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

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.

Silver-Catalyzed Cascade Cyclization of Amino-NH-1,2,3-Triazoles with 2-Alkynylbenzaldehydes: An Access to Pentacyclic Fused Triazoles

“…Broad attention has been paid to 1,2,3-triazole-containing heterocycles, which have been widely applied in the fields of medicine [ 1 , 2 , 3 , 4 , 5 ], pesticide [ 6 , 7 , 8 , 9 , 10 ], biochemistry [ 11 , 12 , 13 , 14 ], and material science [ 15 , 16 , 17 , 18 , 19 , 20 ] since the ‘Click’ triazole chemistry was founded at the beginning of this century [ 21 , 22 ]. For instance, some of the well-known drugs bearing triazole moiety are presented in Figure 1 , including A (Cefatrizine) and B (Tazobactum) as β -lactam antibiotic [ 1 , 23 , 24 , 25 , 26 , 27 ], C as anti-cancer reagent [ 23 , 28 ], D as potential nonpeptidic angiotensin (II) receptor antagonists [ 29 , 30 ], E as a toll-like receptor [ 29 , 31 ], F as a mental disorders medicine [ 32 ], and G as a wall teichoic acid active antibiotic [ 11 ].…”