We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
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.
- Authors
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-Shar'i, Nizar A.; Morsy, Mohamed A.
- 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.
- Subjects
ANOPHELES arabiensis; INSECT growth regulators; MALARIA; MOSQUITOES; STRUCTURE-activity relationships
- Publication
Molecules, 2022, Vol 27, Issue 9, p2676
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules27092676