Synthesis of 2- and 3-methoxy-substituted Amino Chalcone Derivatives and Eval-uation of Their Antimalarial Activity

Authors

  • Rahma Dona Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Ihsan Ikhtiarudin Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Melzi Octaviani Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Enda Mora Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Putri Johanda Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Laras Maharani Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia
  • Cindy Fatma Yunita Sekolah Tinggi Ilmu Farmasi Riau, Jalan Kamboja, Kelurahan Simpang Baru, Pekanbaru, Indonesia

DOI:

https://doi.org/10.25077/jrk.v17i2.874

Keywords:

Amino Methoxy Chalcone, Synthesis, Antimalarial, In Vitro, Hemin Polimeryzation

Abstract

This study involved the synthesis of chalcone analogues with variations in benzaldehyde (A; B; C), the characterisation of the compounds, and in vitro testing of their antimalarial activity. The aim of this study was to investigate the antimalarial potential of dimethoxy and trimethoxy amino group variations in chalcone derivatives. The synthesis was carried out using Claisen-Schmidt condensation reaction with stirring method for 7 hours at room temperature, using NaOH 40%(b/v) base catalyst and ethanol solvent p.a. The synthesised compound was purified, obtained orange yellow pure compound with yield of 19,42-50,19%. Purity tests using TLC, melting point and HPLC showed high purity. Structural characterization using UV–Vis, FT‑IR, and ¹H‑NMR spectroscopy verified the successful formation of the targeted chalcone analogue structures. Antimalarial activity test showed the compounds A, B, and C inhibited the polymerisation of hemin to β-hematin with IC50 values of 107,30 µg/mL (378,71 µM); 79,89 µg/mL (282 µM); 57,47 µg/mL (183,41 µM), respectively better than the positive control hydroxychloroquine sulfate with IC50 value of 187,02 ppm (430,9 µM). From these results, differences in the position of the methoxy group in chalcone derivatives also result in differences in antimalarial activity, with compound C showing better inhibitory potential, followed by B and A respectively

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Published

2026-09-30

How to Cite

Dona, R., Ikhtiarudin, I., Octaviani, M., Mora, E., Johanda, P., Maharani, L., & Yunita, C. F. (2026). Synthesis of 2- and 3-methoxy-substituted Amino Chalcone Derivatives and Eval-uation of Their Antimalarial Activity . Jurnal Riset Kimia, 17(2), 51–62. https://doi.org/10.25077/jrk.v17i2.874

Issue

Vol. 17 No. 2 (2026): September

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