1. Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases
- Author
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Kadarkarai Murugan, Chellasamy Panneerselvam, Jayapal Subramaniam, Manickam Paulpandi, Rajapandian Rajaganesh, Murugan Vasanthakumaran, Jagannathan Madhavan, S. Syed Shafi, Mathath Roni, Johan S. Portilla-Pulido, Stelia C. Mendez, Jonny E. Duque, Lan Wang, Al Thabiani Aziz, Balamurugan Chandramohan, Devakumar Dinesh, Shanmughavel Piramanayagam, and Jiang-Shiou Hwang
- Subjects
Medicine ,Science - Abstract
Abstract Mosquito borne diseases are on the rise because of their fast spread worldwide and the lack of effective treatments. Here we are focusing on the development of a novel anti-malarial and virucidal agent with biocidal effects also on its vectors. We have synthesized a new quinoline (4,7-dichloroquinoline) derivative which showed significant larvicidal and pupicidal properties against a malarial and a dengue vector and a lethal toxicity ranging from 4.408 µM/mL (first instar larvae) to 7.958 µM/mL (pupal populations) for Anopheles stephensi and 5.016 µM/mL (larva 1) to 10.669 µM/mL (pupae) for Aedes aegypti. In-vitro antiplasmodial efficacy of 4,7-dichloroquinoline revealed a significant growth inhibition of both sensitive strains of Plasmodium falciparum with IC50 values of 6.7 nM (CQ-s) and 8.5 nM (CQ-r). Chloroquine IC50 values, as control, were 23 nM (CQ-s), and 27.5 nM (CQ-r). In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. The quinoline compound showed significant activity against the viral pathogen serotype 2 (DENV-2). In vitro conditions and the purified quinoline exhibited insignificant toxicity on the host system up to 100 µM/mL. Overall, 4,7-dichloroquinoline could provide a good anti-vectorial and anti-malarial agent.
- Published
- 2022
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