1,2,3-Triazolyl-tetrahydropyrimidine conjugates as potential Sterol Carrier Protein-2 Inhibitors: Larvicidal activity against the Malaria Vector Anopheles arabiensis and In Silico Molecular Docking Study

Alteration of insect growth regulators by the action of inhibitors is becoming an attractive strategy to combat disease-transmitting insects. In the present study, we investigated the larvicidal effect of 1,2,3-triazolyl-pyrimidinone derivatives against the larvae of the mosquito Anopheles arabiensi...

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Detalles Bibliográficos
Autores: Venugopala, Katharigatta N., Shinu, Pottathil, Tratrat, Christophe, Deb, Pran Kishore, Gleiser, Raquel M., Chandrashekharappa, Sandeep, Chopra, Deepak, Attimarad, Mahesh, Nair, Anroop B., Sreeharsha, Nagaraja, Mahomoodally, Fawzi M., Haroun, Michelyne, Kandeel, Mahmoud, Asdaq, Syed Mohammed Basheeruddin, Mohanlall, Viresh, Al-Shari, Nizar A., Morsy, Mohamed A.
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/200568
Acceso en línea:http://hdl.handle.net/11336/200568
Access Level:acceso abierto
Palabra clave:ANOPHELES ARABIENSIS
BIGINELLI REACTION
CLICK CHEMISTRY
IN SILICO DOCKING
MOLECULAR HYBRIDIZATION
MOSQUITO LARVICIDAL ACTIVITY
PYRIMIDINE
STEROL CARRIER PROTEIN-2
TRIAZOLE
https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
Descripción
Sumario:Alteration of insect growth regulators by the action of inhibitors is becoming an attractive strategy to combat disease-transmitting insects. In the present study, we investigated the larvicidal effect of 1,2,3-triazolyl-pyrimidinone derivatives against the larvae of the mosquito Anopheles arabiensis, a vector of malaria. All compounds demonstrated insecticidal activity against mosquito larvae in a dose-dependent fashion. A preliminary study of the structure–activity relationship indicated that the electron-withdrawing substituent in the para position of the 4-phenyl-pyrimidinone moiety enhanced the molecules’ potency. A docking study of these derivatives revealed favorable binding affinity for the sterol carrier protein-2 receptor, a protein present in the intestine of the mosquito larvae. Being effective insecticides against the malaria-transmitting Anopheles arabiensis, 1,2,3-triazole-based pyrimidinones represent a starting point to develop novel inhibitors of insect growth regulators.

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