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

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.

MOLECULES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Año: 2022 vol. 27

1420-3049

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.