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Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity.
Uliassi E, Fiorani G, Krauth-Siegel RL, Bergamini C, Fato R, Bianchini G, Carlos Menéndez J, Molina MT, López-Montero E, Falchi F, Cavalli A, Gul S, Kuzikov M, Ellinger B, Witt G, Moraes CB, Freitas-Junior LH, Borsari C, Costi MP, Bolognesi ML. Uliassi E, et al. Among authors: witt g. Eur J Med Chem. 2017 Dec 1;141:138-148. doi: 10.1016/j.ejmech.2017.10.005. Epub 2017 Oct 3. Eur J Med Chem. 2017. PMID: 29031061
Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.
Borsari C, Luciani R, Pozzi C, Poehner I, Henrich S, Trande M, Cordeiro-da-Silva A, Santarem N, Baptista C, Tait A, Di Pisa F, Dello Iacono L, Landi G, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Gribbon P, Kohler M, Keminer O, Behrens B, Costantino L, Tejera Nevado P, Bifeld E, Eick J, Clos J, Torrado J, Jiménez-Antón MD, Corral MJ, Alunda JM, Pellati F, Wade RC, Ferrari S, Mangani S, Costi MP. Borsari C, et al. Among authors: witt g. J Med Chem. 2016 Aug 25;59(16):7598-616. doi: 10.1021/acs.jmedchem.6b00698. Epub 2016 Aug 5. J Med Chem. 2016. PMID: 27411733 Free article.
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.
Borsari C, Santarem N, Torrado J, Olías AI, Corral MJ, Baptista C, Gul S, Wolf M, Kuzikov M, Ellinger B, Witt G, Gribbon P, Reinshagen J, Linciano P, Tait A, Costantino L, Freitas-Junior LH, Moraes CB, Bruno Dos Santos P, Alcântara LM, Franco CH, Bertolacini CD, Fontana V, Tejera Nevado P, Clos J, Alunda JM, Cordeiro-da-Silva A, Ferrari S, Costi MP. Borsari C, et al. Among authors: witt g. Eur J Med Chem. 2017 Jan 27;126:1129-1135. doi: 10.1016/j.ejmech.2016.12.017. Epub 2016 Dec 9. Eur J Med Chem. 2017. PMID: 28064141
Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery.
Linciano P, Dawson A, Pöhner I, Costa DM, Sá MS, Cordeiro-da-Silva A, Luciani R, Gul S, Witt G, Ellinger B, Kuzikov M, Gribbon P, Reinshagen J, Wolf M, Behrens B, Hannaert V, Michels PAM, Nerini E, Pozzi C, di Pisa F, Landi G, Santarem N, Ferrari S, Saxena P, Lazzari S, Cannazza G, Freitas-Junior LH, Moraes CB, Pascoalino BS, Alcântara LM, Bertolacini CP, Fontana V, Wittig U, Müller W, Wade RC, Hunter WN, Mangani S, Costantino L, Costi MP. Linciano P, et al. Among authors: witt g. ACS Omega. 2017 Sep 30;2(9):5666-5683. doi: 10.1021/acsomega.7b00473. Epub 2017 Sep 11. ACS Omega. 2017. PMID: 28983525 Free PMC article.
Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
Linciano P, Moraes CB, Alcantara LM, Franco CH, Pascoalino B, Freitas-Junior LH, Macedo S, Santarem N, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Ellinger B, Ferrari S, Luciani R, Quotadamo A, Costantino L, Costi MP. Linciano P, et al. Among authors: witt g. Eur J Med Chem. 2018 Feb 25;146:423-434. doi: 10.1016/j.ejmech.2018.01.043. Epub 2018 Jan 31. Eur J Med Chem. 2018. PMID: 29407968
In vitro and in silico analysis of the effects of D2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations.
de Witte WEA, Versfelt JW, Kuzikov M, Rolland S, Georgi V, Gribbon P, Gul S, Huntjens D, van der Graaf PH, Danhof M, Fernández-Montalván A, Witt G, de Lange ECM. de Witte WEA, et al. Among authors: witt g. Br J Pharmacol. 2018 Nov;175(21):4121-4136. doi: 10.1111/bph.14456. Epub 2018 Sep 21. Br J Pharmacol. 2018. PMID: 30051456 Free PMC article.
α-Amino Diphenyl Phosphonates as Novel Inhibitors of Escherichia coli ClpP Protease.
Moreno-Cinos C, Sassetti E, Salado IG, Witt G, Benramdane S, Reinhardt L, Cruz CD, Joossens J, Van der Veken P, Brötz-Oesterhelt H, Tammela P, Winterhalter M, Gribbon P, Windshügel B, Augustyns K. Moreno-Cinos C, et al. Among authors: witt g. J Med Chem. 2019 Jan 24;62(2):774-797. doi: 10.1021/acs.jmedchem.8b01466. Epub 2019 Jan 11. J Med Chem. 2019. PMID: 30571121
Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform.
Moraes CB, Witt G, Kuzikov M, Ellinger B, Calogeropoulou T, Prousis KC, Mangani S, Di Pisa F, Landi G, Iacono LD, Pozzi C, Freitas-Junior LH, Dos Santos Pascoalino B, Bertolacini CP, Behrens B, Keminer O, Leu J, Wolf M, Reinshagen J, Cordeiro-da-Silva A, Santarem N, Venturelli A, Wrigley S, Karunakaran D, Kebede B, Pöhner I, Müller W, Panecka-Hofman J, Wade RC, Fenske M, Clos J, Alunda JM, Corral MJ, Uliassi E, Bolognesi ML, Linciano P, Quotadamo A, Ferrari S, Santucci M, Borsari C, Costi MP, Gul S. Moraes CB, et al. Among authors: witt g. SLAS Discov. 2019 Mar;24(3):346-361. doi: 10.1177/2472555218823171. SLAS Discov. 2019. PMID: 30784368 Free PMC article.
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
Linciano P, Pozzi C, Iacono LD, di Pisa F, Landi G, Bonucci A, Gul S, Kuzikov M, Ellinger B, Witt G, Santarem N, Baptista C, Franco C, Moraes CB, Müller W, Wittig U, Luciani R, Sesenna A, Quotadamo A, Ferrari S, Pöhner I, Cordeiro-da-Silva A, Mangani S, Costantino L, Costi MP. Linciano P, et al. Among authors: witt g. J Med Chem. 2019 Apr 25;62(8):3989-4012. doi: 10.1021/acs.jmedchem.8b02021. Epub 2019 Apr 9. J Med Chem. 2019. PMID: 30908048
138 results