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Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.
Dandapani S, Germain AR, Jewett I, le Quement S, Marie JC, Muncipinto G, Duvall JR, Carmody LC, Perez JR, Engel JC, Gut J, Kellar D, Siqueira-Neto JL, McKerrow JH, Kaiser M, Rodriguez A, Palmer MA, Foley M, Schreiber SL, Munoz B. Dandapani S, et al. Among authors: rodriguez a. ACS Med Chem Lett. 2013 Dec 29;5(2):149-53. doi: 10.1021/ml400403u. eCollection 2014 Feb 13. ACS Med Chem Lett. 2013. PMID: 24900788 Free PMC article.
Identification of small-molecule inhibitors of Trypansoma cruzi replication.
Germain AR, Carmody LC, Dockendorff C, Galan-Rodriguez C, Rodriguez A, Johnston S, Bittker JA, MacPherson L, Dandapani S, Palmer M, Schreiber SL, Munoz B. Germain AR, et al. Among authors: rodriguez a. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7197-200. doi: 10.1016/j.bmcl.2011.09.057. Epub 2011 Sep 29. Bioorg Med Chem Lett. 2011. PMID: 22018462
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
Andriani G, Amata E, Beatty J, Clements Z, Coffey BJ, Courtemanche G, Devine W, Erath J, Juda CE, Wawrzak Z, Wood JT, Lepesheva GI, Rodriguez A, Pollastri MP. Andriani G, et al. Among authors: rodriguez a. J Med Chem. 2013 Mar 28;56(6):2556-67. doi: 10.1021/jm400012e. Epub 2013 Mar 13. J Med Chem. 2013. PMID: 23448316 Free PMC article.
Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides.
Russell S, Rahmani R, Jones AJ, Newson HL, Neilde K, Cotillo I, Rahmani Khajouei M, Ferrins L, Qureishi S, Nguyen N, Martinez-Martinez MS, Weaver DF, Kaiser M, Riley J, Thomas J, De Rycker M, Read KD, Flematti GR, Ryan E, Tanghe S, Rodriguez A, Charman SA, Kessler A, Avery VM, Baell JB, Piggott MJ. Russell S, et al. Among authors: rodriguez a. J Med Chem. 2016 Nov 10;59(21):9686-9720. doi: 10.1021/acs.jmedchem.6b00442. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27548560 Free article.
Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
Woodring JL, Behera R, Sharma A, Wiedeman J, Patel G, Singh B, Guyett P, Amata E, Erath J, Roncal N, Penn E, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP. Woodring JL, et al. Among authors: rodriguez a. ACS Med Chem Lett. 2018 Sep 4;9(10):996-1001. doi: 10.1021/acsmedchemlett.8b00245. eCollection 2018 Oct 11. ACS Med Chem Lett. 2018. PMID: 30344906 Free PMC article.
Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.
Bachovchin KA, Sharma A, Bag S, Klug DM, Schneider KM, Singh B, Jalani HB, Buskes MJ, Mehta N, Tanghe S, Momper JD, Sciotti RJ, Rodriguez A, Mensa-Wilmot K, Pollastri MP, Ferrins L. Bachovchin KA, et al. Among authors: rodriguez a. J Med Chem. 2019 Jan 24;62(2):665-687. doi: 10.1021/acs.jmedchem.8b01365. Epub 2019 Jan 10. J Med Chem. 2019. PMID: 30565932 Free PMC article.
Discovery and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease.
Harrison JR, Sarkar S, Hampton S, Riley J, Stojanovski L, Sahlberg C, Appelqvist P, Erath J, Mathan V, Rodriguez A, Kaiser M, Pacanowska DG, Read KD, Johansson NG, Gilbert IH. Harrison JR, et al. Among authors: rodriguez a. J Med Chem. 2020 Mar 26;63(6):3066-3089. doi: 10.1021/acs.jmedchem.9b01852. Epub 2020 Mar 5. J Med Chem. 2020. PMID: 32134269
Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
Singh B, Bernatchez JA, McCall LI, Calvet CM, Ackermann J, Souza JM, Thomas D, Silva EM, Bachovchin KA, Klug DM, Jalani HB, Bag S, Buskes MJ, Leed SE, Roncal NE, Penn EC, Erath J, Rodriguez A, Sciotti RJ, Campbell RF, McKerrow J, Siqueira-Neto JL, Ferrins L, Pollastri MP. Singh B, et al. Among authors: rodriguez a. ACS Med Chem Lett. 2020 Jan 10;11(3):249-257. doi: 10.1021/acsmedchemlett.9b00453. eCollection 2020 Mar 12. ACS Med Chem Lett. 2020. PMID: 32184953 Free PMC article.
8,212 results