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Items: 1 to 50 of 301

1.

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.

Stoye A, Juillard A, Tang AH, Legac J, Gut J, White KL, Charman SA, Rosenthal PJ, Grau GER, Hunt NH, Payne RJ.

J Med Chem. 2019 Jun 13;62(11):5562-5578. doi: 10.1021/acs.jmedchem.9b00504. Epub 2019 May 22.

PMID:
31062592
2.

Efficacy of subcutaneous doses and a new oral amorphous solid dispersion formulation of flubendazole on male jirds (Meriones unguiculatus) infected with the filarial nematode Brugia pahangi.

Fischer C, Ibiricu Urriza I, Bulman CA, Lim KC, Gut J, Lachau-Durand S, Engelen M, Quirynen L, Tekle F, Baeten B, Beerntsen B, Lustigman S, Sakanari J.

PLoS Negl Trop Dis. 2019 Jan 16;13(1):e0006787. doi: 10.1371/journal.pntd.0006787. eCollection 2019 Jan.

3.

Endoperoxide-8-aminoquinoline hybrids as dual-stage antimalarial agents with enhanced metabolic stability.

Capela R, Magalhães J, Miranda D, Machado M, Sanches-Vaz M, Albuquerque IS, Sharma M, Gut J, Rosenthal PJ, Frade R, Perry MJ, Moreira R, Prudêncio M, Lopes F.

Eur J Med Chem. 2018 Apr 10;149:69-78. doi: 10.1016/j.ejmech.2018.02.048. Epub 2018 Feb 19.

PMID:
29499488
4.

Non-invasive Detection of Bladder Tumors Through Volatile Organic Compounds: A Pilot Study with an Electronic Nose.

Heers H, Gut JM, Hegele A, Hofmann R, Boeselt T, Hattesohl A, Koczulla AR.

Anticancer Res. 2018 Feb;38(2):833-837.

PMID:
29374709
5.

Microwave-promoted facile access to 4-aminoquinoline-phthalimides: Synthesis and anti-plasmodial evaluation.

Rani A, Singh A, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2018 Jan 1;143:150-156. doi: 10.1016/j.ejmech.2017.11.033. Epub 2017 Nov 16.

PMID:
29174811
6.

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).

Previti S, Ettari R, Cosconati S, Amendola G, Chouchene K, Wagner A, Hellmich UA, Ulrich K, Krauth-Siegel RL, Wich PR, Schmid I, Schirmeister T, Gut J, Rosenthal PJ, Grasso S, Zappalà M.

J Med Chem. 2017 Aug 24;60(16):6911-6923. doi: 10.1021/acs.jmedchem.7b00405. Epub 2017 Aug 11.

PMID:
28763614
7.

4-Aminoquinoline-chalcone/-N-acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation.

Kumar S, Saini A, Gut J, Rosenthal PJ, Raj R, Kumar V.

Eur J Med Chem. 2017 Sep 29;138:993-1001. doi: 10.1016/j.ejmech.2017.07.041. Epub 2017 Jul 22.

PMID:
28756265
8.

Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.

Blank BR, Gut J, Rosenthal PJ, Renslo AR.

J Med Chem. 2017 Jul 27;60(14):6400-6407. doi: 10.1021/acs.jmedchem.7b00699. Epub 2017 Jul 10.

9.

Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation.

Singh A, Rani A, Gut J, Rosenthal PJ, Kumar V.

Chem Biol Drug Des. 2017 Oct;90(4):590-595. doi: 10.1111/cbdd.12982. Epub 2017 Apr 26.

PMID:
28332319
10.

A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue.

Sonoiki E, Ng CL, Lee MC, Guo D, Zhang YK, Zhou Y, Alley MR, Ahyong V, Sanz LM, Lafuente-Monasterio MJ, Dong C, Schupp PG, Gut J, Legac J, Cooper RA, Gamo FJ, DeRisi J, Freund YR, Fidock DA, Rosenthal PJ.

Nat Commun. 2017 Mar 6;8:14574. doi: 10.1038/ncomms14574.

11.

Familial hematuria: A review.

Plevová P, Gut J, Janda J.

Medicina (Kaunas). 2017;53(1):1-10. doi: 10.1016/j.medici.2017.01.002. Epub 2017 Jan 31. Review.

12.

Using ultrasound technology for the inactivation and thermal sensitization of peroxidase in green coconut water.

Rojas ML, Trevilin JH, Funcia EDS, Gut JAW, Augusto PED.

Ultrason Sonochem. 2017 May;36:173-181. doi: 10.1016/j.ultsonch.2016.11.028. Epub 2016 Nov 25.

PMID:
28069198
13.

4-Aminoquinoline-ferrocenyl-chalcone conjugates: Synthesis and anti-plasmodial evaluation.

Singh A, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2017 Jan 5;125:269-277. doi: 10.1016/j.ejmech.2016.09.044. Epub 2016 Sep 15.

PMID:
27688182
14.

Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites.

Carrasco MP, Machado M, Gonçalves L, Sharma M, Gut J, Lukens AK, Wirth DF, André V, Duarte MT, Guedes RC, Dos Santos DJ, Rosenthal PJ, Mazitschek R, Prudêncio M, Moreira R.

ChemMedChem. 2016 Oct 6;11(19):2194-2204. doi: 10.1002/cmdc.201600327. Epub 2016 Aug 19.

PMID:
27538856
15.

Cryptosporidium and Toxoplasma Parasites Are Inhibited by a Benzoxaborole Targeting Leucyl-tRNA Synthetase.

Palencia A, Liu RJ, Lukarska M, Gut J, Bougdour A, Touquet B, Wang ED, Li X, Alley MR, Freund YR, Rosenthal PJ, Hakimi MA, Cusack S.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):5817-27. doi: 10.1128/AAC.00873-16. Print 2016 Oct.

16.

Antimalarial Benzoxaboroles Target Plasmodium falciparum Leucyl-tRNA Synthetase.

Sonoiki E, Palencia A, Guo D, Ahyong V, Dong C, Li X, Hernandez VS, Zhang YK, Choi W, Gut J, Legac J, Cooper R, Alley MR, Freund YR, DeRisi J, Cusack S, Rosenthal PJ.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4886-95. doi: 10.1128/AAC.00820-16. Print 2016 Aug.

17.

Novel squaramides with in vitro liver stage antiplasmodial activity.

Ribeiro CJ, Espadinha M, Machado M, Gut J, Gonçalves LM, Rosenthal PJ, Prudêncio M, Moreira R, Santos MM.

Bioorg Med Chem. 2016 Apr 15;24(8):1786-92. doi: 10.1016/j.bmc.2016.03.005. Epub 2016 Mar 3.

PMID:
26968650
18.

Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.

Lauterwasser EM, Fontaine SD, Li H, Gut J, Katneni K, Charman SA, Rosenthal PJ, Bogyo M, Renslo AR.

ACS Med Chem Lett. 2015 Oct 2;6(11):1145-9. doi: 10.1021/acsmedchemlett.5b00296. eCollection 2015 Nov 12.

19.

Enantiopure Indolizinoindolones with in vitro Activity against Blood- and Liver-Stage Malaria Parasites.

Pereira NA, Monteiro Â, Machado M, Gut J, Molins E, Perry MJ, Dourado J, Moreira R, Rosenthal PJ, Prudêncio M, Santos MM.

ChemMedChem. 2015 Dec;10(12):2080-9. doi: 10.1002/cmdc.201500429. Epub 2015 Nov 3.

PMID:
26525306
20.

Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease.

Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin MR, Ellman JA, Renslo AR.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4834-4837. doi: 10.1016/j.bmcl.2015.06.066. Epub 2015 Jun 23.

21.

Extracts from Annona Muricata L. and Annona Reticulata L. (Annonaceae) Potently and Selectively Inhibit Plasmodium Falciparum.

Yamthe LRT, Fokou PVT, Mbouna CDJ, Keumoe R, Ndjakou BL, Djouonzo PT, Mfopa AN, Legac J, Tsabang N, Gut J, Rosenthal PJ, Boyom FF.

Medicines (Basel). 2015 Apr 30;2(2):55-66. doi: 10.3390/medicines2020055.

22.

Synthesis and in vitro antiplasmodial evaluation of 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone conjugates.

Raj R, Saini A, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2015 May 5;95:230-9. doi: 10.1016/j.ejmech.2015.03.045. Epub 2015 Mar 20.

PMID:
25817773
23.

Targeting the erythrocytic and liver stages of malaria parasites with s-triazine-based hybrids.

Rodrigues CA, Frade RF, Albuquerque IS, Perry MJ, Gut J, Machado M, Rosenthal PJ, Prudêncio M, Afonso CA, Moreira R.

ChemMedChem. 2015 May;10(5):883-90. doi: 10.1002/cmdc.201500011. Epub 2015 Mar 17.

PMID:
25784585
24.

Impact of antimalarial treatment and chemoprevention on the drug sensitivity of malaria parasites isolated from ugandan children.

Tumwebaze P, Conrad MD, Walakira A, LeClair N, Byaruhanga O, Nakazibwe C, Kozak B, Bloome J, Okiring J, Kakuru A, Bigira V, Kapisi J, Legac J, Gut J, Cooper RA, Kamya MR, Havlir DV, Dorsey G, Greenhouse B, Nsobya SL, Rosenthal PJ.

Antimicrob Agents Chemother. 2015;59(6):3018-30. doi: 10.1128/AAC.05141-14. Epub 2015 Mar 9.

25.

N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity.

Figueiras M, Coelho L, Wicht KJ, Santos SA, Lavrado J, Gut J, Rosenthal PJ, Nogueira F, Egan TJ, Moreira R, Paulo A.

Bioorg Med Chem. 2015 Apr 1;23(7):1530-9. doi: 10.1016/j.bmc.2015.02.007. Epub 2015 Feb 13.

PMID:
25725608
26.

Repurposing auranofin as a lead candidate for treatment of lymphatic filariasis and onchocerciasis.

Bulman CA, Bidlow CM, Lustigman S, Cho-Ngwa F, Williams D, Rascón AA Jr, Tricoche N, Samje M, Bell A, Suzuki B, Lim KC, Supakorndej N, Supakorndej P, Wolfe AR, Knudsen GM, Chen S, Wilson C, Ang KH, Arkin M, Gut J, Franklin C, Marcellino C, McKerrow JH, Debnath A, Sakanari JA.

PLoS Negl Trop Dis. 2015 Feb 20;9(2):e0003534. doi: 10.1371/journal.pntd.0003534. eCollection 2015 Feb.

27.

Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2.

Sharma RK, Younis Y, Mugumbate G, Njoroge M, Gut J, Rosenthal PJ, Chibale K.

Eur J Med Chem. 2015 Jan 27;90:507-18. doi: 10.1016/j.ejmech.2014.11.061. Epub 2014 Dec 2.

PMID:
25486422
28.

Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.

Conroy T, Guo JT, Elias N, Cergol KM, Gut J, Legac J, Khatoon L, Liu Y, McGowan S, Rosenthal PJ, Hunt NH, Payne RJ.

J Med Chem. 2014 Dec 26;57(24):10557-63. doi: 10.1021/jm501439w. Epub 2014 Dec 8.

PMID:
25412465
29.

Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

Vieira DF, Choi JY, Calvet CM, Siqueira-Neto JL, Johnston JB, Kellar D, Gut J, Cameron MD, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Dec 11;57(23):10162-75. doi: 10.1021/jm501568b. Epub 2014 Nov 25.

30.

Drug delivery to the malaria parasite using an arterolane-like scaffold.

Fontaine SD, Spangler B, Gut J, Lauterwasser EM, Rosenthal PJ, Renslo AR.

ChemMedChem. 2015 Jan;10(1):47-51. doi: 10.1002/cmdc.201402362. Epub 2014 Oct 14.

31.

Lead identification to clinical candidate selection: drugs for Chagas disease.

Neitz RJ, Chen S, Supek F, Yeh V, Kellar D, Gut J, Bryant C, Gallardo-Godoy A, Molteni V, Roach SL, Khare S, Stinson M, Chatterjee AK, Robertson S, Renslo AR, Arkin M, Glynne R, McKerrow J, Siqueira-Neto JL.

J Biomol Screen. 2015 Jan;20(1):101-11. doi: 10.1177/1087057114553103. Epub 2014 Oct 3. Erratum in: J Biomol Screen. 2015 Aug;20(7):927.

PMID:
25281737
32.

4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.

Calvet CM, Vieira DF, Choi JY, Kellar D, Cameron MD, Siqueira-Neto JL, Gut J, Johnston JB, Lin L, Khan S, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Aug 28;57(16):6989-7005. doi: 10.1021/jm500448u. Epub 2014 Aug 19.

33.

β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.

Nisha, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2014 Sep 12;84:566-73. doi: 10.1016/j.ejmech.2014.07.064. Epub 2014 Jul 21.

PMID:
25062007
34.

Discovery of highly selective 7-chloroquinoline-thiohydantoins with potent antimalarial activity.

Raj R, Mehra V, Gut J, Rosenthal PJ, Wicht KJ, Egan TJ, Hopper M, Wrischnik LA, Land KM, Kumar V.

Eur J Med Chem. 2014 Sep 12;84:425-32. doi: 10.1016/j.ejmech.2014.07.048. Epub 2014 Jul 15.

PMID:
25038484
35.

Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.

Dandapani S, Germain AR, Jewett I, le Quement S, Marie JC, Muncipinto G, Duvall JR, Carmody LC, Perez JR, Engel JC, Gut J, Kellar D, Siqueira-Neto JL, McKerrow JH, Kaiser M, Rodriguez A, Palmer MA, Foley M, Schreiber SL, Munoz B.

ACS Med Chem Lett. 2013 Dec 29;5(2):149-53. doi: 10.1021/ml400403u. eCollection 2014 Feb 13.

36.

Novel endoperoxide-based transmission-blocking antimalarials with liver- and blood-schizontocidal activities.

Miranda D, Capela R, Albuquerque IS, Meireles P, Paiva I, Nogueira F, Amewu R, Gut J, Rosenthal PJ, Oliveira R, Mota MM, Moreira R, Marti F, Prudêncio M, O'Neill PM, Lopes F.

ACS Med Chem Lett. 2013 Dec 20;5(2):108-12. doi: 10.1021/ml4002985. eCollection 2014 Feb 13.

37.

Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids.

Andayi WA, Egan TJ, Gut J, Rosenthal PJ, Chibale K.

ACS Med Chem Lett. 2013 May 20;4(7):642-6. doi: 10.1021/ml4001084. eCollection 2013 Jul 11.

38.

Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.

Njogu PM, Gut J, Rosenthal PJ, Chibale K.

ACS Med Chem Lett. 2013 May 22;4(7):637-41. doi: 10.1021/ml400164t. eCollection 2013 Jul 11.

39.

Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

Tukulula M, Njoroge M, Abay ET, Mugumbate GC, Wiesner L, Taylor D, Gibhard L, Norman J, Swart KJ, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Kameni-Tcheudji J, Chibale K.

ACS Med Chem Lett. 2013 Oct 1;4(12):1198-202. doi: 10.1021/ml400311r. eCollection 2013 Dec 12.

40.

Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials.

Oliveira R, Guedes RC, Meireles P, Albuquerque IS, Gonçalves LM, Pires E, Bronze MR, Gut J, Rosenthal PJ, Prudêncio M, Moreira R, O'Neill PM, Lopes F.

J Med Chem. 2014 Jun 12;57(11):4916-23. doi: 10.1021/jm5004528. Epub 2014 May 22.

PMID:
24824551
41.

