Pesquisa | BVS Integralidade em Saúde

1.

Veterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs.

Giordani, Federica; Paape, Daniel; Vincent, Isabel M; Pountain, Andrew W; Fernández-Cortés, Fernando; Rico, Eva; Zhang, Ning; Morrison, Liam J; Freund, Yvonne; Witty, Michael J; Peter, Rosemary; Edwards, Darren Y; Wilkes, Jonathan M; van der Hooft, Justin J J; Regnault, Clément; Read, Kevin D; Horn, David; Field, Mark C; Barrett, Michael P.

PLoS Pathog ; 16(11): e1008932, 2020 11.

Artigo em Inglês | MEDLINE | ID: mdl-33141865

2.

The trypanocidal benzoxaborole AN7973 inhibits trypanosome mRNA processing.

Begolo, Daniela; Vincent, Isabel M; Giordani, Federica; Pöhner, Ina; Witty, Michael J; Rowan, Timothy G; Bengaly, Zakaria; Gillingwater, Kirsten; Freund, Yvonne; Wade, Rebecca C; Barrett, Michael P; Clayton, Christine.

PLoS Pathog ; 14(9): e1007315, 2018 09.

Artigo em Inglês | MEDLINE | ID: mdl-30252911

3.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig, Christel; Lawrence, Nina; Taylor, Dale; Abay, Efrem; Njoroge, Mathew; Basarab, Gregory S; Le Manach, Claire; Paquet, Tanya; Cabrera, Diego Gonzàlez; Nchinda, Aloysius T; de Kock, Carmen; Wiesner, Lubbe; Denti, Paolo; Waterson, David; Blasco, Benjamin; Leroy, Didier; Witty, Michael J; Donini, Cristina; Duffy, James; Wittlin, Sergio; White, Karen L; Charman, Susan A; Jiménez-Díaz, Maria Belén; Angulo-Barturen, Iñigo; Herreros, Esperanza; Gamo, Francisco Javier; Rochford, Rosemary; Mancama, Dalu; Coetzer, Theresa L; van der Watt, Mariëtte E; Reader, Janette; Birkholtz, Lyn-Marie; Marsh, Kennan C; Solapure, Suresh M; Burke, John E; McPhail, Jacob A; Vanaerschot, Manu; Fidock, David A; Fish, Paul V; Siegl, Peter; Smith, Dennis A; Wirjanata, Grennady; Noviyanti, Rintis; Price, Ric N; Marfurt, Jutta; Silue, Kigbafori D; Street, Leslie J; Chibale, Kelly.

Antimicrob Agents Chemother ; 62(9)2018 09.

Artigo em Inglês | MEDLINE | ID: mdl-29941635

4.

Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT).

Akama, Tsutomu; Zhang, Yong-Kang; Freund, Yvonne R; Berry, Pamela; Lee, Joanne; Easom, Eric E; Jacobs, Robert T; Plattner, Jacob J; Witty, Michael J; Peter, Rosemary; Rowan, Tim G; Gillingwater, Kirsten; Brun, Reto; Nare, Bakela; Mercer, Luke; Xu, Musheng; Wang, Jiangong; Liang, Hao.

Bioorg Med Chem Lett ; 28(1): 6-10, 2018 01 01.

Artigo em Inglês | MEDLINE | ID: mdl-29169674

5.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig, Christel; Lawrence, Nina; Taylor, Dale; Abay, Efrem; Njoroge, Mathew; Basarab, Gregory S; Le Manach, Claire; Paquet, Tanya; Gonzàlez Cabrera, Diego; Nchinda, Aloysius T; de Kock, Carmen; Wiesner, Lubbe; Denti, Paolo; Waterson, David; Blasco, Benjamin; Leroy, Didier; Witty, Michael J; Donini, Cristina; Duffy, James; Wittlin, Sergio; White, Karen L; Charman, Susan A; Jiménez-Díaz, Maria Belén; Angulo-Barturen, Iñigo; Herreros, Esperanza; Gamo, Francisco Javier; Rochford, Rosemary; Mancama, Dalu; Coetzer, Theresa L; van der Watt, Mariëtte E; Reader, Janette; Birkholtz, Lyn-Marie; Marsh, Kennan C; Solapure, Suresh M; Burke, John E; McPhail, Jacob A; Vanaerschot, Manu; Fidock, David A; Fish, Paul V; Siegl, Peter; Smith, Dennis A; Wirjanata, Grennady; Noviyanti, Rintis; Price, Ric N; Marfurt, Jutta; Silue, Kigbafori D; Street, Leslie J; Chibale, Kelly.

Antimicrob Agents Chemother ; 62(11)2018 11.

Artigo em Inglês | MEDLINE | ID: mdl-30355750

6.

Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum.

Le Manach, Claire; Scheurer, Christian; Sax, Sibylle; Schleiferböck, Sarah; Cabrera, Diego Gonzalez; Younis, Yassir; Paquet, Tanya; Street, Leslie; Smith, Peter; Ding, Xavier C; Waterson, David; Witty, Michael J; Leroy, Didier; Chibale, Kelly; Wittlin, Sergio.

Malar J ; 12: 424, 2013 Nov 16.

Artigo em Inglês | MEDLINE | ID: mdl-24237770

7.

Repositioning of a Diaminothiazole Series Confirmed to Target the Cyclin-Dependent Kinase CRK12 for Use in the Treatment of African Animal Trypanosomiasis.

Smith, Alasdair; Wall, Richard J; Patterson, Stephen; Rowan, Tim; Rico Vidal, Eva; Stojanovski, Laste; Huggett, Margaret; Hampton, Shahienaz E; Thomas, Michael G; Corpas Lopez, Victoriano; Gillingwater, Kirsten; Duke, Jeff; Napier, Grant; Peter, Rose; Vitouley, Hervé S; Harrison, Justin R; Milne, Rachel; Jeacock, Laura; Baker, Nicola; Davis, Susan H; Simeons, Frederick; Riley, Jennifer; Horn, David; Brun, Reto; Zuccotto, Fabio; Witty, Michael J; Wyllie, Susan; Read, Kevin D; Gilbert, Ian H.

J Med Chem ; 65(7): 5606-5624, 2022 04 14.

Artigo em Inglês | MEDLINE | ID: mdl-35303411

8.

Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity.

Musonda, Chitalu C; Whitlock, Gavin A; Witty, Michael J; Brun, Reto; Kaiser, Marcel.

Bioorg Med Chem Lett ; 19(2): 401-5, 2009 Jan 15.

Artigo em Inglês | MEDLINE | ID: mdl-19091562

9.

Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.

Musonda, Chitalu C; Whitlock, Gavin A; Witty, Michael J; Brun, Reto; Kaiser, Marcel.

Bioorg Med Chem Lett ; 19(2): 481-4, 2009 Jan 15.

Artigo em Inglês | MEDLINE | ID: mdl-19054674

10.

Mission possible.

Hopkins, Andrew L; Witty, Michael J; Nwaka, Solomon.

Nature ; 449(7159): 166-9, 2007 Sep 13.

Artigo em Inglês | MEDLINE | ID: mdl-17851512

11.

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

Paquet, Tanya; Le Manach, Claire; Cabrera, Diego González; Younis, Yassir; Henrich, Philipp P; Abraham, Tara S; Lee, Marcus C S; Basak, Rajshekhar; Ghidelli-Disse, Sonja; Lafuente-Monasterio, María José; Bantscheff, Marcus; Ruecker, Andrea; Blagborough, Andrew M; Zakutansky, Sara E; Zeeman, Anne-Marie; White, Karen L; Shackleford, David M; Mannila, Janne; Morizzi, Julia; Scheurer, Christian; Angulo-Barturen, Iñigo; Martínez, María Santos; Ferrer, Santiago; Sanz, Laura María; Gamo, Francisco Javier; Reader, Janette; Botha, Mariette; Dechering, Koen J; Sauerwein, Robert W; Tungtaeng, Anchalee; Vanachayangkul, Pattaraporn; Lim, Chek Shik; Burrows, Jeremy; Witty, Michael J; Marsh, Kennan C; Bodenreider, Christophe; Rochford, Rosemary; Solapure, Suresh M; Jiménez-Díaz, María Belén; Wittlin, Sergio; Charman, Susan A; Donini, Cristina; Campo, Brice; Birkholtz, Lyn-Marie; Hanson, Kirsten K; Drewes, Gerard; Kocken, Clemens H M; Delves, Michael J; Leroy, Didier; Fidock, David A.

Sci Transl Med ; 9(387)2017 04 26.

Artigo em Inglês | MEDLINE | ID: mdl-28446690

12.

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

Le Manach, Claire; Nchinda, Aloysius T; Paquet, Tanya; Gonzàlez Cabrera, Diego; Younis, Yassir; Han, Ze; Bashyam, Sridevi; Zabiulla, Mohammed; Taylor, Dale; Lawrence, Nina; White, Karen L; Charman, Susan A; Waterson, David; Witty, Michael J; Wittlin, Sergio; Botha, Mariëtte E; Nondaba, Sindisiswe H; Reader, Janette; Birkholtz, Lyn-Marie; Jiménez-Díaz, María Belén; Martínez, María Santos; Ferrer, Santiago; Angulo-Barturen, Iñigo; Meister, Stephan; Antonova-Koch, Yevgeniya; Winzeler, Elizabeth A; Street, Leslie J; Chibale, Kelly.

