Chalcone analogue as potent anti-malarial compounds against Plasmodium falciparum: Synthesis, biological evaluation, and docking simulation study
10.1016/j.apjtb.2017.07.004
- Author:
Jufrizal SYAHRI
1
;
Jufrizal SYAHRI
2
;
Emmy YUANITA
2
;
Beta Achromi NUROHMAH
2
;
Ria ARMUNANTO
2
;
Bambang PURWONO
2
;
Emmy YUANITA
3
Author Information
1. Department of Chemistry, Universitas Muhammadiyah Riau
2. Department of Chemistry, Universitas Gadjah Mada
3. Department of Chemistry, Universitas Mataram
- Publication Type:Journal Article
- Keywords:
Antimalarial;
Chalcone;
Docking;
Plasmodium falciparum 3D7
- From:Asian Pacific Journal of Tropical Biomedicine
2017;7(8):675-679
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate in vitro antimalarial activity of chalcone derivative compounds against Plasmodium falciparum 3D7 (Pf3D7) strain and in silico antimalarial activity. Methods Synthesis of the chalcone derivatives was conducted via Claisen-Schmidt method using NaOH 60% base as catalyst. An in vitro antimalarial activity assay was carried out according to the Rieckmann method against the chloroquine-sensitive Pf3D7 strain. Molecular docking studies of the prepared compounds were performed using Discovery Studio 3.1 (Accelrys, Inc., San Diego, USA) software to dihydrofolate reductases–thymidylate synthase (PfDHFR-TS) protein with Protein Data Bank ID of 1J3I.pdb (sensitive-protein) and ID: 4DP3.pdb (resistance-protein). Results This work has successfully synthesized seven chalcone derivatives with a great antimalarial activity. It has been revealed that allyloxy, hydroxy and alkoxy functional groups could increase the antimalarial activity of the chalcone derivatives. The best antimalarial activity of the prepared compounds was possessed by 3b with an IC
