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Publikationer i urvalet

16 träffar

Bibliografisk träff 2024-07-14

Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3.

Calic PPS, Ashton TD, Mansouri M, Loi K, Jarman KE, Qiu D, Lehane AM, Roy S, Rao GP, Maity B, Wittlin S, Crespo B, Gamo FJ, Deni I, Fidock DA, Chowdury M, de Koning-Ward TF, Cowman AF, Jackson PF, Baud D, Brand S, Laleu B, Sleebs BE.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116677

Bibliografisk träff 2024-06-25

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy.

Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.4c01154

Bibliografisk träff 2024-03-25

Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein.

Nguyen W, Boulet C, Dans MG, Loi K, Jarman KE, Watson GM, Tham WH, Fairhurst KJ, Yeo T, Fidock DA, Wittlin S, Chowdury M, de Koning-Ward TF, Chen G, Yan D, Charman SA, Baud D, Brand S, Jackson PF, Cowman AF, Gilson PR, Sleebs BE.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116354

Bibliografisk träff 2023-05-20

Recent developments in antimalarial drug discovery.

Umumararungu T, Nkuranga JB, Habarurema G, Nyandwi JB, Mukazayire MJ, Mukiza J, Muganga R, Hahirwa I, Mpenda M, Katembezi AN, Olawode EO, Kayitare E, Kayumba PC.

Bioorg Med Chem · review; journal article · DOI 10.1016/j.bmc.2023.117339

Bibliografisk träff 2022-09-27

Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro.

Galal KA, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin ME, Merten E, Ong HW, Willis C, Abdelwaly A, Helal MA, Derbyshire ER, Zutshi R, Drewry DH.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.2c00996

Bibliografisk träff 2021-02-12

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.

Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/acs.jmedchem.1c00034

Bibliografisk träff 2020-10-25

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.

Horatscheck A, Andrijevic A, Nchinda AT, Le Manach C, Paquet T, Khonde LP, Dam J, Pawar K, Taylor D, Lawrence N, Brunschwig C, Gibhard L, Njoroge M, Reader J, van der Watt M, Wicht K, de Sousa ACC, Okombo J, Maepa K, Egan TJ, Birkholtz LM, Basarab GS, Wittlin S, Fish PV, Street LJ, Duffy J, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c01411

Bibliografisk träff 2020-10-22

An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.

Madhav H, Hoda N.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.112955

Bibliografisk träff 2019-08-20

The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.

Ashton TD, Devine SM, Möhrle JJ, Laleu B, Burrows JN, Charman SA, Creek DJ, Sleebs BE.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.9b00761

Bibliografisk träff 2018-06-27

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b00648

Bibliografisk träff 2018-06-04

Plasmodial Kinase Inhibitors: License to Cure?

Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; review-article; journal article · DOI 10.1021/acs.jmedchem.8b00329

Bibliografisk träff 2018-04-27

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b00382

Bibliografisk träff 2017-02-07

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K, Chibale K.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b01641

Bibliografisk träff 2013-12-31

Quinoline-pyrimidine hybrids: synthesis, antiplasmodial activity, SAR, and mode of action studies.

Singh K, Kaur H, Smith P, de Kock C, Chibale K, Balzarini J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm4014778

Bibliografisk träff 2013-06-10

Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.

Singh K, Kaur H, Chibale K, Balzarini J.

Eur J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.ejmech.2013.05.046

Bibliografisk träff 2012-03-21

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.

Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Hardick D, Wittlin S, Avery V, Charman SA, Chibale K.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm3001373

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Publikationer i urvalet

Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3.

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of <i>Plasmodium falciparum</i> Phosphatidylinositol-4-kinase and Hemozoin Formation with <i>In Vivo</i> Efficacy.

Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein.

Recent developments in antimalarial drug discovery.

Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial <i>Pf</i>GSK3/<i>Pf</i>PK6 with Activity against Blood Stage Parasites In Vitro.

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite <i>Plasmodium falciparum</i> and Optimization Efforts.

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and <i>In Vivo</i> Efficacy in the <i>Plasmodium falciparum</i> NSG Mouse Model.

An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.

The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

Plasmodial Kinase Inhibitors: License to Cure?

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ <sup>null</sup> Mouse Model of Malaria.

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Quinoline-pyrimidine hybrids: synthesis, antiplasmodial activity, SAR, and mode of action studies.

Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.