Publications

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    2017

  • Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites
    Tamila Galaka, Mariana Ferrer Casal, Melissa Storey, Catherine Li, Maria N. Chao, Sergio H. Szajnman, Roberto Docampo, Silvia N. J. Moreno and Juan B. Rodriguez
    Molecules 2017, 22, 82 doi: 10.3390/molecules22010082


  • 2016

  • Activity of Fluorine-Containing Analogues of WC-9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii
    Maria N. Chao, Catherine Li, Melissa Storey, Dr. Bruno N. Falcone, Dr. Sergio H. Szajnman, Prof. Dr. Sergio M. Bonesi, Prof. Dr. Roberto Docampo, Prof. Dr. Silvia N. J. Moreno, Prof. Dr. Juan B. Rodriguez
    ChemMedChem 2016, 1, 2690-2702 doi: 10.1002/cmdc.201600505


  • WC-9 a Lead Drug with Great Prospects for American Trypanosomiasis and Toxoplasmosis
    Rodriguez JB
    Mini-Reviews in Med. Chem. 2016, 16, 1195 - 1200 doi: 10.2174/1389557516666160611015034


  • Detection and treatment of Trypanosoma cruzi: a patent review (2011-2015).
    Rodriguez JB, Falcone BN, Szajnman SH.
    Expert Opin. Ther. Pat. 2016, 29, 993-1015. doi: 10.1080/13543776.2016.1209487


  • Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase
    Rodriguez, Juan B., Falcone, Bruno N., Szajnman, Sergio H.
    Expert Opinion on Drug Discovery 2016, 441, 307-320. doi: 10.1517/17460441.2016.1143814


  • 2015

  • Aryloxyethyl thiocyanates are potent growth inhibitors of Trypanosoma cruzi and Toxoplasma gondii.
    Chao, M.N., Matiuzzi, C.E., Storey, M., Li, C., Szajnman, S.H., Docampo, R., Moreno, S.N.J., Rodriguez, J.B.
    ChemMedChem 2015, 10, 1094-1108. doi: 10.1002/cmdc.201500100


  • 2014

  • New Insights into Molecular Recognition of 1,1-Bisphosphonic Acids by Farnesyl Pyrophosphate Synthase.
    Ferrer-Casal, M.;Li, C.; Galizzi, M.; Stortz, Carlos A.; Szajnman, Sergio H.; Docampo, Roberto; Moreno, Silvia N. J.; Rodriguez. Juan B.
    Bioorg. Med. Chem. 2014, 22, 398-405. doi: 10.1016/j.bmc.2013.11.010


  • Solanesyl diphosphate synthase, an enzyme of the ubiquinone synthetic pathway, is required throughout the life cycle of Trypanosoma brucei.
    Lai, D.-H., Poropat, E., Pravia, C., Landoni, M., Couto, A.S., Pérez Rojo, F.G., Fuchs, A.G., Dubin, M., Elingold, I., Rodríguez, J.B., Ferella, M., Esteva, M.I., Bontempi, E.J., Lukes, J.
    Eukaryotic Cell 2014, 13, 320-328. doi: 10.1128/EC.00271-13


  • Tetraethyl vinylidenebisphosphonate: A versatile synthon for the preparation of bisphosphonates.
    Juan B. Rodriguez.
    Synthesis 2014, 46, 1129-1142. doi: 10.1055/s-0033-1340952


  • 2013

  • Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.
    Recher, M; Borboza, A. P.; Li, Z.-H.; Galizzi, M.; Ferrer-Casal, M.; Szajnman, S. H.; Docampo, R.; Morena, S. N. J.; Rodriguez, J. B.
    Eup. J. Med. Chem. 2013, 60, 431-440. doi: 10.1016/j.ejmech.2012.12.015


  • 1,3-Dipolar cycloadditions on the versatile intermediate tetraethyl ethylidene bisphosphonate.
    Ferrer Casal, M.; Barboza, A. P.; Sergio H. Szajnman, S. H. and Rodriguez, J. B.
    Synthesis 2013, 45, 2397-404. doi: 10.1055/s-0033-1338498


