caa a22 4500 445341815 CHVBK 20180317142815.0 cr unu---uuuuu 170323e20110101xx s 000 0 eng 10.1007/s00436-010-2073-x doi (NATIONALLICENCE)springer-10.1007/s00436-010-2073-x Antileishmanial activity of imidothiocarbamates and imidoselenocarbamates [Elektronische Daten] [David Moreno, Daniel Plano, Ylenia Baquedano, Antonio Jiménez-Ruiz, Juan Antonio Palop, Carmen Sanmartín] In the present study, a family of 15 imidothio- and imidoselenocarbamates (1-15) analogs have been synthesized and screened for their in vitro antileishmanial potential against Leishmania infantum promastigotes. The six most active ones (2, 4, 7, 13, 14, and 15) were also tested in an axenic amastigote model. In order to establish their selectivity indexes (SI) the cytotoxic effect of each compound was also assayed against Jurkat and THP-1 cell lines. Compounds 2 and 4, both with a pyridine moiety, showed a moderate antileishmanial activity with an IC50 value of 4.68 ± 0.46 and 3.03 ± 0.24μM, respectively, in the amastigote model. The activity was compared with that of standard drugs, edelfosine (IC50 = 0.82 ± 0.13μM) and miltefosine (IC50 = 2.84 ± 0.10μM). Related to selectivity, the SI of both compounds are similar to those of the standard drugs when compared against the THP-1 cell line. Moreover, compound 4 was able to reduce the number of amastigote-infected THP-1 cells to 40% of that observed in untreated controls after a 96-h period of treatment. These derivatives thus represent two new leads for further studies aimed at establishing their mechanism of action. Springer-Verlag, 2010 Moreno David Departamento de Bioquímica y Biología Molecular, Universidad de Alcalá, Carretera Madrid-Barcelona Km 33,600, 28871, Alcalá de Henares, Madrid, Spain aut Plano Daniel Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut Baquedano Ylenia Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut Jiménez-Ruiz Antonio Departamento de Bioquímica y Biología Molecular, Universidad de Alcalá, Carretera Madrid-Barcelona Km 33,600, 28871, Alcalá de Henares, Madrid, Spain aut Antonio Palop Juan Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut Sanmartín Carmen Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut Parasitology Research Springer-Verlag 108/1(2011-01-01), 233-239 0932-0113 108:1<233 2011 108 436 https://doi.org/10.1007/s00436-010-2073-x text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s00436-010-2073-x text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Moreno David Departamento de Bioquímica y Biología Molecular, Universidad de Alcalá, Carretera Madrid-Barcelona Km 33,600, 28871, Alcalá de Henares, Madrid, Spain aut NATIONALLICENCE 700 1- Plano Daniel Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut NATIONALLICENCE 700 1- Baquedano Ylenia Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut NATIONALLICENCE 700 1- Jiménez-Ruiz Antonio Departamento de Bioquímica y Biología Molecular, Universidad de Alcalá, Carretera Madrid-Barcelona Km 33,600, 28871, Alcalá de Henares, Madrid, Spain aut NATIONALLICENCE 700 1- Antonio Palop Juan Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut NATIONALLICENCE 700 1- Sanmartín Carmen Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea, 1, E-31008, Pamplona, Spain aut NATIONALLICENCE 773 0- Parasitology Research Springer-Verlag 108/1(2011-01-01), 233-239 0932-0113 108:1<233 2011 108 436 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer