«Synthesis, biophysical and biological studies of N-phenylbenzamide derivatives targeting kinetoplastid parasites» Nué-Martinez, J. J.; Cisneros, D.; Moreno-Blázquez, M. V.; Fonseca-Berzal, C.; Manzano, J. I.; Kraeutler, D.; Ungogo, M.; Aloraini, M.; Elati , H.; Ibáñez-Escribano, A.; Lagartera, L.; Herraiz, T.; Gamarro, F.; de Koning, H.; Gómez-Barrio, A.; Dardonville, C. J. Med. Chem. 2023, 66, 13452-13480.
«Methyl N-(tert-butoxycarbonyl)pyridine-2-carbimidothioate: A new reagent for the synthesis of N-phenylpyridinecarboxamidine (“arylimidamide”) DNA-minor groove binders from poorly nucleophilic amines». Nué-Martinez, J.J.; Cisneros, D.; Dardonville, C. Bioorg. Med. Chem. Lett. 2022, 74, 128926.
«Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure–Activity Relationship Studies» Cisneros, D.; Cueto-Díaz, E. J.; Medina-Gil, T.; Chevillard, R.; Bernal-Fraile, T.; López-Sastre, R.; Aldfer, M. M.; Ungogo, M. A.; Elati, H. A. A.; Arai, N.; Otani, M.; Matsushiro, S.; Kojima, C.; Ebiloma, G. U.; Shiba, T.; de Koning, H. P.; Dardonville, C. ACS Med. Chem. Lett. 2022, 13, 312-318
«High yield synthesis of trans-azoxybenzene versus 2-isopropoxy-4-nitrobenzoic acid: influence of temperature and base concentration» Nué-Martínez, J.J.; Alkorta, I.; Dardonville, C. Arkivoc 2021, viii, 265-273.
«Synthesis, biological, and photophysical studies of molecular rotor-based fluorescent inhibitors of the Trypanosome Alternative Oxidase» Cueto-Díaz, E. J.; Ebiloma, G. U.; Alfayez, I. A.; Ungogo, M. A.; Lemgruber, L.; González-García, M. C.; Giron, M. D.; Salto, R.; Fueyo-González, F. J.; Shiba, T.; González-Vera, J. A.; Ruedas Rama, M. J.; Orte, A.; de Koning, H. P.; Dardonville, C. Eur. J. Med. Chem. 2021, 220, 113470.
«Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei« Alghamdi, A. H.; Munday, J. C.; Campagnaro, G. D.; Gurvic, D.; Svensson, F.; Okpara, C. E.; Kumar, A.; Quintana, J.; Martin Abril, M. E.; Milic, P.; Watson, L.; Paape, D.; Settimo, L.; Dimitriou, A.; Wielinska, J.; Smart, G.; Anderson, L. F.; Woodley, C. M.; Kelly, S. P. Y.; Ibrahim, H. M.; Hulpia, F.; Al-Salabi, M. I.; Eze, A. A.; Sprenger, T.; Teka, I. A.; Gudin, S.; Weyand, S.; Field, M.; Dardonville, C.; Tidwell, R. R.; Carrington, M.; O’Neill, P.; Boykin, D. W.; Zachariae, U.; De Koning, H. P. Elife 2020, 9.
«Aqueous pKa Prediction for Tautomerisable Compounds Using Equilibrium Bond Lengths» Caine, B.; Bronzato, M.; Fraser, T.; Kidley, N.; Dardonville, C.; Popelier, P.L.A. Commun. Chem. 2020, 3, 21
«A theoretical and spectroscopic (NMR and IR) study of indirubin in solution and in the solid-state» Alkorta, I.; Elguero, J.; Dardonville, C.; Reviriego, F.; Santa María, D.; Claramunt, R.M.; Marín-Luna, M. J. Phys. Org. Chem. 2020, 33, e4043.
«Discovery and Pharmacological Studies of 4-Hydroxyphenyl-Derived Phosphonium Salts Active in a Mouse Model of Visceral Leishmaniasis» Manzano, J. I.; Cueto-Díaz, E. J.; Olías-Molero, A. I.; Perea, A.; Herraiz, T.; Torrado, J. J.; Alunda, J. M.; Gamarro, F.; Dardonville, C. J. Med. Chem. 2019, 62, 10664-10675.
«Alternative oxidase inhibitors: Mitochondrion-targeting as a strategy for new drugs against pathogenic parasites and fungi” Ebiloma, G. U.; Balogun, E. O.; Cueto-Díaz, E. J.; de Koning, H. P.; Dardonville, C. Med. Res. Rev. 2019, 39, 1553-1602.