  • Design, Synthesis and Biological Evaluation of WC-9 Analogues as Antiparasitic Agents.
    Pablo Elicio, Maria N. Chao, Zhu-Hong Li, Melina Galizzi, Sergio H. Szajnman, Roberto Docampo, Silvia N. J. Moreno, and Juan B. Rodriguez.
    Eur. J. Med. Chem. 2013, 69, 480-489. doi: 10.1016/j.ejmech.2013.09.009


  • 2012

  • 1-(Fluoroalkylidene)-1,1-bisphosphonic Acids are Potent and Selective Inhibitors of the Enzymatic Activity of Toxoplasma gondii Farnesyl Pyrophosphate Synthase.
    Szajnman, S. H., Rosso, V. S., Malayil, L., Smith, A., Moreno, S. N. J., Docampo, R., Rodriguez, J. B.;
    Org. Biomol. Chem. 2012 10, 1424-33. doi: 10.1039/c1ob06602a


  • New antibacterials for the treatment of toxoplasmosis; a patent review.
    Rodriguez, J.B., Szajnman, S.H.
    Expert Opin Ther Pat. 2012, 22, 311-33. doi: 10.1517/13543776.2012.668886


  • Trypanosoma cruzi Squalene Synthase is a Major Target for 2-Alkylaminoethyl-1,1-Bisphosphonates.
    Carlos Poveda, Dolores Gonzalez-Pacanowska, Sergio H. Szajnman, and Juan B. Rodriguez,
    Antimicrob. Agents Chemother. 2012, 56, 4483-4486. doi: 10.1128/AAC.00796-12


  • Design, Synthesis, Calorimetry and Crystallographic analysis of 2-Alkylaminoethyl-1,1-Bisphosphonates as inhibitors of Trypanosoma cruzi Farnesyl Diphosphate Synthase.
    Srinivas Aripirala, Sergio H. Szajnman, Jean Jakoncic, Juan B. Rodriguez, Roberto Docampo, Sandra B. Gabelli, and L. Mario Amzel.
    J. Med. Chem. 2012, 55, 6445-6454. doi: 10.1021/jm300425y


  • 2011

  • Synthesis and Biological Evaluation of New 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting Farnesyl Diphosphate Synthase.
    V. S. Rosso, S. H. Szajnman, L. Malayil, M. Galizzi, S. N. J. Moreno, R. Docampo, and J. B. Rodriguez.
    Bioorg. Med. Chem. 2011, 19, 2211-2217. doi: 10.1016/j.bmc.2011.02.037


  • Electron Transfer Dynamics of Rhodotermus marinus caa3 Cytochrome c Domain on Biomimetic Films.
    M. F. Molinas, A. De Candia, S. H. Szajnman, J. B. Rodriguez, M. Marti, S. Todorovic, and D. H. Murgida.
    Phys. Chem. Chem. Phys. 2011, 13, 18088-18098. doi: 10.1039/c1cp21925a


  • 2010

  • Synthesis and biological evaluation of N-thia-carba-thymidine as an antiherpetic agent.
    E. Elhalem, C. A Pujol, E. B Damonte and J. B. Rodriguez
    Tetrahedron 2010, 66. 3332-3340. doi: 10.1016/j.tet.2010.02.092


  • 2010 - 2005

  • Synthesis and Biological Evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting Farnesyl Diphosphate Synthase.
    S. H. Szajnman, G. E. Garcia Linares, Zhu-Hong Li, Melina Galizzi, Cuiying Jiang, E. Bontempi,M. Ferella, S. N. J. Moreno, R. Docampo and J. B. Rodriguez.
    Bioorg. Med. Chem. 2008, 16, 3283-3290. doi: 10.1016/j.bmc.2007.12.010


  • Fluorine-Containing Aryloxyethyl Thiocyanate Derivatives are Potent Inhibitors of Trypanosoma cruzi and Toxoplasma gondii Proliferation.
    G. Garcia Linares, S. Gismondi, N. Osa Codesido, S. N. J. Moreno, R. Docampo and J. B. Rodriguez.
    Bioorg. Med. Chem. Lett. 2007, 17, 5068-5071. doi: 10.1016/j.bmcl.2007.07.012


