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Items: 41

1.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

2.

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K.

J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16.

PMID:
30256636
3.

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.

Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS.

Antimicrob Agents Chemother. 2018 Nov 26;62(12). pii: e00261-18. doi: 10.1128/AAC.00261-18. Print 2018 Dec.

4.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

5.

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K.

J Med Chem. 2018 Jul 12;61(13):5692-5703. doi: 10.1021/acs.jmedchem.8b00648. Epub 2018 Jun 27.

PMID:
29889526
6.

Expedient synthesis of tetrahydroquinoline-3-spirohydantoin derivatives via the Lewis acid-catalyzed tert-amino effect reaction.

Briones JF, Basarab GS.

Chem Commun (Camb). 2016 Jun 30;52(55):8541-4. doi: 10.1039/c6cc03600g.

PMID:
27314439
7.

Absorption, distribution, metabolism and elimination of 14C-ETX0914, a novel inhibitor of bacterial type-II topoisomerases in rodents.

Guo J, Joubran C, Luzietti RA Jr, Basarab GS, Grimm SW, Vishwanathan K.

Xenobiotica. 2017 Jan;47(1):31-49. doi: 10.3109/00498254.2016.1156186. Epub 2016 Apr 28.

PMID:
27122100
8.

Corrigendum: Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases.

Basarab GS, Kern GH, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, Alm RA, Barvian K, Doig P, Galullo V, Gardner H, Gowravaram M, Huband M, Kimzey A, Morningstar M, Kutschke A, Lahiri SD, Perros M, Singh R, Schuck VJ, Tommasi R, Walkup G, Newman JV.

Sci Rep. 2015 Sep 18;5:14157. doi: 10.1038/srep14157. No abstract available.

9.

Structural Insights Lead to a Negamycin Analogue with Improved Antimicrobial Activity against Gram-Negative Pathogens.

McKinney DC, Basarab GS, Cocozaki AI, Foulk MA, Miller MD, Ruvinsky AM, Scott CW, Thakur K, Zhao L, Buurman ET, Narayan S.

ACS Med Chem Lett. 2015 Jul 12;6(8):930-5. doi: 10.1021/acsmedchemlett.5b00205. eCollection 2015 Aug 13.

10.

Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases.

Basarab GS, Kern GH, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, Alm RA, Barvian K, Doig P, Galullo V, Gardner H, Gowravaram M, Huband M, Kimzey A, Morningstar M, Kutschke A, Lahiri SD, Perros M, Singh R, Schuck VJ, Tommasi R, Walkup G, Newman JV.

Sci Rep. 2015 Jul 14;5:11827. doi: 10.1038/srep11827. Erratum in: Sci Rep. 2015;5:14157.

11.

Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914).

Basarab GS, Doig P, Galullo V, Kern G, Kimzey A, Kutschke A, Newman JP, Morningstar M, Mueller J, Otterson L, Vishwanathan K, Zhou F, Gowravaram M.

J Med Chem. 2015 Aug 13;58(15):6264-82. doi: 10.1021/acs.jmedchem.5b00863. Epub 2015 Jul 24.

PMID:
26158756
12.

Inhibition of Neisseria gonorrhoeae Type II Topoisomerases by the Novel Spiropyrimidinetrione AZD0914.

Kern G, Palmer T, Ehmann DE, Shapiro AB, Andrews B, Basarab GS, Doig P, Fan J, Gao N, Mills SD, Mueller J, Sriram S, Thresher J, Walkup GK.

J Biol Chem. 2015 Aug 21;290(34):20984-94. doi: 10.1074/jbc.M115.663534. Epub 2015 Jul 6.

13.

Illicit Transport via Dipeptide Transporter Dpp is Irrelevant to the Efficacy of Negamycin in Mouse Thigh Models of Escherichia coli Infection.

McKinney DC, Bezdenejnih-Snyder N, Farrington K, Guo J, McLaughlin RE, Ruvinsky AM, Singh R, Basarab GS, Narayan S, Buurman ET.

ACS Infect Dis. 2015 May 8;1(5):222-30. doi: 10.1021/acsinfecdis.5b00027. Epub 2015 Apr 7.

PMID:
27622650
14.

Synthesis of a tetrahydronaphthyridine spiropyrimidinetrione DNA gyrase inhibiting antibacterial agent--differential substitution at all five carbon atoms of pyridine.

Basarab GS, Galullo V, DeGrace N, Hauck S, Joubran C, Wesolowski SS.

