Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases

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作者
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
Jiang-Shiou Hwang
机构
[1] University of Science & Technology,Division of Entomology, Department of Zoology, School of Life Sciences
[2] Techno City,Department of Biology, Faculty of Science
[3] Bharathiar University,Department of Zoology
[4] University of Tabuk,Department of Chemistry
[5] Kongunadu Arts and Science College,Grupo de Investigación en Bioquímica y Microbiología (GIBIM). Escuela de Química
[6] Thiruvalluvar University,Centro de Investigaciones en Enfermedades Tropicales
[7] Universidad Industrial de Santander,CINTROP, Facultad de Salud, Escuela de Medicina, Departamento de Ciencias Básicas
[8] Universidad Industrial de Santander,School of Life Science
[9] Shanxi University,Computational Biology Lab, Department of Bioinformatics
[10] Bharathiar University,Institute of Marine Biology
[11] National Taiwan Ocean University,Center of Excellence for Ocean Engineering
[12] National Taiwan Ocean University,Center of Excellence for the Oceans
[13] National Taiwan Ocean University,undefined
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摘要
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.
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