  • Current Status and Progresses made in Malaria Chemotherapy.
    G. Garcia Linares and J. B. Rodriguez
    Curr. Med. Chem. 2007, 14, 289-314. doi: 10.2174/092986707779941096


  • Synthesis of Conformationally Locked Carbocyclic Nucleosides Built on a Thiabicyclo[3.1.0]hexane System as a Pseudosugar Surrogate.
    E. Elhalem, M. J. Comin and J. B. Rodriguez
    Eur. J. Org. Chem. 2006, 4473-4482. doi: 10.1002/ejoc.200600488


  • Design, Synthesis and Biological Evaluation of Phosphinopeptides against Trypanosoma cruzi Targeting Trypanothione Biosynthesis
    E. L. Ravaschino, R. Docampo and J. B. Rodriguez
    J. Med. Chem. 2006, 49, 426-435. doi: 10.1021/jm050922i


  • Progresses in the Field of Drug Design to Combat Tropical Protozoan Parasitic Diseases.
    G. Garcia Linares, E. L. Ravaschino and J. B. Rodriguez
    Curr. Med. Chem. 2006, 13, 335-360. doi: 10.2174/092986706775476043


  • Photoinduced Changes of Absorption and Circular Dichroism in a Chiral Nematic Phase containing a Photochromic Fulgide.
    M. Bossi, J. B. Rodriguez and P. Aramendia
    J. Photochem. Photobiol. A: Chemistry 2006, 179, 35-41. doi: 10.1016/j.jphotochem.2005.07.009


  • First Synthesis of (+)-Neplanocin B.
    M. J. Comin, S. C. Pellegrinet and J. B. Rodriguez
    Arkivoc 2005, Part (xii), 205-213. Numero homenaje Prof. Rosa R. de Lederkremer. doi: 10.3998/ark.5550190.0006.c15


  • Synthesis and Biological Evaluation of 1-Amino-1,1-Bisphosphonates Derived from Fatty Acids against Trypanosoma cruzi targeting Farnesyl Pyrophosphate Synthase.
    S. H. Szajnman, E. L. Ravaschino, R. Docampo and J. B. Rodriguez
    Bioorg. Med. Chem. Lett. 2005, 15, 4685-4690. doi: 10.1016/j.bmcl.2005.07.060


  • New Insights into the Chemistry of gem-Bis(phosphonates): Unexpected Rearrangement of Michael-type Acceptors.
    S. H. Szajnman, G. Garcia Linares, P. Moro and J. B. Rodriguez
    Eur. J. Org. Chem. 2005, 3687-3696. doi: 10.1002/ejoc.200500097


  • Synthetic Studies towards the Preparation of (4R,5R)-(-)-3-[(Benzyloxy)methyl]-4,5-Oisopropylidene- cyclopenten-2-one. An Important Synthetic Intermediate for Carbanucleosides.
    E. Elhalem, M. J. Comin, J. Leitofuter, G. Garcia-Linares and J. B. Rodriguez
    Tetrahedron : Asymmetry, 2005, 16, 425-431. doi: 10.1016/j.tetasy.2004.11.069/


  • 2004 - 2000

  • Cerium Ammonium Nitrate: A New Catalyst for Regioselective Protection of Glycols.
    M. J. Comin, E. Elhalem and J. B. Rodriguez
    Tetrahedron 2004, 60, 11851-11860.
    doi: 10.1016/j.tet.2004.09.097


  • Structural Determinants of Efficacy at A3 Adenosine Receptors: Modification of the Ribose Moiety.
    Z. -G. Gao, L. S. Jeong, H. R. Moon, H. O. Kim, W. J. Choi, D. H. Shin, E. Elhalem, M. J. Comin, N. Melman, L. Mamedova, A. S. Gross, J. B. Rodriguez and K. A. Jacobson
    Biochem. Pharmacol. 2004, 67, 893-901. doi: 10.1016/j.bcp.2003.10.006


  • Synthesis and Biological Evaluation of Glutathione-like Tripeptides against Trypanosoma cruzi.
    E. L. Ravaschino, R. Docampo and J. B. Rodriguez
    Arkivoc 2003, Part (x), 298-313. Numero homenaje Prof. E. Ruveda & Prof. R. Rossi.