“SAR of 4-Alkoxybenzoic Acid Inhibitors of the Trypanosome Alternative Oxidase” Meco-Navas, A.; Ebiloma, G. U.; Martín-Domínguez, A.; Martínez-Benayas, I.; Cueto-Díaz, E. J.; Alhejely, A. S.; Balogun, E. O.; Saito, M.; Matsui, M.; Arai, N.; Shiba, T.; Harada, S.; de Koning, H. P.; Dardonville, C. ACS Med. Chem. Lett. 2018, 9, 923-928.
«Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense” Ebiloma, G. U.; Ayuga, T. D.; Balogun, E. O.; Gil, L. A.; Donachie, A.; Kaiser, M.; Herraiz, T.; Inaoka, D. K.; Shiba, T.; Harada, S.; Kita, K.; de Koning, H. P.; Dardonville, C. Eur. J. Med. Chem. 2018, 150, 385-402.
“Prediction of Aqueous pKa Values for Guanidine-Containing Compounds Using Ab Initio Gas-Phase Equilibrium Bond Lengths” Caine, B.A.; Dardonville, C.; Popelier, P.L.A. ACS OMEGA 2018, 3, 3835-3850.
“The structure of fosfomycin salts in solution and in the solid state by nuclear magnetic resonance spectroscopy and DFT calculations” Pérez Torralba, M.; Sanz, D.; Claramunt, R.M.; Alkorta, I.; Dardonville, C.; Elguero, J. Tetrahedron 2018, 74, 3937-3942.
“Automated techniques in pKa determination: low, medium and high-throughput screening methods” Dardonville, C. Drug Discov. Today Technol. 2018, 27, 49-58.
“Substituent effect on the basicity (pKa) of aryl guanidines and 2-(arylimino)imidazolidines: correlations of pH-metric and UV-metric values with predictions from gas-phase ab initio bond lengths” Dardonville, C.; Caine, B.A.; Navarro de la Fuente, M.; Martín Herranz, G.; Corrales Mariblanca, B.; Popelier, P.L.A. New J. Chem. 2017, 41, 11016-11028.
“Bis(2-aminoimidazolines) and Bisguanidines: Synthetic Approaches, Antiparasitic Activity and DNA Binding Properties” Dardonville, C.; Nué Martinez, J.J. Curr. Med. Chem. 2017, 24, 3606-3632.
“Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast” Millan, C.; Acosta-Reyes, F.; Lagartera, L.; Ebiloma, G.; Lemgruber, L.; Nué Martinez, J.J.; Saperas, N.; Dardonville, C.; de Koning, H.; Campos, J.L. Nucleic Acids Res. 2017, 45, 8378-8391
«Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Anti-parasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion” Fueyo González, F. J.; Ebiloma, G. U.; Izquierdo García, C.; Bruggeman, V.; Sánchez Villamañán, J. M.; Donachie, A.; Balogun, E. O.; Inaoka, D. K.; Shiba, T.; Harada, S.; Kita, K.; de Koning, H. P.; Dardonville, C. J. Med. Chem. 2017, 60, 1509-1522
«Trypanocidal action of bisphosphonium salts through a mitochondrial target in bloodstream form Trypanosoma brucei» Alkhaldi, A.A.M.; Martinek, J.; Panicucci, B.; Dardonville, C.; Zíková, A.; de Koning, H.P. Int. J. Parasitol.-Drugs Drug Resist., 2016, 6, 23-34.
«Bisimidazoline arylamides binding to the DNA minor groove. N1-hydroxylation enhances binding affinity and selectivity to AATT sites» Ríos Martínez, C.H. Lagartera, L., Trujillo, C., Dardonville, C. MedChemComm, 2015, 6, 2036-2042.
«Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro» Ríos Martínez, C.H.; Nué Martínez, J.J.; Ebiloma, G.U.; de Koning, H.P.; Alkorta, I.; Dardonville, C. Eur. J. Med. Chem. 2015, 101, 806-817.
«Influence of ornithine decarboxylase antizymes and antizyme inhibitors on agmatine uptake by mammalian cells»
Ramos.Molina, B.; López-Contreras, A.J.; Lambertos, A.; Dardonville, C.; Cremades, A.; Penafiel, R. Amino Acids 2015, 47, 1025-1034.
«Antiprotozoal activity and DNA binding of dicationic acridones»
Montalvo-Quirós, S.; Taladriz-Sender, A.; Kaiser, M.; Dardonville, C.
J. Med. Chem. 2015, 58, 1940-1949.
«Observation of diastereotopic signals in 15N NMR spectroscopy»
Alkorta, I.; Dardonville, C.; Elguero, J. Angew. Chem. Int. Ed. 2015, 54, 3997-4000.
«A new nonpolar N-hydroxy imidazoline lead compound with improved activity in a murine model of late-stage Trypanosoma brucei brucei infection is not cross-resistant with diamidines.»
Ríos Martínez C.H., Miller F., Ganeshamoorthy K., Glacial F., Kaiser M., de Koning H.P., Eze A.A., Lagartera L., Herraiz T., Dardonville C.
