RT Journal Article
T1 Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
A1 Ibáñez Escribano, Alexandra
A1 Fonseca Berzal, Cristina Rosa
A1 Martínez Montiel, Pilar
A1 Álvarez-Márquez, M
A1 Gómez-Núñez, M
A1 Lacueva-Arnedo, M
A1 Espinosa-Buitrago, T
A1 Martín-Pérez, T
A1 Escario García-Trevijano, José Antonio
A1 Merino-Montiel, P
A1 Montiel-Smith, S
A1 Gómez Barrio, Alicia
A1 López, Óscar
A1 Fernández-Bolaños, J.G.
AB Herein, we report the preparation of a panel of Schiff bases analogues as antiprotozoal agents by modification of the stereoelectronic effects of the substituents on N-1 and N-4 and the nature of the chalcogen atom (S, Se). These compounds were evaluated towards Trypanosoma cruzi and Trichomonas vaginalis. Thiosemicarbazide 31 showed the best trypanocidal profile (epimastigotes), similar to benznidazole (BZ): IC50 (31)=28.72 μM (CL-B5 strain) and 33.65 μM (Y strain), IC50 (BZ)=25.31 μM (CL-B5) and 22.73 μM (Y); it lacked toxicity over mammalian cells (CC50 > 256 µM). Thiosemicarbazones 49, 51 and 63 showed remarkable trichomonacidal effects (IC50 =16.39, 14.84 and 14.89 µM) and no unspecific cytotoxicity towards Vero cells (CC50 ≥ 275 µM). Selenoisosters 74 and 75 presented a slightly enhanced activity (IC50=11.10 and 11.02 µM, respectively). Hydrogenosome membrane potential and structural changes were analysed to get more insight into the trichomonacidal mechanism.
PB Taylor & Francis Online
YR 2022
FD 2022-02-07
LK https://hdl.handle.net/20.500.14352/102828
UL https://hdl.handle.net/20.500.14352/102828
LA eng
NO MCIN/AEI/10.13039/501100011033,
NO UCM Research Group 911120
NO Mexican CONACYT
NO Junta de Andalucia (FQM-134)
DS Docta Complutense
RD 4 abr 2025