  • Bisphosphonates Derived from Fatty Acids are Potent Inhibitors of Trypanosoma cruzi
    Farnesyl Pyrophosphate Synthase.
    S. H. Szajnman, A. Montalvetti, Y. Wang, R. Docampo and J. B. Rodriguez
    Bioorg. Med. Chem. Lett. 2003, 13, 3231-3235. doi: 10.1016/S0960-894X(03)00663-2


  • Mechanism of action of 4-phenoxyphenoxy derivatives against Trypanosoma cruzi, the causative agent of Chagas disease.
    J. A. Urbina, J. L. Concepcion, A. Montalvetti, J. B. Rodriguez and R. Docampo.
    Antimicrob. Agents Chemother. 2003, 47, 2047-2050. doi: 10.1128/AAC.47.6.2047-2050.2003


  • Synthesis of Conformationally Locked Carbocyclic Nucleosides Built on an Oxabicyclo[3.1.0]hexane System.
    M. J. Comin, J. B. Rodriguez, P. Russ and V. E. Marquez
    Tetrahedron 2003, 59, 295-301. doi:10.1016/S0040-4020(02)01528-4


  • New Progresses in the Enantioselective Synthesis and Biological Properties of Carbocyclic Nucleosides.
    J. B. Rodriguez and M. J. Comin.
    Mini Rev. Med. Chem. 2003, 3, 95-114. doi: 10.2174/1389557033405331


  • Solubility of Two Stable Iminium Salts in 12 Polar Solvents.
    M. C. Grande, C. R. Barrero, C. M. Marschoff, J. B. Rodriguez and E. G. Gros.
    J. Chem. Eng. Data 2002, 47, 1337-1338. doi: 10.1021/je010263o


  • Glutathione-like Tripeptides as Inhibitors of Glutathionylspermidine Synthetase: 1. Substitution of the Glycine Carboxylic Acid Group.
    K. Amssoms, S. L. Oza, E. Ravaschino, A. Yamani, A. -M. Lambeir, P. Rajan, G. Bal, J. B. Rodriguez, A. H. Fairlamb, K. Augustyns and A. Haemers.
    Bioorg. Med. Chem. Lett. 2002, 12, 2553-2556. doi: 10.1016/S0960-894X(02)00489-4


  • Design, Synthesis and Biological Evaluation of Aryloxyethyl Thiocyanate Derivatives against Trypanosoma cruzi.
    E. Elhalem, B. N. Bailey, R. Docampo, I. Ujvary, S. H. Szajnman and J. B. Rodriguez
    J. Med. Chem. 2002, 45, 3984-3999. doi: 10.1021/jm0201518


  • Enantioselective Synthesis of (+)-Neplanocin F.
    M. J. Comin, J. Leitofuter and J. B. Rodriguez
    Tetrahedron 2002, 58, 3129-3136. doi: 10.1016/S0040-4020(02)00287-9


  • Specific Molecular Targets to Control Tropical Diseases.
    J. B. Rodriguez.
    Curr. Pharm. Des. 2001, 7, 1105-1116. doi: 10.2174/13816120133975550


  • Bisphosphonates Derived from Fatty Acids are Potent Growth Inhibitors of Trypanosoma cruzi.
    S. H. Szajnman, B. N. Bailey, R. Docampo and J. B. Rodriguez
    Bioorg. Med. Chem. Lett. 2001, 11, 789-792. doi: 10.1016/S0960-894X(01)00057-9


  • First Synthesis of (-)-Neplanocin C.
    M. J. Comin and J. B. Rodriguez
    Tetrahedron 2000, 56, 4639-4649. doi: 10.1016/S0040-4020(00)00379-30


