Synthesis and antiplasmodial activity of novel phenanthroline derivatives: An in vivo study

Publish Year: 1397
نوع سند: مقاله ژورنالی
زبان: English
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شناسه ملی سند علمی:

JR_IJBMS-21-2_013

تاریخ نمایه سازی: 27 مهر 1400

Abstract:

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 ۱,۱۰-phenanthroline derivatives containing amino-alcohol and amino-ether substituents were synthesized via facile procedures, starting with ۵,۶-epoxy-۱,۱۰-phenanthroline. Their antiplasmodial activity was then evaluated using Peter's ۴-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 ۶-(۳-(dibutylamino)propylamino)-۵,۶-dihydro-۱,۱۰-phenanthroline-۵-ol (۷b) at the dose of ۱۵۰ mg/kg/day and ۴-(۱,۱۰-phenanthroline-۵-yloxy)-N,N-dipropylbutan-۱-amine (۸b) at the dose of ۱۵ mg/kg/day have ۹۰.۵۸% and ۸۸.۳۲% 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.

Keywords:

Antiplasmodial activity Malaria Plasmodium berghei Peter's test ۱ , ۱۰-Phenanthroline Quinoline

Authors

Azar Tahghighi

Malaria and Vector Research Group (MVRG), Biotechnology Research Center (BRC), Pasteur Institute of Iran, Tehran, Iran

Safoura Karimi

Malaria and Vector Research Group (MVRG), Biotechnology Research Center (BRC), Pasteur Institute of Iran, Tehran, Iran

Arezoo Rafie Parhizgar

Malaria and Vector Research Group (MVRG), Biotechnology Research Center (BRC), Pasteur Institute of Iran, Tehran, Iran

Sedigheh Zakeri

Malaria and Vector Research Group (MVRG), Biotechnology Research Center (BRC), Pasteur Institute of Iran, Tehran, Iran

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  • ۱.World Health Organization. World Malaria Report ۲۰۱۵. Geneva ۲۰۱۵. Available ...
  • ۲.Golan DE, Tashjian AH, Armstrong EJ. Principles of pharmacology: the ...
  • ۳.Enserink M. Malaria's drug miracle in danger. Science ۲۰۱۰; ۳۲۸:۸۴۴-۸۴۶ ...
  • ۴.Kappe SH, Vaughan AM, Boddey JA, Cowman AF. That was ...
  • ۵.Nosten F, Van Vugt M, Price R, Luxemburger C, Thway ...
  • ۶.Beshir K, Sutherland CJ, Merinopoulos I, Durrani N, Leslie T, ...
  • ۷.Smrkovski LL, Buck RL, Alcantara AK, Rodriguez CS, Uylangco CV. ...
  • ۸.Croft AM. A lesson learnt: the rise and fall of ...
  • ۹.ter Kuile FO, Dolan G, Nosten F, Edstein MD, Luxemburger ...
  • ۱۰.Cui L, Su XZ. Discovery, mechanisms of action and combination ...
  • ۱۱.Lim P, Alker AP, Khim N, Shah NK, Incardona S, ...
  • ۱۲.Sunjic V, Parnham MJ. Signposts to chiral drugs: organic synthesis ...
  • ۱۳.Biamonte MA, Wanner J, Le Roch KG. Recent advances in ...
  • ۱۴.Hadanu R, Mastjeh S, Jumina J, Mustofa M, Widjayanti MA, ...
  • ۱۵.Hadanu R, Matsjeh S, Jumina M, Widjayanti MA, Sholikhah EN. ...
  • ۱۶.Sholikhah EN, Supargiyono S, Jumina J, Wijayanti MA, Tahir I, ...
  • ۱۷.Wijayanti MA, Sholikhah EN, Hadanu R, Jumina J, Supargiyono S, ...
  • ۱۸.Wijayanti MA, Sholikhah EN, Tahir I, Hadanu R, Jumina J, ...
  • ۱۹.Fitriastuti D, Mardjan MID, Jumina J, Mustofa M. Synthesis and ...
  • ۲۰.Egan TJ, Koch KR, Swan PL, Clarkson C, Van Schalkwyk ...
  • ۲۱.Shahroosvand H, Abbasi P, Notash B, Najafi L. Separation of ...
  • ۲۲.Howell BA, Dumitrascu A. Thermal stability of bidendate nitrogen ligands ...
  • ۲۳.Knight DJ, Peters W. The anti-malarial activity of N-benzyloxydihydrotriazines. I. ...
  • ۲۴.Shen Y, Sullivan BP. A Versatile Preparative Route to ۵-Substituted-۱,۱۰-Phenanthroline ...
  • ۲۵.Sullivan DJ, Gluzman IY, Russell DG, Goldberg DE. On the ...
  • ۲۶.Kumar S, Guha M, Choubey V, Maity P, Bandyopadhyay U. ...
  • ۲۷.Coronado LM, Nadovich CT, Spadafora C. Malarial hemozoin: from target ...
  • ۲۸.Weissbuch I, Leiserowitz L . Interplay between malaria, crystalline hemozoin ...
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