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Items: 9

1.

Design, synthesis and structure-activity relationship study of wollamide B; a new potential anti TB agent.

Asfaw H, Laqua K, Walkowska AM, Cunningham F, Martinez-Martinez MS, Cuevas-Zurita JC, Ballell-Pages L, Imming P.

PLoS One. 2017 Apr 19;12(4):e0176088. doi: 10.1371/journal.pone.0176088. eCollection 2017.

2.

N-Benzyl-4-((heteroaryl)methyl)benzamides: A New Class of Direct NADH-Dependent 2-trans Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity.

Guardia A, Gulten G, Fernandez R, Gómez J, Wang F, Convery M, Blanco D, Martínez M, Pérez-Herrán E, Alonso M, Ortega F, Rullás J, Calvo D, Mata L, Young R, Sacchettini JC, Mendoza-Losana A, Remuiñán M, Ballell Pages L, Castro-Pichel J.

ChemMedChem. 2016 Apr 5;11(7):687-701. doi: 10.1002/cmdc.201600020. Epub 2016 Mar 2.

PMID:
26934341
3.

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold.

Pajk S, Živec M, Šink R, Sosič I, Neu M, Chung CW, Martínez-Hoyos M, Pérez-Herrán E, Álvarez-Gómez D, Álvarez-Ruíz E, Mendoza-Losana A, Castro-Pichel J, Barros D, Ballell-Pages L, Young RJ, Convery MA, Encinas L, Gobec S.

Eur J Med Chem. 2016 Apr 13;112:252-257. doi: 10.1016/j.ejmech.2016.02.008. Epub 2016 Feb 8.

PMID:
26900657
4.

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
5.

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
6.

Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis.

Šink R, Sosič I, Živec M, Fernandez-Menendez R, Turk S, Pajk S, Alvarez-Gomez D, Lopez-Roman EM, Gonzales-Cortez C, Rullas-Triconado J, Angulo-Barturen I, Barros D, Ballell-Pages L, Young RJ, Encinas L, Gobec S.

J Med Chem. 2015 Jan 22;58(2):613-24. doi: 10.1021/jm501029r. Epub 2014 Dec 29.

PMID:
25517015
7.

Testing tuberculosis drug efficacy in a zebrafish high-throughput translational medicine screen.

Ordas A, Raterink RJ, Cunningham F, Jansen HJ, Wiweger MI, Jong-Raadsen S, Bos S, Bates RH, Barros D, Meijer AH, Vreeken RJ, Ballell-Pages L, Dirks RP, Hankemeier T, Spaink HP.

Antimicrob Agents Chemother. 2015 Feb;59(2):753-62. doi: 10.1128/AAC.03588-14. Epub 2014 Nov 10.

8.

High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis.

Silva-Miranda M, Ekaza E, Breiman A, Asehnoune K, Barros-Aguirre D, Pethe K, Ewann F, Brodin P, Ballell-Pages L, Altare F.

Antimicrob Agents Chemother. 2015 Jan;59(1):693-7. doi: 10.1128/AAC.03705-14. Epub 2014 Oct 27.

9.

Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.

Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G.

J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5.

PMID:
24450589

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