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Items: 29

1.

Substituted Aminoacetamides as Novel Leads for Malaria Treatment.

Norcross NR, Wilson C, Baragaña B, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Fletcher D, Sinden R, Delves M, Ruecker A, Duffy S, Meister S, Antonova-Koch Y, Crespo B, de Cózar C, Sanz LM, Gamo FJ, Avery VM, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis PA, Read KD, Gilbert IH.

ChemMedChem. 2019 Jul 17;14(14):1329-1335. doi: 10.1002/cmdc.201900329. Epub 2019 Jul 3.

PMID:
31188540
2.

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.

Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20.

3.

Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing N-Methyl Amino Acids as Antiplasmodial Agents.

Fagundez C, Sellanes D, Peña S, Scarone L, Aguiar ACC, de Souza JO, Guido RVC, Stewart L, Yardley V, Ottilie S, Winzeler EA, Gamo FJ, Sanz LM, Serra GL.

ACS Med Chem Lett. 2018 Dec 26;10(1):137-141. doi: 10.1021/acsmedchemlett.8b00543. eCollection 2019 Jan 10.

PMID:
30655961
4.

Overexpression of plasmepsin II and plasmepsin III does not directly cause reduction in Plasmodium falciparum sensitivity to artesunate, chloroquine and piperaquine.

Loesbanluechai D, Kotanan N, de Cozar C, Kochakarn T, Ansbro MR, Chotivanich K, White NJ, Wilairat P, Lee MCS, Gamo FJ, Sanz LM, Chookajorn T, Kümpornsin K.

Int J Parasitol Drugs Drug Resist. 2019 Apr;9:16-22. doi: 10.1016/j.ijpddr.2018.11.004. Epub 2018 Dec 1.

5.

Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria.

Gilson PR, Nguyen W, Poole WA, Teixeira JE, Thompson JK, Guo K, Stewart RJ, Ashton TD, White KL, Sanz LM, Gamo FJ, Charman SA, Wittlin S, Duffy J, Tonkin CJ, Tham WH, Crabb BS, Cooke BM, Huston CD, Cowman AF, Sleebs BE.

Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e01804-18. doi: 10.1128/AAC.01804-18. Print 2019 Mar.

PMID:
30559138
6.

A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.

Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS, Coombs PJ, Whalley D, Harding DJ, Smiljanic-Hurley E, Wheldon MC, Walker EM, Dessens JT, Lafuente MJ, Sanz LM, Gamo FJ, Ferrer SB, Hui R, Bousema T, Angulo-Barturén I, Merritt AT, Croft SL, Gutteridge WE, Kettleborough CA, Osborne SA.

Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x.

7.

Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate.

Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Freund YR, Berry P, Ciaravino V, Erve JCL, Rosenthal PJ, Campo B, Gamo FJ, Sanz LM, Cao J.

J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29.

PMID:
28635296
8.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

9.

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.

10.

Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito FJ, Gnädig NF, Heidmann B, Jiménez-Díaz MB, Leroy D, Martínez MS, Meyer S, Moehrle JJ, Ng CL, Noviyanti R, Ruecker A, Sanz LM, Sauerwein RW, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price RN, Weller T, Fischli W, Fidock DA, Clozel M, Wittlin S.

PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct.

11.

Development of a Novel High-Density [3H]Hypoxanthine Scintillation Proximity Assay To Assess Plasmodium falciparum Growth.

de Cózar C, Caballero I, Colmenarejo G, Sanz LM, Álvarez-Ruiz E, Gamo FJ, Cid C.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):5949-56. doi: 10.1128/AAC.00433-16. Print 2016 Oct.

12.

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

13.

Identifying rapidly parasiticidal anti-malarial drugs using a simple and reliable in vitro parasite viability fast assay.

Linares M, Viera S, Crespo B, Franco V, Gómez-Lorenzo MG, Jiménez-Díaz MB, Angulo-Barturen Í, Sanz LM, Gamo FJ.

Malar J. 2015 Nov 5;14:441. doi: 10.1186/s12936-015-0962-2.

14.

Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.

McConville M, Fernández J, Angulo-Barturen Í, Bahamontes-Rosa N, Ballell-Pages L, Castañeda P, de Cózar C, Crespo B, Guijarro L, Jiménez-Díaz MB, Martínez-Martínez MS, de Mercado J, Santos-Villarejo Á, Sanz LM, Frigerio M, Washbourn G, Ward SA, Nixon GL, Biagini GA, Berry NG, Blackman MJ, Calderón F, O'Neill PM.

J Med Chem. 2015 Aug 27;58(16):6448-55. doi: 10.1021/acs.jmedchem.5b00434. Epub 2015 Aug 17.

PMID:
26222445
15.

A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122.

16.

Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Sanders V, Freund YR, Campo B, Rosenthal PJ, Bu W, Gamo FJ, Sanz LM, Ge M, Li L, Ding J, Yang Y.

J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23.

17.

A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.

Keurulainen L, Vahermo M, Puente-Felipe M, Sandoval-Izquierdo E, Crespo-Fernández B, Guijarro-López L, Huertas-Valentín L, de las Heras-Dueña L, Leino TO, Siiskonen A, Ballell-Pages L, Sanz LM, Castañeda-Casado P, Jiménez-Díaz MB, Martínez-Martínez MS, Viera S, Kiuru P, Calderón F, Yli-Kauhaluoma J.

