(6):991-1002.

PMID:
10428367
37.

Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor.

Wu-Wong JR, Dixon DB, Chiou WJ, Dayton BD, Novosad EI, Adler AL, Wessale JL, Calzadilla SV, Hernandez L, Marsh KC, Liu G, Szczepankiewicz B, von Geldern TW, Opgenorth TJ.

Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.

PMID:
10082200
38.

The effects of diminishing albumin binding to some Endothelin receptor antagonists.

Szczepankiewicz BG, Bal RB, von Geldern TW, Wu-Wong JR, Chiou WJ, Dixon DB, Opgenorth TJ, Hoffman DJ, Borre AJ, Marsh KC, Nguyen BN.

Life Sci. 1998;63(21):1905-12.

PMID:
9825768
39.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).

Liu G, Henry KJ Jr, Szczepankiewicz BG, Winn M, Kozmina NS, Boyd SA, Wasicak J, von Geldern TW, Wu-Wong JR, Chiou WJ, Dixon DB, Nguyen B, Marsh KC, Opgenorth TJ.

J Med Chem. 1998 Aug 13;41(17):3261-75.

PMID:
9703472
40.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.

Jae HS, Winn M, Dixon DB, Marsh KC, Nguyen B, Opgenorth TJ, von Geldern TW.

J Med Chem. 1997 Sep 26;40(20):3217-27.

PMID:
9379441
41.
42.

Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.

Tasker AS, Sorensen BK, Jae HS, Winn M, von Geldern TW, Dixon DB, Chiou WJ, Dayton BD, Calzadila S, Hernandez L, Marsh KC, WuWong JR, Opgenorth TJ.

J Med Chem. 1997 Jan 31;40(3):322-30.

PMID:
9022798
43.

An essential myosin light chain peptide induces supramaximal stimulation of cardiac myofibrillar ATPase activity.

Rarick HM, Opgenorth TJ, von Geldern TW, Wu-Wong JR, Solaro RJ.

J Biol Chem. 1996 Oct 25;271(43):27039-43.

44.

2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.

Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, Kester JA, Mantei RA, Bal R, Sorensen BK, Wu-Wong JR, Chiou WJ, Dixon DB, Novosad EI, Hernandez L, Marsh KC.

J Med Chem. 1996 Mar 1;39(5):1039-48.

PMID:
8676339
45.

Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.

von Geldern TW, Hoffman DJ, Kester JA, Nellans HN, Dayton BD, Calzadilla SV, Marsh KC, Hernandez L, Chiou W, Dixon DB, Wu-Wong JR, Opgenorth TJ.

J Med Chem. 1996 Feb 16;39(4):982-91.

PMID:
8632421
46.

Azole endothelin antagonists. 2. Structure-activity studies.

von Geldern TW, Kester JA, Bal R, Wu-Wong JR, Chiou W, Dixon DB, Opgenorth TJ.

J Med Chem. 1996 Feb 16;39(4):968-81.

PMID:
8632420
47.

Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.

von Geldern TW, Hutchins C, Kester JA, Wu-Wong JR, Chiou W, Dixon DB, Opgenorth TJ.

J Med Chem. 1996 Feb 16;39(4):957-67.

PMID:
8632419
48.

Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist.

Opgenorth TJ, Adler AL, Calzadilla SV, Chiou WJ, Dayton BD, Dixon DB, Gehrke LJ, Hernandez L, Magnuson SR, Marsh KC, Novosad EI, Von Geldern TW, Wessale JL, Winn M, Wu-Wong JR.

J Pharmacol Exp Ther. 1996 Feb;276(2):473-81.

PMID:
8632312
49.

Endothelins and endothelin receptor antagonists: binding to plasma proteins.

Wu-Wong JR, Chiou WJ, Hoffman DJ, Winn M, von Geldern TW, Opgenorth TJ.

Life Sci. 1996;58(21):1839-47.

PMID:
8637410
50.

Atrial natriuretic peptide and glomerular hyperfiltration during onset of spontaneous diabetes mellitus.

Okwueze MI, Opgenorth TJ, von Geldern TW, Vari RC.

Am J Physiol. 1994 Feb;266(2 Pt 2):R572-7.

PMID:
8141417

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