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Page 1
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: chiu fck. 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.
A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.
Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Shackleford DM, Chiu FC, Campbell M, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Martinez MS, Lafuente-Monasterio M, Kaminsky W, Silue K, Zeeman AM, Kocken C, Leroy D, Blasco B, Rossignol E, Rueckle T, Matthews D, Burrows JN, Waterson D, Palmer MJ, Rathod PK, Charman SA. Phillips MA, et al. ACS Infect Dis. 2016 Dec 9;2(12):945-957. doi: 10.1021/acsinfecdis.6b00144. Epub 2016 Oct 4. ACS Infect Dis. 2016. PMID: 27641613 Free PMC article.
Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).
Wang C, Zhao Q, Vargas M, Jones JO, White KL, Shackleford DM, Chen G, Saunders J, Ng AC, Chiu FC, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wang C, et al. J Med Chem. 2016 Dec 8;59(23):10705-10718. doi: 10.1021/acs.jmedchem.6b01410. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933964 Free PMC article.
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL. Dong Y, et al. J Med Chem. 2017 Apr 13;60(7):2654-2668. doi: 10.1021/acs.jmedchem.6b01586. Epub 2017 Jan 18. J Med Chem. 2017. PMID: 28052200
Structure-Activity Relationship of Antischistosomal Ozonide Carboxylic Acids.
Wu J, Wang X, Chiu FCK, Häberli C, Shackleford DM, Ryan E, Kamaraj S, Bulbule VJ, Wallick AI, Dong Y, White KL, Davis PH, Charman SA, Keiser J, Vennerstrom JL. Wu J, et al. Among authors: chiu fck. J Med Chem. 2020 Apr 9;63(7):3723-3736. doi: 10.1021/acs.jmedchem.0c00069. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32134263 Free PMC article.
Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials.
Laleu B, Akao Y, Ochida A, Duffy S, Lucantoni L, Shackleford DM, Chen G, Katneni K, Chiu FCK, White KL, Chen X, Sturm A, Dechering KJ, Crespo B, Sanz LM, Wang B, Wittlin S, Charman SA, Avery VM, Cho N, Kamaura M. Laleu B, et al. Among authors: chiu fck. J Med Chem. 2021 Sep 9;64(17):12582-12602. doi: 10.1021/acs.jmedchem.1c00441. Epub 2021 Aug 26. J Med Chem. 2021. PMID: 34437804 Free article.
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
Wang X, Dong Y, Wittlin S, Charman SA, Chiu FC, Chollet J, Katneni K, Mannila J, Morizzi J, Ryan E, Scheurer C, Steuten J, Santo Tomas J, Snyder C, Vennerstrom JL. Wang X, et al. J Med Chem. 2013 Mar 28;56(6):2547-55. doi: 10.1021/jm400004u. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23489135
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA. Keenan M, et al. J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24304150 Free PMC article.
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
Xue L, Shi DH, Harjani JR, Huang F, Beveridge JG, Dingjan T, Ban K, Diab S, Duffy S, Lucantoni L, Fletcher S, Chiu FCK, Blundell S, Ellis K, Ralph SA, Wirjanata G, Teguh S, Noviyanti R, Chavchich M, Creek D, Price RN, Marfurt J, Charman SA, Cuellar ME, Strasser JM, Dahlin JL, Walters MA, Edstein MD, Avery VM, Baell JB. Xue L, et al. Among authors: chiu fck. J Med Chem. 2019 Mar 14;62(5):2485-2498. doi: 10.1021/acs.jmedchem.8b01799. Epub 2019 Mar 5. J Med Chem. 2019. PMID: 30715882
An in vitro toolbox to accelerate anti-malarial drug discovery and development.
Charman SA, Andreu A, Barker H, Blundell S, Campbell A, Campbell M, Chen G, Chiu FCK, Crighton E, Katneni K, Morizzi J, Patil R, Pham T, Ryan E, Saunders J, Shackleford DM, White KL, Almond L, Dickins M, Smith DA, Moehrle JJ, Burrows JN, Abla N. Charman SA, et al. Among authors: chiu fck. Malar J. 2020 Jan 2;19(1):1. doi: 10.1186/s12936-019-3075-5. Malar J. 2020. PMID: 31898492 Free PMC article.
41 results