Szajnman, Sergio Hernán

Doctor en Ciencias Químicas, UBA.

Email:

shs@qo.fcen.uba.ar

Síntesis Orgánica aplicada al diseño de agentes antiparasitarios, antivirales y antitumorales

Integrantes del Proyecto

Tamila Galaka (Beca Doctoral Conicet)
Sheila Irina de Diego Saadia. (Beca Doctoral UBA)

El interés del grupo está centrado en la Síntesis total de compuestos de importancia farmacológica. En primer lugar el grupo está interesado en la síntesis de nucleósidos conformacionalmente restringidos siendo la síntesis asimétrica la estrategia fundamental para la obtención de los mismos. El segundo interés del grupo está centrado en el diseño de drogas mediante un riguroso estudio de la relación estructura química-actividad biológica (SAR) de diferentes agentes antivirales y antiparasitarios, para lo cual es fundamental comprender el modo de acción y el reconocimiento molecular de dichos agentes.

Organic Synthesis applied to the Design of Antiparasitic, Antiviral and Antitumor agents

We are interested in the total synthesis of compounds of pharmacological importance. In the first place, we are involved in the synthesis of conformationally restricted nucleosides, asymmetric synthesis being the fundamental strategy for obtaining them. Our second attention is focused on the design of drugs through a rigorous study of the relationship between chemical structure and biological activity (SAR) of different antiviral and antiparasitic agents, for which it is essential to understand the mode of action and molecular recognition of these agents

Selected publications

Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of trypanosoma cruzi farnesyl diphosphate synthase. Aripirala, S., Szajnman, S.H., Jakoncic, J., Rodriguez, J.B., Docampo, R., Gabelli, S.B., Amzel, L.M. Journal of Medicinal Chemistry, 2012, 55, 6445-6454.

Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents. Recher, M., Barboza, A.P., Li, Z.-H., Galizzi, M., Ferrer-Casal, M., Szajnman, S.H., Docampo, R., Moreno, S.N.J., Rodriguez, J.B. European Journal of Medicinal Chemistry, 2013, 60, 431-440.

Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents. Elicio, P.D., Chao, M.N., Galizzi, M., Li, C., Szajnman, S.H., Docampo, R., Moreno, S.N.J., Rodriguez, J.B. European Journal of Medicinal Chemistry, 2013, 69, 480-489.

In Vitro and in Vivo activities of sulfur-containing linear bisphosphonates against apicomplexan parasites. Szajnman, S.H., Galaka, T., Li, Z.-H., Li, C., Howell, N.M., Chao, M.N., Striepen, B., Muralidharan, V., Moreno, S.N.J., Rodriguez, J.B. Antimicrobial Agents and Chemotherapy, 2017, 61, art. no. e01590.

Synergistic activity between statins and bisphosphonates against acute experimental toxoplasmosis. Li, Z.-H., Li, C., Szajnman, S.H., Rodriguez, J.B., Moreno, S.N.J. Antimicrobial Agents and Chemotherapy, 2017, 61, art. no. e02628.

Selenium-containing analogues of WC-9 are extremely potent inhibitors of Trypanosoma cruzi proliferation. Chao, M.N., Storey, M., Li, C., Rodríguez, M.G., Di Salvo, F., Szajnman, S.H., Moreno, S.N.J., Docampo, R., Rodriguez, J.B. Bioorganic and Medicinal Chemistry, 2017, 25, 6435-6449.

Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi. Chao, M.N.; Lorenzo-Ocampo, M.V.; Szajnman, S.H.; Docampo, R., Rodriguez, J.B. Bioorganic and Medicinal Chemistry, 2019, 27, 1350-1361.

Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii. Galaka, T.; Falcone, B.; Li, C.; Szajnman, S.H.; Moreno, S.N.J.; Docampo, R.; b, Rodriguez, J.B. Bioorganic and Medicinal Chemistry, 2019, 27, 3663–3673.