Antimicrob. Agents Chemother. 2015, 59, 890-904.
«SAR studies of diphenyl cationic trypanocides: superior activity of phosphonium over ammonium salts.»
Dardonville, C.; Alkhaldi, A.; de Koning, H.
ACS Med. Chem. Lett. 2015, 6, 151–155.
«Antiprotozoal activity and DNA binding of N-Substituted N-phenylbenzamide and 1,3-Diphenylurea Bisguanidines»
Ríos Martínez, C.H., Lagartera, L., Kaiser, M., Dardonville, C.
Eur. J. Med. Chem. 2014, 81, 481–491.
«In and Out the minor groove: Interaction of an AT-rich DNA with the CD27 drug»
Acosta-Reyes, F. J.; Dardonville, C.; de Koning, H. P.; Natto, M.; Subirana, J. A.; Campos, J. L. Acta Cryst. 2014, D70, 1614-1621
«Rapid Determination of Ionization Constants (pKa) by UV Spectroscopy Using 96-Well Microtiter Plates”
Ríos Martínez, C.H., Dardonville, C. ACS Med. Chem. Lett.. 2013, 4, 142-145.
“Discovery of Nitroheterocycles Active against African Trypanosomes. In Vitro Screening and Preliminary SAR Studies” Arán, V. J., Kaiser, M., Dardonville, C. Bioorg. Med. Chem. Lett. 2012, 22, 4506-4516.
”Validation of novel fluorescence assays for the routine screening of drug susceptibilities of Trichomonas vaginalis”
Natto, M.; Savioli, F.; Quashie, N.; Dardonville, C.; Rodenko, B.; De Koning, H. J. Antimicrob. Chemother. 2012, 67, 933-943
”Synthesis and Structure-Activity Analysis of New Phosphonium Salts with Potent Activity Against African Trypanosomes” Taladriz, A.; Healy, A.;Flores Pérez, E.; Herrero García, V.; Ríos Martínez, C.; Alkhaldi, A.; Eze, A.; Kaiser, M.; De Koning, H.; Chana, A.; Dardonville, C. J. Med. Chem. 2012, 55, 2606-2622
”Synthesis and Antiprotozoal Activity of N-Alkoxy Analogues of the Trypanocidal Lead Compound 4,4′-Bis(imidazolinylamino)diphenylamine with Improved Human Blood Brain Barrier Permeability.”
Nieto Garrido, L.; Mascaraque, A.; Miller, F.; Glacial, F.; Rios Martinez, C.; Kaiser, M.; Brun, R.; Dardonville, C. J. Med. Chem. 2011, 54, 485-494.
“New benzophenone-derived bisphosphonium salts as leishmaniccidal leads targeting mitochondria through inhibition of respiratory complex II”
Luque-Ortega, J. Román; Reuther, P.; Rivas, L.; Dardonville, C.
J. Med. Chem. 2010, 53, 1788-1798.
”Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives”
Dardonville, C.; Fernández-Fernández, C.; Gibbons, S-L.; Jagerovic, N.; Nieto, L.; Ryan, G.; Kaiser, M.; Brun, R.
Antimicrob. Agents Chemother. 2009, 53(9), 3815-3821.
«Crystal Structure of a Trypanocidal 4,4´-Bis(imidazolinylamino)diphenylamine Bound to DNA”
Glass, L.S.; Nguyen, B.; Goodwin, K.D.; Dardonville, C.; Wilson, W.D.; Long, E.C.; Georgiadis, M.M. Biochemistry 2009, 48, 5943-5952.
”Efficient one-pot synthesis of 1-alkoxy-2-arylaminoimidazolines from N-alkoxy-N-(2-aminoethyl)-2-nitrobenzenesulfonamides and arylisothiocyanates”
Mascaraque, A.; Nieto, L.; Dardonville, C. Tetrahedron Lett. 2008, 49, 4571-4574.
”New Bis(2-aminoimidazoline) and Bisguanidine DNA Minor Groove Binders with Potent in Vivo Antitrypanosomal and Antiplasmodial Activity” Rodríguez, F.; Rozas, I.; Kaiser, M.; Brun, R.; Nguyen, B.; Wilson, W.D.; García, R.N.; Dardonville, C. J. Med. Chem. 2008, 51, 909–923.
”DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.”
Dardonville, C.; Barrett, M. P.; Brun, R.; Kaiser, M.; Tanious, F.; Wilson, W.D. J. Med. Chem. 2006, 49, 3748-3752.
”Recent advances in anti-trypanosomal chemotherapy: patent literature 2002-2004.”
Dardonville, C. Exp. Opin. Ther. Patent. 2005, 15, 1241-1257.
”Bisguanidinium, bis(2-aminoimidazolinium) and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.”
Dardonville, C.; Brun, R. J. Med. Chem. 2004, 47, 2296-2307.