Synthesis and antiplasmodial activity of novel phenanthroline derivatives: An in vivo study | ||
| Iranian Journal of Basic Medical Sciences | ||
| مقاله 13، دوره 21، شماره 2، اردیبهشت 2018، صفحه 202-211 اصل مقاله (1.09 M) | ||
| نوع مقاله: Original Article | ||
| شناسه دیجیتال (DOI): 10.22038/ijbms.2017.24558.6106 | ||
| نویسندگان | ||
| Azar Tahghighi* 1؛ Safoura Karimi1، 2؛ Arezoo Rafie Parhizgar1، 2؛ Sedigheh Zakeri1 | ||
| 1Malaria and Vector Research Group (MVRG), Biotechnology Research Center (BRC), Pasteur Institute of Iran, Tehran, Iran | ||
| 2Department of Medicinal Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran | ||
| چکیده | ||
| Objective(s): Due to the rapid increased drug resistance to Plasmodium parasites, an urgent need to achieve new antiplasmodial drugs is felt. Therefore, in this study, the new synthetic phenanthroline derivatives were synthesized with antiplasmodial activity. Materials and Methods: A series of 1,10-phenanthroline derivatives containing amino-alcohol and amino-ether substituents were synthesized via facile procedures, starting with 5,6-epoxy-1,10-phenanthroline. Their antiplasmodial activity was then evaluated using Peter's 4-day suppressive test against Plasmodium berghei-infected mice (ANKA strain). Furthermore, the mean survival time of the mice treated with synthetic compounds was compared with the negative control group. Results: The results demonstrated that the compounds 6-(3-(dibutylamino)propylamino)-5,6-dihydro-1,10-phenanthroline-5-ol (7b) at the dose of 150 mg/kg/day and 4-(1,10-phenanthroline-5-yloxy)-N,N-dipropylbutan-1-amine (8b) at the dose of 15 mg/kg/day have 90.58% and 88.32% suppression, respectively. All synthetic compounds prolonged the mean survival time of treated mice in comparison with negative control groups, indicating the in vivo antiplasmodial activity of these new compounds. Conclusion: The present study is the first attempt to achieve new, effective synthetic compounds based on phenanthroline scaffold with the antiplasmodial activity. However, more research is needed to optimize their antimalarial activity. | ||
| کلیدواژهها | ||
| Antiplasmodial activity Malaria Plasmodium berghei Peter's test 1؛ 10-Phenanthroline Quinoline | ||
| مراجع | ||
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