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Items: 46

1.

Bifunctional Small Molecules Enhance Neutrophil Activities Against Aspergillus fumigatus in vivo and in vitro.

Jones CN, Ellett F, Robertson AL, Forrest KM, Judice K, Balkovec JM, Springer M, Markmann JF, Vyas JM, Warren HS, Irimia D.

Front Immunol. 2019 Apr 9;10:644. doi: 10.3389/fimmu.2019.00644. eCollection 2019.

2.

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP.

Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27.

PMID:
30952592
3.

Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21.

PMID:
30926247
4.

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.

Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD.

J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2.

PMID:
28252959
5.

Preclinical Evaluation of the Stability, Safety, and Efficacy of CD101, a Novel Echinocandin.

Ong V, Hough G, Schlosser M, Bartizal K, Balkovec JM, James KD, Krishnan BR.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6872-6879. doi: 10.1128/AAC.00701-16. Print 2016 Nov.

6.

Novel orally active inhibitors of β-1,3-glucan synthesis derived from enfumafungin.

Apgar JM, Wilkening RR, Greenlee ML, Balkovec JM, Flattery AM, Abruzzo GK, Galgoci AM, Giacobbe RA, Gill CJ, Hsu MJ, Liberator P, Misura AS, Motyl M, Nielsen Kahn J, Powles M, Racine F, Dragovic J, Habulihaz B, Fan W, Kirwan R, Lee S, Liu H, Mamai A, Nelson K, Peel M.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5813-8. doi: 10.1016/j.bmcl.2015.10.011. Epub 2015 Oct 9.

PMID:
26542966
7.

Rapid development of two factor IXa inhibitors from hit to lead.

Parker DL Jr, Walsh S, Li B, Kim E, Sharipour A, Smith C, Chen YH, Berger R, Harper B, Zhang T, Park M, Shu M, Wu J, Xu J, Dewnani S, Sherer EC, Hruza A, Reichert P, Geissler W, Sonatore L, Ellsworth K, Balkovec J, Greenlee W, Wood HB.

Bioorg Med Chem Lett. 2015 Jun 1;25(11):2321-5. doi: 10.1016/j.bmcl.2015.04.025. Epub 2015 Apr 13.

PMID:
25937013
8.

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9.

9.

Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.

He S, Hong Q, Lai Z, Wu Z, Yu Y, Kim DW, Ting PC, Kuethe JT, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sperbeck DM, Sonatore LM, Wiltsie J, Chung CC, Gibson JT, Lisnock J, Murphy BA, Gorski JN, Liu J, Chen D, Chen X, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2013 Jun 6;4(8):773-8. doi: 10.1021/ml400168h. eCollection 2013 Aug 8.

10.

Discovery and development of first in class antifungal caspofungin (CANCIDAS®)--a case study.

Balkovec JM, Hughes DL, Masurekar PS, Sable CA, Schwartz RE, Singh SB.

Nat Prod Rep. 2014 Jan;31(1):15-34. doi: 10.1039/c3np70070d. Review.

PMID:
24270605
11.

Pharmacological inhibition of diacylglycerol acyltransferase 1 reduces body weight and modulates gut peptide release--potential insight into mechanism of action.

Liu J, Gorski JN, Gold SJ, Chen D, Chen S, Forrest G, Itoh Y, Marsh DJ, McLaren DG, Shen Z, Sonatore L, Carballo-Jane E, Craw S, Guan X, Karanam B, Sakaki J, Szeto D, Tong X, Xiao J, Yoshimoto R, Yu H, Roddy TP, Balkovec J, Pinto S.

Obesity (Silver Spring). 2013 Jul;21(7):1406-15. doi: 10.1002/oby.20193. Epub 2013 May 13.

12.

11β-HSD1 inhibition reduces atherosclerosis in mice by altering proinflammatory gene expression in the vasculature.

Luo MJ, Thieringer R, Springer MS, Wright SD, Hermanowski-Vosatka A, Plump A, Balkovec JM, Cheng K, Ding GJ, Kawka DW, Koo GC, Grand CB, Luo Q, Maletic MM, Malkowitz L, Shah K, Singer I, Waddell ST, Wu KK, Yuan J, Zhu J, Stepaniants S, Yang X, Lum PY, Wang IM.