Hsp90 inhibitors as new leads to target parasitic diarrheal diseases.

Debnath A, Shahinas D, Bryant C, Hirata K, Miyamoto Y, Hwang G, Gut J, Renslo AR, Pillai DR, Eckmann L, Reed SL, McKerrow JH.

Antimicrob Agents Chemother. 2014 Jul;58(7):4138-44. doi: 10.1128/AAC.02576-14. Epub 2014 May 12.

42.

Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity.

Carrasco MP, Newton AS, Gonçalves L, Góis A, Machado M, Gut J, Nogueira F, Hänscheid T, Guedes RC, dos Santos DJ, Rosenthal PJ, Moreira R.

Eur J Med Chem. 2014 Jun 10;80:523-34. doi: 10.1016/j.ejmech.2014.04.076. Epub 2014 Apr 28.

PMID:
24813880
43.

Bis-alkylamine Indolo[3,2-b]quinolines as hemozoin ligands: implications for antimalarial cytostatic and cytocidal activities.

Paulo A, Figueiras M, Machado M, Charneira C, Lavrado J, Santos SA, Lopes D, Gut J, Rosenthal PJ, Nogueira F, Moreira R.

J Med Chem. 2014 Apr 24;57(8):3295-313. doi: 10.1021/jm500075d. Epub 2014 Apr 15.

PMID:
24673163
44.

Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of α-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum.

Weldon DJ, Shah F, Chittiboyina AG, Sheri A, Chada RR, Gut J, Rosenthal PJ, Shivakumar D, Sherman W, Desai P, Jung JC, Avery MA.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1274-9. doi: 10.1016/j.bmcl.2014.01.062. Epub 2014 Jan 31.

PMID:
24507921
45.

Identification of Diversity-Oriented Synthesis Derived Small Molecule, ML341, with Cidal Activity Against Trypanosoma cruzi.

Carmody LC, Germain AR, Engel JC, Gut J, Kaiser M, Jewett I, LeQuemen S, Marie JC, Dandapani S, Rodriguez A, Perez JR, McKerrow JH, Palmer MAJ, Munoz B, Schrieber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 17 [updated 2013 Nov 7].

46.

1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: synthesis and antimalarial evaluation.

Raj R, Gut J, Rosenthal PJ, Kumar V.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):756-9. doi: 10.1016/j.bmcl.2013.12.109. Epub 2014 Jan 3.

PMID:
24424135
47.

7-chloroquinoline-isatin conjugates: antimalarial, antitubercular, and cytotoxic evaluation.

Raj R, Biot C, Carrère-Kremer S, Kremer L, Guérardel Y, Gut J, Rosenthal PJ, Forge D, Kumar V.

Chem Biol Drug Des. 2014 May;83(5):622-9. doi: 10.1111/cbdd.12273. Epub 2014 Mar 14.

PMID:
24341638
48.

Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.

Singh P, Raj R, Singh P, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2014 Jan;71:128-34. doi: 10.1016/j.ejmech.2013.10.079. Epub 2013 Nov 9.

PMID:
24287561
49.

Novel anti-plasmodial hits identified by virtual screening of the ZINC database.

Mugumbate G, Newton AS, Rosenthal PJ, Gut J, Moreira R, Chibale K, Guedes RC.

J Comput Aided Mol Des. 2013 Oct;27(10):859-71. doi: 10.1007/s10822-013-9685-z. Epub 2013 Oct 25.

PMID:
24158745
50.

Flavones as isosteres of 4(1H)-quinolones: discovery of ligand efficient and dual stage antimalarial lead compounds.

Rodrigues T, Ressurreição AS, da Cruz FP, Albuquerque IS, Gut J, Carrasco MP, Gonçalves D, Guedes RC, dos Santos DJ, Mota MM, Rosenthal PJ, Moreira R, Prudêncio M, Lopes F.

Eur J Med Chem. 2013 Nov;69:872-80. doi: 10.1016/j.ejmech.2013.09.008. Epub 2013 Sep 20.

PMID:
24125849

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