  • Design and Synthesis of Aryloxyethyl Thiocyanate Derivatives as Potent Inhibitors of Trypanosoma cruzi Proliferation.
    S. H. Szajnman, W. Yan, B. N. Bailey, R. Docampo, E. Elhalem and J. B. Rodriguez
    J. Med. Chem. 2000, 43, 1826-1840. doi: 10.1021/jm9905007


  • Sulfur-containing Derivatives Structurally related to Fenoxycarb are Potent Growth Inhibitors against the Intracellular Form of Trypanosoma cruzi.
    J. B. Rodriguez, R. Docampo and E. G. Gros. Int.
    J. Antimicrob. Agents 2000, 13, 215-218. doi: 10.1016/S0924-8579(99)00125-9


  • 1999 - 1988

  • Biological Activity of very Potent Antiparasitic Agents Towards T84 Colon Tumor Cells.
    J. B. Rodriguez, E. Cafferata, T. A. Santa-Coloma and E. G. Gros.
    Rev. Latinoam. Quim. 1999, 27, 51-55.


  • Synthesis of C-5'-nor-Dideoxycarbanucleosides Structurally Related to Neplanocin C.
    M. J. Comin, C. A. Pujol, E. B. Damonte and J. B. Rodriguez
    Nucleosides Nucleotides 1999, 18, 2219-2231.


  • Chiral 1,4-Dicarbonyl-2,3-O-Isopropylidene Derivatives. Rapid Racemization on Standing.
    J. B. Rodriguez
    Tetrahedron 1999, 55, 2157-2170.


  • Growth Inhibitory Effect of Juvenile Hormone Analogues on Epimastigotes of Trypanosoma cruzi.
    J. B. Rodriguez, L. Zhong, R. Docampo, Z. Wimmer, and E. G. Gros.
    Bioorg. Med. Chem. Lett. 1998, 8, 3257-3260.


  • Expeditious Preparation of Aristeromicyn Analogues. Synthesis of 2',3'-Deoxyaristeromycin.
    M. J. Comin and J. B. Rodriguez.
    Anal. Asoc. Quim. Arg. 1998, 86, 131-138. (Numero homenaje al Dr. E. G. Gros).


  • Structure-Activity Relationship of New Growth Inhibitors of Trypanosoma cruzi.
    G. M. Cinque, S. H. Szajnman, L. Zhong, R. Docampo, A. J. Schvartzapel, J. B. Rodriguez and E. G. Gros.
    J. Med. Chem. 1998, 41, 1540-1554.


  • Design, Synthesis and Biological Evaluation of Isoprenoid Derivatives as Inhibitors of Trypanosoma cruzi Replication.
    J. B. Rodriguez, E. G. Gros and A. M. Stoka.
    Anal. Soc. Cient. Argentina 1997, 227, 87-91. (Dedicado al Dr. P. Cattaneo).


  • Design, Synthesis and Biological Evaluation of New Growth Inhibitors of Trypanosoma cruzi (Epimastigotes).
    A. J. Schvartzapel, L. Zhong, R. Docampo, J. B. Rodriguez and E. G. Gros.
    J. Med. Chem. 1997, 40, 2314-2322.


  • Biological Evaluation of Two Potent Inhibitors of Trypanosoma cruzi epimastigotes against the Intracellular Form of the Parasite.
    J. B. Rodriguez, L. Zhong, R. Docampo and E. G. Gros. Bioorg.
    Med. Chem. Lett. 1996, 6, 2783-2786.


  • The Sterols of Cucurbita moschata ("Calabacita") Seed Oil.
    J. B. Rodriguez, E. G. Gros, M. H. Bertoni and P. Cattaneo.
    Lipids 1996, 31, 1205-1208.


  • Recent Developments in the Control of Trypanosoma cruzi, the Causative Agent for Chagas' Disease.
    J. B. Rodriguez and E. G. Gros.
    Curr. Med. Chem. 1995, 2, 723-742.


  • Ritter Reaction on Terpenoids. IV. Remarkable Tendency to Produce 3-Aza-bicyclo [3.3.1] non-2-ene Systems from Mono and Sesquiterpenes.
    J. B. Rodriguez, E. G. Gros, J. A. Caram and C. M. Marschoff.
    Tetrahedron Lett. 1995, 36, 7825-7828.


