Synthesis biological studies of some new heterocyclic compound derived from 2-chloro-3-formyl quinoline and 4-(benzyl sulfonyl) acetophenone

Abstract

A new series of quinoline chalcones have been prepared from condensations of 2-chloro-3-formyl quinoline (1) with 4-(benzothio) acetophenone(2) and 4-(benzyl sulfonyl) acetophenone(3). The reaction of chalcones(4,5) with bromine gives dibromide(6,7). New pyrazoline derivatives were synthesized by condensation of chalcones (4 or 5) with hydrazine hydrate to give (8,9) and with hydrazine hydrate in glacial acetic acid(gla) to give (10,11) and with phenyl hydrazine to give (12,13). The prepared chalcones (4,5) and dibromide(6,7) and pyrazoline derivative (8-13)have been screened for antibacterial activities against two gram positive staphylococcus aureus and staphylococcus epidermidis and two gram negative Escherichia coli and Proteus vulgaris. The synthesized compounds are proven by IR & NMR spectral and physical method.

Preparation of New Complexes from a Mixture of Aspirin (acetylsalicylic acid), Paracetamol and Methyldopa with Divalent Manganese , Iron, Cobalt, Nickel and Copper, With a Study of Their Physical and Chemical Properties.

“…Aspirin (acetylsalicylic acid ) ligand spectrum shows bands at 1304, 1679 cm-1 which may be assigned to (C-N) and cyano group (C=N) groups respectively [24,25] . The band of (C-O) appeared at [26,27] .…”

Identification of naphthyridine and quinoline derivatives as potential Nsp16-Nsp10 inhibitors: a pharmacoinformatics study

“…Molecular docking is one of the most widely used structure-based approaches for identifying novel binders by estimating their binding mode and affinity. In the current effort, a set of 58 compounds recently synthesized by our research group (Saleh et al, 2020) were screened through a molecular docking study against the Nsp16-Nsp10 protein. In the dataset, 10 compounds belong to the 2-chloro-3-formyl quinoline and the remaining belong to the 2-chloro-3-formyl-1,8-Naphthyridine (Saleh et al, 2020).…”

“…In the current effort, a set of 58 compounds recently synthesized by our research group (Saleh et al, 2020) were screened through a molecular docking study against the Nsp16-Nsp10 protein. In the dataset, 10 compounds belong to the 2-chloro-3-formyl quinoline and the remaining belong to the 2-chloro-3-formyl-1,8-Naphthyridine (Saleh et al, 2020). After synthesis, the molecular structures were generated using a molecular drawing tool and subsequently optimized through the density functional theory (DFT) (Becke, 1988) at B3LYP/SDD level implemented in Gaussian09 (Frisch et al, 2016).…”

“…Similarly, quinoline is belonged to the class of nitrogen heterocyclic compounds and possess anti-malarial, anti-inflammatory, antibacterial, anticancer, anti-microbial, anthelmintic and anti-fungal types of biological activities (Amer et al, 2018;Cocco et al, 2000;Mukherjee et al, 2001;Narender et al, 2005). For instance, the 1,8-naphthyridine and quinoline (Saleh et al, 2020) represent a core for several vital drugs included Gemiflloxacin (antimicrobial) (Marchese et al, 2000) and anticonvulsants (Leonard et al, 2002). Beyond above, molecules containing naphthyridine and quinoline scaffolds are also used for dementia (Mekheimer et al, 2007) and cancer therapy (Jiang et al, 2006).…”

“…Therefore, in the current study, the major efforts were undertaken to identify the novel small molecules that belong to naphthyridine and quinoline derivatives. The molecular docking study was performed on a set of naphthyridine and quinoline derivatives, recently synthesized by our research group (Saleh et al, 2020). Further, in silico pharmacokinetics assessment was carried out and finally conventional all-atoms molecular dynamics (MD) simulation was performed.…”