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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: basarab gs. 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.
Plasmodial Kinase Inhibitors: License to Cure?
Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K. Cabrera DG, et al. J Med Chem. 2018 Sep 27;61(18):8061-8077. doi: 10.1021/acs.jmedchem.8b00329. Epub 2018 Jun 4. J Med Chem. 2018. PMID: 29771541 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: basarab gs. 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
UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.
Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K. Brunschwig C, et al. Among authors: basarab gs. Antimicrob Agents Chemother. 2018 Aug 27;62(9):e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Antimicrob Agents Chemother. 2018. PMID: 29941635 Free PMC article.
Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.
Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS. Gibhard L, et al. Among authors: basarab gs. Antimicrob Agents Chemother. 2018 Nov 26;62(12):e00261-18. doi: 10.1128/AAC.00261-18. Print 2018 Dec. Antimicrob Agents Chemother. 2018. PMID: 30249687 Free PMC article.
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: basarab gs. 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
Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".
Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K. Brunschwig C, et al. Among authors: basarab gs. Antimicrob Agents Chemother. 2018 Oct 24;62(11):e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. Antimicrob Agents Chemother. 2018. PMID: 30355750 Free PMC article. No abstract available.
60 results