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Page 1
Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites.
Verlinden BK, de Beer M, Pachaiyappan B, Besaans E, Andayi WA, Reader J, Niemand J, van Biljon R, Guy K, Egan T, Woster PM, Birkholtz LM. Verlinden BK, et al. Among authors: birkholtz lm. Bioorg Med Chem. 2015 Aug 15;23(16):5131-43. doi: 10.1016/j.bmc.2015.01.036. Epub 2015 Jan 28. Bioorg Med Chem. 2015. PMID: 25684422 Free PMC article.
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. Singh K, et al. Among authors: birkholtz lm. J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7. J Med Chem. 2017. PMID: 28094524
Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria.
Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates C, Wittlin S, Prudêncio M, Chibale K. Mayoka G, et al. Among authors: birkholtz lm. J Med Chem. 2019 Jan 24;62(2):1022-1035. doi: 10.1021/acs.jmedchem.8b01769. Epub 2018 Dec 24. J Med Chem. 2019. PMID: 30562027
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. Horatscheck A, et al. Among authors: birkholtz lm. J Med Chem. 2020 Nov 12;63(21):13013-13030. doi: 10.1021/acs.jmedchem.0c01411. Epub 2020 Oct 25. J Med Chem. 2020. PMID: 33103428 Free PMC article.
Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies.
Dziwornu GA, Coertzen D, Leshabane M, Korkor CM, Cloete CK, Njoroge M, Gibhard L, Lawrence N, Reader J, van der Watt M, Wittlin S, Birkholtz LM, Chibale K. Dziwornu GA, et al. Among authors: birkholtz lm. J Med Chem. 2021 Apr 22;64(8):5198-5215. doi: 10.1021/acs.jmedchem.1c00354. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844521
Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model.
Mambwe D, Korkor CM, Mabhula A, Ngqumba Z, Cloete C, Kumar M, Barros PL, Leshabane M, Coertzen D, Taylor D, Gibhard L, Njoroge M, Lawrence N, Reader J, Moreira DR, Birkholtz LM, Wittlin S, Egan TJ, Chibale K. Mambwe D, et al. Among authors: birkholtz lm. J Med Chem. 2022 Dec 22;65(24):16695-16715. doi: 10.1021/acs.jmedchem.2c01516. Epub 2022 Dec 12. J Med Chem. 2022. PMID: 36507890
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 C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K. Le Manach C, et al. Among authors: birkholtz lm. J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2. J Med Chem. 2015. PMID: 26502160
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 C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K. Le Manach C, et al. Among authors: birkholtz lm. J Med Chem. 2016 Nov 10;59(21):9890-9905. doi: 10.1021/acs.jmedchem.6b01265. Epub 2016 Oct 26. J Med Chem. 2016. PMID: 27748596
101 results