J Med Chem. 2015 Jun 11;58(11):4573-80. doi: 10.1021/acs.jmedchem.5b00114. Epub 2015 May 19.

PMID:
25906200
18.

Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate.

Hameed P S, Solapure S, Patil V, Henrich PP, Magistrado PA, Bharath S, Murugan K, Viswanath P, Puttur J, Srivastava A, Bellale E, Panduga V, Shanbag G, Awasthy D, Landge S, Morayya S, Koushik K, Saralaya R, Raichurkar A, Rautela N, Roy Choudhury N, Ambady A, Nandishaiah R, Reddy J, Prabhakar KR, Menasinakai S, Rudrapatna S, Chatterji M, Jiménez-Díaz MB, Martínez MS, Sanz LM, Coburn-Flynn O, Fidock DA, Lukens AK, Wirth DF, Bandodkar B, Mukherjee K, McLaughlin RE, Waterson D, Rosenbrier-Ribeiro L, Hickling K, Balasubramanian V, Warner P, Hosagrahara V, Dudley A, Iyer PS, Narayanan S, Kavanagh S, Sambandamurthy VK.

Nat Commun. 2015 Mar 31;6:6715. doi: 10.1038/ncomms7715.

19.

Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans.

Malmquist NA, Sundriyal S, Caron J, Chen P, Witkowski B, Menard D, Suwanarusk R, Renia L, Nosten F, Jiménez-Díaz MB, Angulo-Barturen I, Santos Martínez M, Ferrer S, Sanz LM, Gamo FJ, Wittlin S, Duffy S, Avery VM, Ruecker A, Delves MJ, Sinden RE, Fuchter MJ, Scherf A.

Antimicrob Agents Chemother. 2015 Feb;59(2):950-9. doi: 10.1128/AAC.04419-14. Epub 2014 Nov 24.

20.

N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds.

Ramachandran S, Hameed P S, Srivastava A, Shanbhag G, Morayya S, Rautela N, Awasthy D, Kavanagh S, Bharath S, Reddy J, Panduga V, Prabhakar KR, Saralaya R, Nanduri R, Raichurkar A, Menasinakai S, Achar V, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Waterson D, Lee MC, Coburn-Flynn O, Fidock DA, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK.

J Med Chem. 2014 Aug 14;57(15):6642-52. doi: 10.1021/jm500715u. Epub 2014 Jul 21.

PMID:
25007124
21.

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.

Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S.

J Med Chem. 2014 Jul 10;57(13):5702-13. doi: 10.1021/jm500535j. Epub 2014 Jun 24.

PMID:
24914738
22.

Quinolone-3-diarylethers: a new class of antimalarial drug.

Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK.

Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029.

23.

P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.

Sanz LM, Crespo B, De-Cózar C, Ding XC, Llergo JL, Burrows JN, García-Bustos JF, Gamo FJ.

PLoS One. 2012;7(2):e30949. doi: 10.1371/journal.pone.0030949. Epub 2012 Feb 23.

24.

Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Ye L, Zhou H, Waterson D, Gamo FJ, Sanz LM, Ge M, Li Z, Li L, Wang H, Cui H.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1299-307. doi: 10.1016/j.bmcl.2011.12.096. Epub 2011 Dec 28.

PMID:
22243961
25.

Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).

Rueda L, Castellote I, Castro-Pichel J, Chaparro MJ, de la Rosa JC, Garcia-Perez A, Gordo M, Jimenez-Diaz MB, Kessler A, Macdonald SJ, Martinez MS, Sanz LM, Gamo FJ, Fernandez E.

ACS Med Chem Lett. 2011 Aug 29;2(11):840-4. doi: 10.1021/ml2001517. eCollection 2011 Nov 10.

26.

Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screen.

Sanz LM, Jiménez-Díaz MB, Crespo B, De-Cozar C, Almela MJ, Angulo-Barturen I, Castañeda P, Ibañez J, Fernández EP, Ferrer S, Herreros E, Lozano S, Martínez MS, Rueda L, Burrows JN, García-Bustos JF, Gamo FJ.

Antimicrob Agents Chemother. 2011 Dec;55(12):5740-5. doi: 10.1128/AAC.05188-11. Epub 2011 Oct 3.

27.

Thousands of chemical starting points for antimalarial lead identification.

Gamo FJ, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera JL, Vanderwall DE, Green DV, Kumar V, Hasan S, Brown JR, Peishoff CE, Cardon LR, Garcia-Bustos JF.

Nature. 2010 May 20;465(7296):305-10. doi: 10.1038/nature09107.

PMID:
20485427
28.

A polymorphic microsatellite located on pig chromosome band 12p11-2/3p13, within the 3'-UTR of the ITGB3 gene.

Sanz LM, Jiménez-Marín A, Yerle M, Llanes D, Barbancho MJ, Pavón JJ.

Anim Genet. 2002 Jun;33(3):239-40. No abstract available.

PMID:
12030937
29.

Diamidinas aromáticas en el tratamiento de ciertas parasitosis.

SANZ LM, AZAGRA ER.

Med Colon. 1946 Jul 1;8(1):51-7. Undetermined Language. No abstract available.

PMID:
20992275

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