Org Lett. 2014 Dec 19;16(24):6456-9. doi: 10.1021/ol503256h. Epub 2014 Dec 2.

PMID:
25458849
15.

In vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potent activity against Gram-positive, fastidious Gram-Negative, and atypical bacteria.

Huband MD, Bradford PA, Otterson LG, Basarab GS, Kutschke AC, Giacobbe RA, Patey SA, Alm RA, Johnstone MR, Potter ME, Miller PF, Mueller JP.

Antimicrob Agents Chemother. 2015 Jan;59(1):467-74. doi: 10.1128/AAC.04124-14. Epub 2014 Nov 10.

16.

Negamycin induces translational stalling and miscoding by binding to the small subunit head domain of the Escherichia coli ribosome.

Olivier NB, Altman RB, Noeske J, Basarab GS, Code E, Ferguson AD, Gao N, Huang J, Juette MF, Livchak S, Miller MD, Prince DB, Cate JH, Buurman ET, Blanchard SC.

Proc Natl Acad Sci U S A. 2014 Nov 18;111(46):16274-9. doi: 10.1073/pnas.1414401111. Epub 2014 Nov 3.

17.

Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.

Basarab GS, Brassil P, Doig P, Galullo V, Haimes HB, Kern G, Kutschke A, McNulty J, Schuck VJ, Stone G, Gowravaram M.

J Med Chem. 2014 Nov 13;57(21):9078-95. doi: 10.1021/jm501174m. Epub 2014 Oct 17.

PMID:
25286019
18.

In vitro and in vivo metabolism of 14C-AZ11, a novel inhibitor of bacterial DNA gyrase/type II topoisomerase.

Guo J, Joubran C, Luzietti RA Jr, Zhou F, Basarab GS, Vishwanathan K.

Xenobiotica. 2015 Feb;45(2):158-70. doi: 10.3109/00498254.2014.952799. Epub 2014 Aug 21.

PMID:
25142218
19.

Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).

Basarab GS, Hill PJ, Garner CE, Hull K, Green O, Sherer BA, Dangel PB, Manchester JI, Bist S, Hauck S, Zhou F, Uria-Nickelsen M, Illingworth R, Alm R, Rooney M, Eakin AE.

J Med Chem. 2014 Jul 24;57(14):6060-82. doi: 10.1021/jm500462x. Epub 2014 Jul 8.

PMID:
24959892
20.

Fragment-to-hit-to-lead discovery of a novel pyridylurea scaffold of ATP competitive dual targeting type II topoisomerase inhibiting antibacterial agents.

Basarab GS, Manchester JI, Bist S, Boriack-Sjodin PA, Dangel B, Illingworth R, Sherer BA, Sriram S, Uria-Nickelsen M, Eakin AE.

J Med Chem. 2013 Nov 14;56(21):8712-35. doi: 10.1021/jm401208b. Epub 2013 Oct 29.

PMID:
24098982
21.

Design of inhibitors of Helicobacter pylori glutamate racemase as selective antibacterial agents: incorporation of imidazoles onto a core pyrazolopyrimidinedione scaffold to improve bioavailabilty.

Basarab GS, Hill P, Eyermann CJ, Gowravaram M, Käck H, Osimoni E.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5600-7. doi: 10.1016/j.bmcl.2012.07.004. Epub 2012 Jul 20.

PMID:
22877632
22.

Design of Helicobacter pylori glutamate racemase inhibitors as selective antibacterial agents: a novel pro-drug approach to increase exposure.

Basarab GS, Hill PJ, Rastagar A, Webborn PJ.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4716-22. doi: 10.1016/j.bmcl.2008.06.092. Epub 2008 Jul 2.

PMID:
18640833
23.

Design of inhibitors of scytalone dehydratase: probing interactions with an asparagine carboxamide.

Basarab GS, Jordan DB, Gehret TC, Schwartz RS.

Bioorg Med Chem. 2002 Dec;10(12):4143-54.

PMID:
12413868
24.
25.

Structure-based design of inhibitors of the rice blast fungal enzyme trihydroxynaphthalene reductase.

Jordan DB, Basarab GS, Liao DI, Johnson WM, Winzenberg KN, Winkler DA.

J Mol Graph Model. 2001;19(5):434-47, 470-1.

PMID:
11552692
26.

Structures of trihydroxynaphthalene reductase-fungicide complexes: implications for structure-based design and catalysis.