  • Design, Synthesis and anti-Trypanosoma cruzi Evaluation of a New Class of Cell Growth Inhibitors Structurally Related to Fenoxycarb.
    A. J. Schvartzapel, L. Fichera, M. Esteva, J. B. Rodriguez and E. G. Gros
    Helv. Chim. Acta 1995, 78, 1207-1214.


  • Effects of Juvenile Hormone Analogues (JHA) on the Development of Trypanosoma cruzi.
    L. Fichera, M. Esteva, Z. Wimmer, J. B. Rodriguez and E. G. Gros
    Z. Naturforsch. C 1995, 50, 578-580.


  • Ritter Reaction on Terpenoids. III. Stereospecific Preparation of Bicyclic[3.3.1]Substituted Piperidines.
    W. N. Samaniego, A. Baldessari, M. A. Ponce, J. B. Rodriguez, E. G. Gros, J. A. Caram and C. M. Marschoff.
    Tetrahedron Lett. 1994, 35, 6967-6970.


  • Conformationally Locked Nucleosides Analogues. Synthesis of Dideoxycarbocyclic Nucleosides Analogues Structurally Related to Neplanocin C.
    J. B. Rodriguez, V. E. Marquez, M. C. Nicklaus, H. Mitsuya and J. J. Barchi, Jr.
    J. Med. Chem. 1994, 37, 3389-3399.


  • Effects of Juvenile Hormone on Mammalian Steroidogenesis.
    E. A. Vladusic, L. E. Bussmann, P. E. Visconti, A. M. Stoka, J. B. Rodriguez, E. G. Gros and E. H. Charreau. J. Steroid.
    Biochem. Mol. Biol. 1994, 50, 181-187.


  • Synthesis of Cyclopropane-fused Dideoxycarbocyclic Nucleosides Structurally Related to Neplanocin C.
    J. B. Rodriguez, V. E. Marquez, M. C. Nicklaus and J. J. Barchi, Jr.
    Tetrahedron Lett. 1993, 34, 6233-6236.


  • Gas Chromatographic-Mass Spectrometric Method for the Assessment of Oxidative Damage to Double Stranded DNA by Quantification Thymine Glycol Residues.
    S. P. Markey, C. J. Markey, T.-C. L. Wang and J. B. Rodriguez.
    J. Am. Soc. Mass Spectrom. 1993, 4, 336-342.


  • Preparation of 2(R) and 2(S) Methyl-2-Methylglycerates.
    J. B. Rodriguez, S. P. Markey and H. Ziffer.
    Tetrahedron : Asymmetry 1993, 4, 101-108.


  • Preparation of Enantiomerically Pure Juvenile Hormone Analogues.
    J. B. Rodriguez and E. G. Gros
    Anal. Asoc. Quim. Arg. 1992, 80, 139-148. (Dedicado al Dr. A. O. M. Stoppani).


  • Synthesis and Biological Activity of Synthetic Juvenile Hormone Analogues for Trypanosoma cruzi.
    J. B. Rodriguez, E. G. Gros and A. M. Stoka.
    Bioorg. Med. Chem. Lett. 1991, 1, 679-682.


  • Biological Activity of Synthetic Juvenile Hormone Analogues for Trypanosoma cruzi.
    A. M. Stoka, C. Rivas, E. Segura, J. B. Rodriguez and E. G. Gros
    Z. Naturforsch. B 1990, 45, 96-98.


  • A Convenient Method for the Preparation of Juvenile Hormone III.
    J. B. Rodriguez and E. G. Gros
    Z. Naturforsch. B 1990, 45, 93-95.


  • Synthesis and Activity of Juvenile Hormone Analogues. Part II.J. B. Rodriguez, E. G. Gros and A. M. Stoka.
    Z. Naturforsch. B 1989, 44, 983-987.


  • Synthesis and Activity of Juvenile Hormone Analogues.
    J. B. Rodriguez, E. G. Gros and A. M. Stoka.
    Z. Naturforsch. B 1988, 43, 1038-1042.