Physiol Genomics. 2013 Jan 7;45(1):47-57. doi: 10.1152/physiolgenomics.00109.2012. Epub 2012 Nov 20.

PMID:
23170035
13.

Synthesis and biological evaluation of antifungal derivatives of enfumafungin as orally bioavailable inhibitors of β-1,3-glucan synthase.

Heasley BH, Pacofsky GJ, Mamai A, Liu H, Nelson K, Coti G, Peel MR, Balkovec JM, Greenlee ML, Liberator P, Meng D, Parker DL, Wilkening RR, Apgar JM, Racine F, Hsu MJ, Giacobbe RA, Kahn JN.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6811-6. doi: 10.1016/j.bmcl.2012.05.031. Epub 2012 May 17.

PMID:
22672801
14.

Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.

Maletic M, Leeman A, Szymonifka M, Mundt SS, Zokian HJ, Shah K, Dragovic J, Lyons K, Thieringer R, Vosatka AH, Balkovec J, Waddell ST.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2568-72. doi: 10.1016/j.bmcl.2011.01.018. Epub 2011 Jan 11.

PMID:
21421311
15.

The use of stable-isotopically labeled oleic acid to interrogate lipid assembly in vivo: assessing pharmacological effects in preclinical species.

McLaren DG, He T, Wang SP, Mendoza V, Rosa R, Gagen K, Bhat G, Herath K, Miller PL, Stribling S, Taggart A, Imbriglio J, Liu J, Chen D, Pinto S, Balkovec JM, Devita RJ, Marsh DJ, Castro-Perez JM, Strack A, Johns DG, Previs SF, Hubbard BK, Roddy TP.

J Lipid Res. 2011 Jun;52(6):1150-61. doi: 10.1194/jlr.M011049. Epub 2011 Mar 17.

16.

Substituted phenyl triazoles as selective inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1.

Sun W, Maletic M, Mundt SS, Shah K, Zokian H, Lyons K, Waddell ST, Balkovec J.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2141-5. doi: 10.1016/j.bmcl.2011.01.125. Epub 2011 Feb 2.

PMID:
21334894
17.

Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.

Ali A, Balkovec JM, Greenlee M, Hammond ML, Rouen G, Taylor G, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Forrest MJ, Carballo-Jane E, Luell S, Lowitz K, Visco D.

Bioorg Med Chem. 2008 Aug 15;16(16):7535-42. doi: 10.1016/j.bmc.2008.07.037. Epub 2008 Jul 20.

PMID:
18691892
18.

Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Zhu Y, Olson SH, Graham D, Patel G, Hermanowski-Vosatka A, Mundt S, Shah K, Springer M, Thieringer R, Wright S, Xiao J, Zokian H, Dragovic J, Balkovec JM.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3412-6. doi: 10.1016/j.bmcl.2008.04.014. Epub 2008 Apr 10.

PMID:
18440812
19.

4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Zhu Y, Olson SH, Hermanowski-Vosatka A, Mundt S, Shah K, Springer M, Thieringer R, Wright S, Xiao J, Zokian H, Balkovec JM.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3405-11. doi: 10.1016/j.bmcl.2008.04.013. Epub 2008 Apr 10.

PMID:
18440811
20.

Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Aster SD, Graham DW, Kharbanda D, Patel G, Ponpipom M, Santorelli GM, Szymonifka MJ, Mundt SS, Shah K, Springer MS, Thieringer R, Hermanowski-Vosatka A, Wright SD, Xiao J, Zokian H, Balkovec JM.

Bioorg Med Chem Lett. 2008 May 1;18(9):2799-804. doi: 10.1016/j.bmcl.2008.04.010. Epub 2008 Apr 9.

PMID:
18434143
21.

Attenuating pregnane X receptor (PXR) activation: a molecular modelling approach.

Gao YD, Olson SH, Balkovec JM, Zhu Y, Royo I, Yabut J, Evers R, Tan EY, Tang W, Hartley DP, Mosley RT.

Xenobiotica. 2007 Feb;37(2):124-38.

PMID:
17484516
22.

Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.

Thompson CF, Quraishi N, Ali A, Mosley RT, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3354-61. Epub 2007 Apr 5.

PMID:
17467988
23.

Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.

