title: Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents.
abstract: A series of novel 4-arylthiazolylhydrazones (TZHs) derived from 1-indanones were synthesized in good yields (66-92%) in a simple procedure using microwave irradiation and then characterized by spectroscopy studies. The compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against the epimastigote, trypomastigote and amastigote forms of the parasite. Most TZHs displayed excellent activity, and were more potent and selective than the reference drug Benznidazole, used in the current chemotherapy. Analysis of the free sterols from parasite incubated with the compounds showed that inhibition of ergosterol biosynthesis is a possible target for the action of these new TZHs. In particular, TZH 9 emerged as a promising antichagasic compound to be evaluated in animal models.
authors: Química Medicinal, Departamento de Farmacología, Facultad de Farmacia y Bioquímica., Universidad de Buenos Aires, Junín 956, 1113, Ciudad Autónoma de Buenos Aires, Argentina.
authors: María E
authors: ME
authors: Caputto
authors: Alejandra
authors: A
authors: Ciccarelli
authors: Fernanda
authors: F
authors: Frank
authors: Albertina G
authors: AG
authors: Moglioni
authors: Graciela Y
authors: GY
authors: Moltrasio
authors: Daniel
authors: D
authors: Vega
authors: Elisa
authors: E
authors: Lombardo
authors: Liliana M
authors: LM
authors: Finkielsztein
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D002522:Chlorocebus aethiops; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D008018:Life Cycle Stages / Q000187:drug effects; D013261:Sterols / Q000096:biosynthesis; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D014709:Vero Cells
chemical_list: D000981:Antiprotozoal Agents; D006835:Hydrazones; D013261:Sterols