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1-Methyl-1H-pyrazole-5-carboxamide Derivatives Exhibit Unexpected Acute Mammalian Toxicity.
Preston S, Garcia-Bustos J, Hall LG, Martin SD, Le TG, Kundu A, Ghoshal A, Nguyen NH, Jiao Y, Ruan B, Xue L, Huang F, Chang BCH, McGee SL, Wells TNC, Palmer MJ, Jabbar A, Gasser RB, Baell JB. Preston S, et al. Among authors: palmer mj. J Med Chem. 2021 Jan 14;64(1):840-844. doi: 10.1021/acs.jmedchem.0c01793. Epub 2020 Dec 22. J Med Chem. 2021. PMID: 33352050
Optimization of Novel 1-Methyl-1 H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm.
Le TG, Kundu A, Ghoshal A, Nguyen NH, Preston S, Jiao Y, Ruan B, Xue L, Huang F, Keiser J, Hofmann A, Chang BCH, Garcia-Bustos J, Jabbar A, Wells TNC, Palmer MJ, Gasser RB, Baell JB. Le TG, et al. Among authors: palmer mj. J Med Chem. 2018 Dec 13;61(23):10875-10894. doi: 10.1021/acs.jmedchem.8b01544. Epub 2018 Nov 29. J Med Chem. 2018. PMID: 30403349
Structure-Activity Relationship Studies of Tolfenpyrad Reveal Subnanomolar Inhibitors of Haemonchus contortus Development.
Le TG, Kundu A, Ghoshal A, Nguyen NH, Preston S, Jiao Y, Ruan B, Xue L, Huang F, Keiser J, Hofmann A, Chang BCH, Garcia-Bustos J, Wells TNC, Palmer MJ, Jabbar A, Gasser RB, Baell JB. Le TG, et al. Among authors: palmer mj. J Med Chem. 2019 Jan 24;62(2):1036-1053. doi: 10.1021/acs.jmedchem.8b01789. Epub 2019 Jan 7. J Med Chem. 2019. PMID: 30571110
Novel 1-Methyl-1 H-pyrazole-5-carboxamide Derivatives with Potent Anthelmintic Activity.
Le TG, Kundu A, Ghoshal A, Nguyen NH, Preston S, Jiao Y, Ruan B, Xue L, Huang F, Keiser J, Hofmann A, Chang BCH, Garcia-Bustos J, Wells TNC, Palmer MJ, Jabbar A, Gasser RB, Baell JB. Le TG, et al. Among authors: palmer mj. J Med Chem. 2019 Apr 11;62(7):3367-3380. doi: 10.1021/acs.jmedchem.8b01790. Epub 2019 Mar 28. J Med Chem. 2019. PMID: 30875218
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J, Bath J, Schindler KA, Yeo T, Shackleford DM, Mok S, Deni I, Lawong A, Huang A, Chen G, Wang W, Jayaseelan J, Katneni K, Patil R, Saunders J, Shahi SP, Chittimalla R, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Tumwebaze PK, Rosenthal PJ, Cooper RA, Aguiar ACC, Guido RVC, Pereira DB, Mittal N, Winzeler EA, Tomchick DR, Laleu B, Burrows JN, Rathod PK, Fidock DA, Charman SA, Phillips MA. Palmer MJ, et al. J Med Chem. 2021 May 13;64(9):6085-6136. doi: 10.1021/acs.jmedchem.1c00173. Epub 2021 Apr 20. J Med Chem. 2021. PMID: 33876936 Free PMC article.
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA. Kokkonda S, et al. Among authors: palmer mj. J Med Chem. 2020 May 14;63(9):4929-4956. doi: 10.1021/acs.jmedchem.0c00311. Epub 2020 Apr 16. J Med Chem. 2020. PMID: 32248693 Free PMC article.
Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum.
Lawong A, Gahalawat S, Okombo J, Striepen J, Yeo T, Mok S, Deni I, Bridgford JL, Niederstrasser H, Zhou A, Posner B, Wittlin S, Gamo FJ, Crespo B, Churchyard A, Baum J, Mittal N, Winzeler E, Laleu B, Palmer MJ, Charman SA, Fidock DA, Ready JM, Phillips MA. Lawong A, et al. Among authors: palmer mj. J Med Chem. 2021 Mar 11;64(5):2739-2761. doi: 10.1021/acs.jmedchem.0c02022. Epub 2021 Feb 23. J Med Chem. 2021. PMID: 33620219 Free PMC article.
212 results