J Med Chem ; 59(21): 9890-9905, 2016 11 10.

Artigo em Inglês | MEDLINE | ID: mdl-27748596

13.

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

Gonzàlez Cabrera, Diego; Douelle, Frederic; Le Manach, Claire; Han, Ze; Paquet, Tanya; Taylor, Dale; Njoroge, Mathew; Lawrence, Nina; Wiesner, Lubbe; Waterson, David; Witty, Michael J; Wittlin, Sergio; Street, Leslie J; Chibale, Kelly.

J Med Chem ; 58(18): 7572-9, 2015 Sep 24.

Artigo em Inglês | MEDLINE | ID: mdl-26322748

14.

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

Le Manach, Claire; Paquet, Tanya; Brunschwig, Christel; Njoroge, Mathew; Han, Ze; Gonzàlez Cabrera, Diego; Bashyam, Sridevi; Dhinakaran, Rajkumar; Taylor, Dale; Reader, Janette; Botha, Mariette; Churchyard, Alisje; Lauterbach, Sonja; Coetzer, Theresa L; Birkholtz, Lyn-Marie; Meister, Stephan; Winzeler, Elizabeth A; Waterson, David; Witty, Michael J; Wittlin, Sergio; Jiménez-Díaz, María-Belén; Santos Martínez, María; Ferrer, Santiago; Angulo-Barturen, Iñigo; Street, Leslie J; Chibale, Kelly.

J Med Chem ; 58(21): 8713-22, 2015 Nov 12.

Artigo em Inglês | MEDLINE | ID: mdl-26502160

15.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

Le Manach, Claire; Paquet, Tanya; Gonzàlez Cabrera, Diego; Younis, Yassir; Taylor, Dale; Wiesner, Lubbe; Lawrence, Nina; Schwager, Sylva; Waterson, David; Witty, Michael J; Wittlin, Sergio; Street, Leslie J; Chibale, Kelly.

J Med Chem ; 57(21): 8839-48, 2014 Nov 13.

Artigo em Inglês | MEDLINE | ID: mdl-25313449

16.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

Le Manach, Claire; Gonzàlez Cabrera, Diego; Douelle, Frederic; Nchinda, Aloysius T; Younis, Yassir; Taylor, Dale; Wiesner, Lubbe; White, Karen L; Ryan, Eileen; March, Corinne; Duffy, Sandra; Avery, Vicky M; Waterson, David; Witty, Michael J; Wittlin, Sergio; Charman, Susan A; Street, Leslie J; Chibale, Kelly.

J Med Chem ; 57(6): 2789-98, 2014 Mar 27.

Artigo em Inglês | MEDLINE | ID: mdl-24568587

17.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

González Cabrera, Diego; Le Manach, Claire; Douelle, Frederic; Younis, Yassir; Feng, Tzu-Shean; Paquet, Tanya; Nchinda, Aloysius T; Street, Leslie J; Taylor, Dale; de Kock, Carmen; Wiesner, Lubbe; Duffy, Sandra; White, Karen L; Zabiulla, K Mohammed; Sambandan, Yuvaraj; Bashyam, Sridevi; Waterson, David; Witty, Michael J; Charman, Susan A; Avery, Vicky M; Wittlin, Sergio; Chibale, Kelly.

J Med Chem ; 57(3): 1014-22, 2014 Feb 13.

Artigo em Inglês | MEDLINE | ID: mdl-24446664

18.

Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries.

Younis, Yassir; Street, Leslie J; Waterson, David; Witty, Michael J; Chibale, Kelly.

J Med Chem ; 56(20): 7750-4, 2013 Oct 24.

Artigo em Inglês | MEDLINE | ID: mdl-23927599

19.

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.

Younis, Yassir; Douelle, Frederic; González Cabrera, Diego; Le Manach, Claire; Nchinda, Aloysius T; Paquet, Tanya; Street, Leslie J; White, Karen L; Zabiulla, K Mohammed; Joseph, Jayan T; Bashyam, Sridevi; Waterson, David; Witty, Michael J; Wittlin, Sergio; Charman, Susan A; Chibale, Kelly.

J Med Chem ; 56(21): 8860-71, 2013 Nov 14.

Artigo em Inglês | MEDLINE | ID: mdl-24099149

20.

Antimalarial aminothiazoles and aminopyridines from phenotypic whole-cell screening of a SoftFocus(®) library.

Paquet, Tanya; Gordon, Richard; Waterson, David; Witty, Michael J; Chibale, Kelly.

Future Med Chem ; 4(18): 2265-77, 2012 Dec.

Artigo em Inglês | MEDLINE | ID: mdl-23234550

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