Liao D, Basarab GS, Gatenby AA, Valent B, Jordan DB.

Structure. 2001 Jan 10;9(1):19-27.

27.

Tight binding inhibitors of scytalone dehydratase: effects of site-directed mutations.

Jordan DB, Basarab GS, Steffens JJ, Schwartz RS, Doughty JG.

Biochemistry. 2000 Jul 25;39(29):8593-602.

PMID:
10913266
28.

Cyclobutane carboxamide inhibitors of fungal melanin: biosynthesis and their evaluation as fungicides.

Jennings LD, Rayner DR, Jordan DB, Okonya JF, Basarab GS, Amorose DK, Anaclerio BM, Lee JK, Schwartz RS, Whitmore KA.

Bioorg Med Chem. 2000 May;8(5):897-907.

PMID:
10882002
29.

Solvolytic enolization of scytalone.

Basarab GS, Jordan DB, Zheng YJ.

Org Lett. 2000 Jun 1;2(11):1541-4.

PMID:
10841474
30.

Selection of a potent inhibitor of trihydroxynaphthalene reductase by sorting disease control data.

Liao DI, Basarab GS, Gatenby AA, Jordan DB.

Bioorg Med Chem Lett. 2000 Mar 6;10(5):491-4.

PMID:
10743955
31.

Stereochemistry of the enolization of scytalone by scytalone dehydratase.

Jordan DB, Zheng YJ, Lockett BA, Basarab GS.

Biochemistry. 2000 Mar 7;39(9):2276-82.

PMID:
10694394
32.

Binding dynamics of two water molecules constrained within the scytalone dehydratase binding pocket.

Jordan DB, Basarab GS.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):23-6.

PMID:
10636235
33.

Wild-type enzyme as a reporter of inhibitor binding by catalytically impaired mutant enzymes.

Basarab GS, Jordan DB.

Biochem Biophys Res Commun. 1999 Oct 5;263(3):617-20.

PMID:
10512727
34.

Design of scytalone dehydratase inhibitors as rice blast fungicides: derivatives of norephedrine.

Basarab GS, Jordan DB, Gehret TC, Schwartz RS, Wawrzak Z.

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1613-8.

PMID:
10386946
35.

Design of scytalone dehydratase inhibitors as rice blast fungicides: (N-phenoxypropyl)-carboxamides.

Jordan DB, Lessen TA, Wawrzak Z, Bisaha JJ, Gehret TC, Hansen SL, Schwartz RS, Basarab GS.

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1607-12.

PMID:
10386945
36.

High-resolution structures of scytalone dehydratase-inhibitor complexes crystallized at physiological pH.

Wawrzak Z, Sandalova T, Steffens JJ, Basarab GS, Lundqvist T, Lindqvist Y, Jordan DB.

Proteins. 1999 Jun 1;35(4):425-39.

PMID:
10382670
37.

Catalytic mechanism of scytalone dehydratase: site-directed mutagenisis, kinetic isotope effects, and alternate substrates.

Basarab GS, Steffens JJ, Wawrzak Z, Schwartz RS, Lundqvist T, Jordan DB.

Biochemistry. 1999 May 11;38(19):6012-24.

PMID:
10320327
38.

Structure-based design of potent inhibitors of scytalone dehydratase: displacement of a water molecule from the active site.

Chen JM, Xu SL, Wawrzak Z, Basarab GS, Jordan DB.

Biochemistry. 1998 Dec 22;37(51):17735-44.

PMID:
9922139
39.

2,3-Dihydro-2,5-dihydroxy-4H-benzopyran-4-one: a nonphysiological substrate for fungal melanin biosynthetic enzymes.

Thompson JE, Basarab GS, Pierce J, Hodge CN, Jordan DB.

Anal Biochem. 1998 Feb 1;256(1):1-6.

PMID:
9466791
40.

Trihydroxynaphthalene reductase from Magnaporthe grisea: realization of an active center inhibitor and elucidation of the kinetic mechanism.

Thompson JE, Basarab GS, Andersson A, Lindqvist Y, Jordan DB.

Biochemistry. 1997 Feb 18;36(7):1852-60.

PMID:
9048570
41.

Crystal structure of scytalone dehydratase--a disease determinant of the rice pathogen, Magnaporthe grisea.

Lundqvist T, Rice J, Hodge CN, Basarab GS, Pierce J, Lindqvist Y.

Structure. 1994 Oct 15;2(10):937-44.

PMID:
7866745

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