Synthesis, SAR studies, and insecticidal activities of certain N-heterocycles derived from 3-((2-chloroquinolin-3-yl)methylene)-5-phenylfuran-2(3H)-one against Culex pipiens L. larvae

Abstract

A new series of N-heterocycles including pyridazinone, oxadiazole, triazolopyridazinone, and triazole derivatives were synthesized from the acid hydrazide via its reaction with certain carbon electrophiles.

Synthesis, toxicological and in silico evaluation of novel spiro pyrimidines against Culex pipiens L. referring to chitinase enzyme

“…It was suggested that the benzene plane forms a special face-to-edge aromatic interaction with the amino acids of a target site. These aromatic moieties increase the hydrophobicity of compounds, which enhances their permeability through the insect integument, thereby increasing insecticidal activity 34 . The substitution of aromatic carboxamide moieties resulted in higher inhibition of Ostrinia furnacalis chitinase h ( Of Chi-h) in contrast to the insertion of non-aromatic moieties.…”

Larvicidal evaluation of two novel cationic gemini surfactants against the potential vector of West Nile virusCulex pipiensLinnaeus (Diptera: Culicidae)

“…Cationic gemini surfactants are a novel class of cationic surfactants; they consist of two identical cationic surfactants (i.e., two identical hydrophilic head groups and two hydrophobic tail-groups [fatty acids] that are separated by a covalent spacer; Labena et al, 2020). The head groups have two electron-withdrawing Cl À atoms with high electronegativity, which draw the electrons and increase the electropositivity of two quaternary ammonium salts (R 4 N + ) (Ramadan et al, 2022) that facilitate the attack on nitrogen atoms by nucleophilic agents such as AChE and nAChR, thus contributing to significant enhancing of the binding with the active site of the enzymes (Wang et al, 2014;Wibowo et al, 2017;Tantawy et al, 2022).…”

Some pyrimidohexahydroquinoline candidates: synthesis, DFT, cytotoxic activity evaluation, molecular docking, and in silico studies

“…22,23 This electron-withdrawing head plays a substantial role in the binding interactions with the receptor subsites via van der Waals interactions and hydrogen bonding. 10 To design a new series of some hexahydroquinoline derivatives, fundamental pharmacophoric features of quinoline were retained while integrating heterocyclic and side chain moieties as follows: (i) a planar aromatic core (chromophore) associated with the active sites of enzymes was retained in their design, which displayed pi-hydrophobic or pi-pi interactions with amino acid residues; (ii) the linker was altered by adding heteroatoms like nitrogen (N), oxygen (O), and sulfur (S) to demonstrate more hydrogen bonding through interactions with tumor proteins; (iii) to enhance the antiproliferative potential, cores of pyrimidine, pyridine, indoline, thiazolidine, and phenyl were included in the design. With these features, this work intended to create some new hexahydroquinoline derivatives with enhanced antiproliferative properties.…”

“…1. [9][10][11][12][13][14][15][16][17][18][19][20][21] Therefore, this work describes the design and preparation of certain pyrimidohexahydroquinolines with potential antiproliferative effects, reinforced by computational chemical approach and molecular docking, which might serve as a drug development target.…”