Gu X, Dragovic J, Koo GC, Koprak SL, LeGrand C, Mundt SS, Shah K, Springer MS, Tan EY, Thieringer R, Hermanowski-Vosatka A, Zokian HJ, Balkovec JM, Waddell ST.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. Epub 2005 Sep 26.

PMID:
16185866
24.

11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.

Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, Noonan H, Nunes CN, Olson SH, Pikounis B, Ren N, Robertson N, Schaeffer JM, Shah K, Springer MS, Strack AM, Strowski M, Wu K, Wu T, Xiao J, Zhang BB, Wright SD, Thieringer R.

J Exp Med. 2005 Aug 15;202(4):517-27.

25.

Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Olson S, Aster SD, Brown K, Carbin L, Graham DW, Hermanowski-Vosatka A, LeGrand CB, Mundt SS, Robbins MA, Schaeffer JM, Slossberg LH, Szymonifka MJ, Thieringer R, Wright SD, Balkovec JM.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4359-62.

PMID:
16039856
26.

Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.

Smith CJ, Ali A, Balkovec JM, Graham DW, Hammond ML, Patel GF, Rouen GP, Smith SK, Tata JR, Einstein M, Ge L, Harris GS, Kelly TM, Mazur P, Thompson CM, Wang CF, Williamson JM, Miller DK, Pandit S, Santoro JC, Sitlani A, Yamin TT, O'Neill EA, Zaller DM, Carballo-Jane E, Forrest MJ, Luell S.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2926-31.

PMID:
15911283
27.

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7.

PMID:
15808489
28.

Selective glucocorticoid receptor nonsteroidal ligands completely antagonize the dexamethasone mediated induction of enzymes involved in gluconeogenesis and glutamine metabolism.

Einstein M, Greenlee M, Rouen G, Sitlani A, Santoro J, Wang C, Pandit S, Mazur P, Smalera I, Weaver AP, Zeng YY, Ge L, Kelly T, Paiva T, Geissler W, Mosley RT, Williamson J, Ali A, Balkovec J, Harris G.

J Steroid Biochem Mol Biol. 2004 Dec;92(5):345-56. Epub 2005 Jan 21.

PMID:
15698539
29.

Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.

Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S.

J Med Chem. 2004 May 6;47(10):2441-52.

PMID:
15115388
30.

The first stereoselective total synthesis of quinine.

Stork G, Niu D, Fujimoto RA, Koft ER, Balkovec JM, Tata JR, Dake GR.

J Am Chem Soc. 2001 Apr 11;123(14):3239-42. Erratum in: J Am Chem Soc 2001 Sep 5;123(35):8644. Fujimoto A [corrected to Fujimoto RA].

PMID:
11457058
31.

Succinic acids as potent inhibitors of plasmid-borne IMP-1 metallo-beta-lactamase.

Toney JH, Hammond GG, Fitzgerald PM, Sharma N, Balkovec JM, Rouen GP, Olson SH, Hammond ML, Greenlee ML, Gao YD.

J Biol Chem. 2001 Aug 24;276(34):31913-8. Epub 2001 Jun 4.

32.

Inhibition of IMP-1 metallo-beta-lactamase and sensitization of IMP-1-producing bacteria by thioester derivatives.

Hammond GG, Huber JL, Greenlee ML, Laub JB, Young K, Silver LL, Balkovec JM, Pryor KD, Wu JK, Leiting B, Pompliano DL, Toney JH.

FEMS Microbiol Lett. 1999 Oct 15;179(2):289-96.

33.

Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.

Greenlee ML, Laub JB, Balkovec JM, Hammond ML, Hammond GG, Pompliano DL, Epstein-Toney JH.

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2549-54.

PMID:
10498206
34.

Alkyl side-chain derivatives of sordaricin as potent antifungal agents against yeast.

Tse B, Balkovec JM, Blazey CM, Hsu MJ, Nielsen J, Schmatz D.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2269-72.

PMID:
9873526
35.

Efficacy of MK-991 (L-743,872), a semisynthetic pneumocandin, in murine models of Pneumocystis carinii.

Powles MA, Liberator P, Anderson J, Karkhanis Y, Dropinski JF, Bouffard FA, Balkovec JM, Fujioka H, Aikawa M, McFadden D, Schmatz D.

Antimicrob Agents Chemother. 1998 Aug;42(8):1985-9.

