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
Katharigatta N. Venugopala, Pottathil Shinu, Christophe Tratrat, Pran Kishore Deb, Raquel M. Gleiser, Sandeep Chandrashekharappa, Deepak Chopra, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Mohamad Fawzi Mahomoodally, Michelyne Haroun, Mahmoud Kandeel, Syed Mohammed Basheeruddin Asdaq, Viresh Mohanlall, Nizar A. Al‐Shar’i, Mohamed A. Morsy
Abstract
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.