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Items: 32

1.

The quest for the holy grail: new antitubercular chemical entities, targets and strategies.

Huszár S, Chibale K, Singh V.

Drug Discov Today. 2020 Feb 13. pii: S1359-6446(20)30071-4. doi: 10.1016/j.drudis.2020.02.003. [Epub ahead of print] Review.

2.

Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.

Karabanovich G, Dušek J, Savková K, Pavliš O, Pávková I, Korábečný J, Kučera T, Kočová Vlčková H, Huszár S, Konyariková Z, Konečná K, Jand'ourek O, Stolaříková J, Korduláková J, Vávrová K, Pávek P, Klimešová V, Hrabálek A, Mikušová K, Roh J.

J Med Chem. 2019 Sep 12;62(17):8115-8139. doi: 10.1021/acs.jmedchem.9b00912. Epub 2019 Aug 22.

PMID:
31393122
3.

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase.

Mori G, Orena BS, Franch C, Mitchenall LA, Godbole AA, Rodrigues L, Aguilar-Pérez C, Zemanová J, Huszár S, Forbak M, Lane TR, Sabbah M, Deboosere N, Frita R, Vandeputte A, Hoffmann E, Russo R, Connell N, Veilleux C, Jha RK, Kumar P, Freundlich JS, Brodin P, Aínsa JA, Nagaraja V, Maxwell A, Mikušová K, Pasca MR, Ekins S.

Tuberculosis (Edinb). 2018 Sep;112:98-109. doi: 10.1016/j.tube.2018.08.004. Epub 2018 Aug 11.

PMID:
30205975
4.

Copper-related toxicity in replicating and dormant Mycobacterium tuberculosis caused by 1-hydroxy-5-R-pyridine-2(1H)-thiones.

Salina EG, Huszár S, Zemanová J, Keruchenko J, Riabova O, Kazakova E, Grigorov A, Azhikina T, Kaprelyants A, Mikušová K, Makarov V.

Metallomics. 2018 Jul 18;10(7):992-1002. doi: 10.1039/c8mt00067k.

PMID:
29946601
5.

New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action.

Vosátka R, Krátký M, Švarcová M, Janoušek J, Stolaříková J, Madacki J, Huszár S, Mikušová K, Korduláková J, Trejtnar F, Vinšová J.

Eur J Med Chem. 2018 May 10;151:824-835. doi: 10.1016/j.ejmech.2018.04.017. Epub 2018 Apr 10.

PMID:
29679902
6.

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK.

Chiarelli LR, Mori G, Orena BS, Esposito M, Lane T, de Jesus Lopes Ribeiro AL, Degiacomi G, Zemanová J, Szádocka S, Huszár S, Palčeková Z, Manfredi M, Gosetti F, Lelièvre J, Ballell L, Kazakova E, Makarov V, Marengo E, Mikusova K, Cole ST, Riccardi G, Ekins S, Pasca MR.

Sci Rep. 2018 Feb 16;8(1):3187. doi: 10.1038/s41598-018-21614-4.

7.

N-Acetylglucosamine-1-Phosphate Transferase, WecA, as a Validated Drug Target in Mycobacterium tuberculosis.

Huszár S, Singh V, Polčicová A, Baráth P, Barrio MB, Lagrange S, Leblanc V, Nacy CA, Mizrahi V, Mikušová K.

Antimicrob Agents Chemother. 2017 Oct 24;61(11). pii: e01310-17. doi: 10.1128/AAC.01310-17. Print 2017 Nov.

8.

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors.

Esposito M, Szadocka S, Degiacomi G, Orena BS, Mori G, Piano V, Boldrin F, Zemanová J, Huszár S, Barros D, Ekins S, Lelièvre J, Manganelli R, Mattevi A, Pasca MR, Riccardi G, Ballell L, Mikušová K, Chiarelli LR.

ACS Infect Dis. 2017 Jun 9;3(6):428-437. doi: 10.1021/acsinfecdis.7b00006. Epub 2017 May 11.

PMID:
28475832
9.

Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.

Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA.

ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10.

10.

Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.

Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11.

PMID:
26810316
11.

Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Raheem IT, Schreier JD, Fuerst J, Gantert L, Hostetler ED, Huszar S, Joshi A, Kandebo M, Kim SH, Li J, Ma B, McGaughey G, Sharma S, Shipe WD, Uslaner J, Vandeveer GH, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):126-32. doi: 10.1016/j.bmcl.2015.11.013. Epub 2015 Nov 10.

PMID:
26602277
12.

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis.

Makarov V, Neres J, Hartkoorn RC, Ryabova OB, Kazakova E, Šarkan M, Huszár S, Piton J, Kolly GS, Vocat A, Conroy TM, Mikušová K, Cole ST.

Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. doi: 10.1128/AAC.00778-15. Epub 2015 May 18.

13.

DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization.

Brecik M, Centárová I, Mukherjee R, Kolly GS, Huszár S, Bobovská A, Kilacsková E, Mokošová V, Svetlíková Z, Šarkan M, Neres J, Korduláková J, Cole ST, Mikušová K.

ACS Chem Biol. 2015 Jul 17;10(7):1631-6. doi: 10.1021/acschembio.5b00237. Epub 2015 Apr 29.

PMID:
25906160
14.

[Assessment of risk factors for fractures in postmenopausal women with osteoporosis].

Ferencz V, Horváth C, Huszár S, Bors K.

Orv Hetil. 2015 Jan 25;156(4):146-53. doi: 10.1556/OH.2015.30088. Hungarian.

PMID:
25597319
15.

Identification of a small molecule with activity against drug-resistant and persistent tuberculosis.

Wang F, Sambandan D, Halder R, Wang J, Batt SM, Weinrick B, Ahmad I, Yang P, Zhang Y, Kim J, Hassani M, Huszar S, Trefzer C, Ma Z, Kaneko T, Mdluli KE, Franzblau S, Chatterjee AK, Johnsson K, Mikusova K, Besra GS, Fütterer K, Robbins SH, Barnes SW, Walker JR, Jacobs WR Jr, Schultz PG.

Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7. doi: 10.1073/pnas.1309171110. Epub 2013 Jun 17. Erratum in: Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15848. Robbins, Scott H [added]; Barnes, S Whitney [added]; Walker, John R [added]; Johnson, Kai [corrected to Johnsson, Kai].

16.

Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.

Parmentier-Batteur S, Hutson PH, Menzel K, Uslaner JM, Mattson BA, O'Brien JA, Magliaro BC, Forest T, Stump CA, Tynebor RM, Anthony NJ, Tucker TJ, Zhang XF, Gomez R, Huszar SL, Lambeng N, Fauré H, Le Poul E, Poli S, Rosahl TW, Rocher JP, Hargreaves R, Williams TM.

Neuropharmacology. 2014 Jul;82:161-73. doi: 10.1016/j.neuropharm.2012.12.003. Epub 2013 Jan 2.

PMID:
23291536
17.

Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Raheem IT, Breslin MJ, Fandozzi C, Fuerst J, Hill N, Huszar S, Kandebo M, Kim SH, Ma B, McGaughey G, Renger JJ, Schreier JD, Sharma S, Smith S, Uslaner J, Yan Y, Coleman PJ, Cox CD.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5903-8. doi: 10.1016/j.bmcl.2012.07.072. Epub 2012 Jul 27.

PMID:
22892116
18.

The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.

Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ.

Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013. Epub 2012 Jun 27.

PMID:
22750078
19.

T-type calcium channel antagonism produces antipsychotic-like effects and reduces stimulant-induced glutamate release in the nucleus accumbens of rats.

Uslaner JM, Smith SM, Huszar SL, Pachmerhiwala R, Hinchliffe RM, Vardigan JD, Nguyen SJ, Surles NO, Yao L, Barrow JC, Uebele VN, Renger JJ, Clark J, Hutson PH.

Neuropharmacology. 2012 Mar;62(3):1413-21. doi: 10.1016/j.neuropharm.2010.11.015. Epub 2010 Nov 24.

PMID:
21110986
20.

Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.

Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA.

ACS Med Chem Lett. 2010 Jul 12;1(8):406-10. doi: 10.1021/ml100115a. eCollection 2010 Nov 11.

21.

Genetic and pharmacological evaluation of cathepsin s in a mouse model of asthma.

Deschamps K, Cromlish W, Weicker S, Lamontagne S, Huszar SL, Gauthier JY, Mudgett JS, Guimond A, Romand R, Frossard N, Percival MD, Slipetz D, Tan CM.

Am J Respir Cell Mol Biol. 2011 Jul;45(1):81-7. doi: 10.1165/rcmb.2009-0392OC. Epub 2010 Sep 20.

PMID:
20855652
22.

3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.

Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD.

Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31.

PMID:
20409708
23.

MK-801 produces a deficit in sucrose preference that is reversed by clozapine, D-serine, and the metabotropic glutamate 5 receptor positive allosteric modulator CDPPB: relevance to negative symptoms associated with schizophrenia?

Vardigan JD, Huszar SL, McNaughton CH, Hutson PH, Uslaner JM.

Pharmacol Biochem Behav. 2010 Apr;95(2):223-9. doi: 10.1016/j.pbb.2010.01.010. Epub 2010 Feb 1.

PMID:
20122952
24.

Combined administration of an mGlu2/3 receptor agonist and a 5-HT 2A receptor antagonist markedly attenuate the psychomotor-activating and neurochemical effects of psychostimulants.

Uslaner JM, Smith SM, Huszar SL, Pachmerhiwala R, Hinchliffe RM, Vardigan JD, Hutson PH.

Psychopharmacology (Berl). 2009 Nov;206(4):641-51. doi: 10.1007/s00213-009-1644-y. Epub 2009 Aug 26.

PMID:
19707745
25.

The behavioral and neurochemical effects of a novel D-amino acid oxidase inhibitor compound 8 [4H-thieno [3,2-b]pyrrole-5-carboxylic acid] and D-serine.

Smith SM, Uslaner JM, Yao L, Mullins CM, Surles NO, Huszar SL, McNaughton CH, Pascarella DM, Kandebo M, Hinchliffe RM, Sparey T, Brandon NJ, Jones B, Venkatraman S, Young MB, Sachs N, Jacobson MA, Hutson PH.

J Pharmacol Exp Ther. 2009 Mar;328(3):921-30. doi: 10.1124/jpet.108.147884. Epub 2008 Dec 16.

PMID:
19088300
26.

Effect of different fat sources on in vitro degradation of nutrients and certain blood parameters in sheep.

Fébel H, Husvéth F, Veresegyházy T, Andrásofszky E, Várhegyi I, Huszár S.

Acta Vet Hung. 2002;50(2):217-29.

PMID:
12113177
27.

Effects of dietary protein and carbohydrate source on rumen fermentation and nutrient flow in sheep.

Fébel H, Huszár S, Harczi IZ.

Acta Vet Hung. 2000;48(2):161-71.

PMID:
11402698
28.
29.

Evaluation of the digestibility of nutrients in pigs by ileal cannulation technique.

Szelényi-Galátai M, Fébel H, Szegedi B, Zsolnai-Harczi I, Huszár S.

Acta Vet Hung. 1996;44(4):411-32.

PMID:
9141278
30.

Effect of avoparcin on rumen fermentation and duodenal nutrient flow in sheep.

Fébel H, Romváry A, Zsolnai-Harczi I, Huszár S.

Acta Vet Hung. 1995;43(2-3):229-46.

PMID:
7491862
31.

[Frequency behavior following myocardial infarct and heart surgery in early phase of mobilization].

Simon H, Huszár S, Kikis D, Fricke G, Esser H.

Verh Dtsch Ges Inn Med. 1973;79:1160-2. German. No abstract available.

PMID:
4790123
32.

[Optimal frequency in auricular fibrillation].

Fricke G, Simon H, Pagenstecher H, Kikis D, Huszár S.

Verh Dtsch Ges Inn Med. 1973;79:1061-4. German. No abstract available.

PMID:
4790096

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