36.

Elongation factor 2 as a novel target for selective inhibition of fungal protein synthesis.

Justice MC, Hsu MJ, Tse B, Ku T, Balkovec J, Schmatz D, Nielsen J.

J Biol Chem. 1998 Feb 6;273(6):3148-51.

37.

Evaluation of the echinocandin antifungal MK-0991 (L-743,872): efficacies in mouse models of disseminated aspergillosis, candidiasis, and cryptococcosis.

Abruzzo GK, Flattery AM, Gill CJ, Kong L, Smith JG, Pikounis VB, Balkovec JM, Bouffard AF, Dropinski JF, Rosen H, Kropp H, Bartizal K.

Antimicrob Agents Chemother. 1997 Nov;41(11):2333-8.

38.

In vitro preclinical evaluation studies with the echinocandin antifungal MK-0991 (L-743,872).

Bartizal K, Gill CJ, Abruzzo GK, Flattery AM, Kong L, Scott PM, Smith JG, Leighton CE, Bouffard A, Dropinski JF, Balkovec J.

Antimicrob Agents Chemother. 1997 Nov;41(11):2326-32.

39.

Determination of the Absolute Stereochemistry of (-)-Galbonolide A.

Tse B, Blazey CM, Tu B, Balkovec J.

J Org Chem. 1997 May 16;62(10):3236-3241.

PMID:
11671709
40.

Increased antifungal activity of L-733,560, a water-soluble, semisynthetic pneumocandin, is due to enhanced inhibition of cell wall synthesis.

Kurtz MB, Douglas C, Marrinan J, Nollstadt K, Onishi J, Dreikorn S, Milligan J, Mandala S, Thompson J, Balkovec JM, et al.

Antimicrob Agents Chemother. 1994 Dec;38(12):2750-7.

41.

Synthesis and antifungal activity of novel cationic pneumocandin B(o) derivatives.

Bouffard FA, Zambias RA, Dropinski JF, Balkovec JM, Hammond ML, Abruzzo GK, Bartizal KF, Marrinan JA, Kurtz MB, McFadden DC, et al.

J Med Chem. 1994 Jan 21;37(2):222-5. No abstract available.

PMID:
8295208
42.

Pneumocandins from Zalerion arboricola. IV. Biological evaluation of natural and semisynthetic pneumocandins for activity against Pneumocystis carinii and Candida species.

Schmatz DM, Abruzzo G, Powles MA, McFadden DC, Balkovec JM, Black RM, Nollstadt K, Bartizal K.

J Antibiot (Tokyo). 1992 Dec;45(12):1886-91.

43.

Antipneumocystis activity of water-soluble lipopeptide L-693,989 in rats.

Schmatz DM, Powles MA, McFadden DC, Pittarelli L, Balkovec J, Hammond M, Zambias R, Liberator P, Anderson J.

Antimicrob Agents Chemother. 1992 Sep;36(9):1964-70.

44.

In vitro antifungal activities and in vivo efficacies of 1,3-beta-D-glucan synthesis inhibitors L-671,329, L-646,991, tetrahydroechinocandin B, and L-687,781, a papulacandin.

Bartizal K, Abruzzo G, Trainor C, Krupa D, Nollstadt K, Schmatz D, Schwartz R, Hammond M, Balkovec J, Vanmiddlesworth F.

Antimicrob Agents Chemother. 1992 Aug;36(8):1648-57.

45.

Synthesis, stability, and biological evaluation of water-soluble prodrugs of a new echinocandin lipopeptide. Discovery of a potential clinical agent for the treatment of systemic candidiasis and Pneumocystis carinii pneumonia (PCP).

Balkovec JM, Black RM, Hammond ML, Heck JV, Zambias RA, Abruzzo G, Bartizal K, Kropp H, Trainor C, Schwartz RE, et al.

J Med Chem. 1992 Jan;35(1):194-8. No abstract available.

PMID:
1732529
46.

Basic carbapenem analogs: synthesis and in vitro activity of 1 beta-methyl-2-(pyridylmethylthio)-carbapenems.

Balkovec JM, Szymonifka M, Heck JV, Ratcliffe RW.

J Antibiot (Tokyo). 1991 Oct;44(10):1172-7. No abstract available.

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