In vitro anti-plasmodial activity of new synthetic derivatives of 1-(heteroaryl)-2- ((5-nitroheteroaryl)methylene) hydrazine
- Author:
Azar TAHGHIGHI
1
;
Akram MEHRIZI
1
;
Sedigheh ZAKERI
1
;
Azar TAHGHIGHI
2
Author Information
- Publication Type:Journal Article
- Keywords: 5-nitroheteroaryl; Acridine; Hydrazine; Plasmodium; Quinazoline; Quinoline
- From: Asian Pacific Journal of Tropical Medicine 2021;14(3):128-138
- CountryChina
- Language:Chinese
- Abstract: Objective: To evaluate new compounds synthesized by integrating quinoline, quinazoline, and acridine rings with the active moiety of (5-nitroheteroaryl) methylene hydrazine. Methods: A new series of compounds (1a, 1b, 2a, 2b, 3a, and 3b) were synthesized and evaluated for cytotoxicity against COS-7 cells using the MTT assay. In vitro anti-plasmodial activity of the compounds was measured against CQ-sensitive (3D7) and CQ-resistant (K1) Plasmodium (P.) falciparum strains. β-hematin assay was performed to assess the inhibitory effects of β-hematin formation for new compounds. Results: The synthetic compounds had anti-plasmodial activity against blood-stage of 3D7 [IC