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Page 1
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.
Soares de Melo C, Singh V, Myrick A, Simelane SB, Taylor D, Brunschwig C, Lawrence N, Schnappinger D, Engelhart CA, Kumar A, Parish T, Su Q, Myers TG, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden PD, Buchanan KI, Bayliss T, Green SR, Ray PC, Wyatt PG, Basarab GS, Eyermann CJ, Chibale K, Ghorpade SR. Soares de Melo C, et al. Among authors: brunschwig c. J Med Chem. 2021 Jan 14;64(1):719-740. doi: 10.1021/acs.jmedchem.0c01727. Epub 2021 Jan 4. J Med Chem. 2021. PMID: 33395287 Free PMC article.
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
van der Westhuyzen R, Winks S, Wilson CR, Boyle GA, Gessner RK, Soares de Melo C, Taylor D, de Kock C, Njoroge M, Brunschwig C, Lawrence N, Rao SP, Sirgel F, van Helden P, Seldon R, Moosa A, Warner DF, Arista L, Manjunatha UH, Smith PW, Street LJ, Chibale K. van der Westhuyzen R, et al. Among authors: brunschwig c. J Med Chem. 2015 Dec 10;58(23):9371-81. doi: 10.1021/acs.jmedchem.5b01542. Epub 2015 Nov 20. J Med Chem. 2015. PMID: 26551248
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K. Wilson CR, et al. Among authors: brunschwig c. J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7. J Med Chem. 2017. PMID: 29148755 Free PMC article.
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. Kandepedu N, et al. Among authors: brunschwig c. J Med Chem. 2018 Jul 12;61(13):5692-5703. doi: 10.1021/acs.jmedchem.8b00648. Epub 2018 Jun 27. J Med Chem. 2018. PMID: 29889526
Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.
Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K. Le Manach C, et al. Among authors: brunschwig c. J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16. J Med Chem. 2018. PMID: 30256636
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: brunschwig c. 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.
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. Le Manach C, et al. Among authors: brunschwig c. J Med Chem. 2021 Feb 25;64(4):2291-2309. doi: 10.1021/acs.jmedchem.1c00034. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33573376
Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure-Activity Relationship, Metabolism, and Biology Triaging.
van der Westhuyzen R, Mabhula A, Njaria PM, Müller R, Ngumbu Muhunga D, Taylor D, Lawrence N, Njoroge M, Brunschwig C, Moosa A, Singh V, Rao SPS, Manjunatha UH, Smith PW, Warner DF, Street LJ, Chibale K. van der Westhuyzen R, et al. Among authors: brunschwig c. J Med Chem. 2021 Jul 8;64(13):9444-9457. doi: 10.1021/acs.jmedchem.1c00707. Epub 2021 Jun 17. J Med Chem. 2021. PMID: 34138573
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: brunschwig c. 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 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. Nchinda AT, et al. Among authors: brunschwig c. J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27. J Med Chem. 2018. PMID: 29665687
44 results