Benzophenone-Based Farnesyltransferase Inhibitors with High Activity against Trypanosoma cruzi was written by Esteva, Monica I.;Kettler, Katja;Maidana, Cristina;Fichera, Laura;Ruiz, Andres M.;Bontempi, Esteban J.;Andersson, Bjoern;Dahse, Hans-Martin;Haebel, Peter;Ortmann, Regina;Klebe, Gerhard;Schlitzer, Martin. And the article was included in Journal of Medicinal Chemistry in 2005.Category: piperazines This article mentions the following:
Less toxic drugs are needed to combat the human parasite Trypanosoma cruzi (Chagas’s disease). One novel target for antitrypanosomal drug design is farnesyltransferase. Several farnesyltransferase inhibitors based on the benzophenone scaffold were assayed in vitro and in vivo with the parasite. The common structural feature of all inhibitors is an amino function which can be protonated. Best in vitro activity (LC50 values 1 and 10 nM, resp.) was recorded for the R-phenylalanine derivative 4a and for the N-propylpiperazinyl derivative 2f. These inhibitors showed no cytotoxicity to cells. When tested in vivo, the survival rates of infected animals receiving the inhibitors at 7 mg/kg body weight/day were 80 and 60% at day 115 postinfection, resp. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics