1383956-99-7Relevant academic research and scientific papers
Synthesis of novel polysubstituted (2SR,4RS)-2-heteroaryltetrahydro-1,4- epoxy-1-benzazepines and cis-2-heteroaryl-4-hydroxytetrahydro-1H-1-benzazepines as antiparasitic agents
Blanco, María C.,Escobar, Patricia,Leal, Sandra M.,Bahsas, Alí,Cobo, Justo,Nogueras, Manuel,Palma, Alirio
, p. 291 - 309 (2014)
New series of polysubstituted (2SR,4RS)-2-heteroaryltetrahydro-1,4-epoxy-1- benzazepines and cis-2-heteroaryl-4-hydroxytetrahydro-1H-1-benzazepines were designed and synthesized in moderate to high yields using a three-step procedure from ortho-allylanilines. Their antiparasitic activity was evaluated against the extracellular and intracellular forms of Trypanosoma cruzi and Leishmania (Leishmania) infantum parasites. Their cytotoxicity was also determined on Vero and THP-1 mammalian cells. Many of the tested compounds inhibited significantly the growth of extracellular forms of T. cruzi and L. (L.) infantum without showing cytotoxicity on Vero and HTP-1 cells. Only compounds 10h and 14f demonstrated good activity against amastigotes of T. cruzi, but none was able to inhibit the growth of L. (L.) infantum amastigotes.
