Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives as potential SSRIs

Cu(BF4)2/AC-Catalyzed Synthesis of N-Substituted Anilines, N-Substituted 1,6-Naphthyridin-5(6H)-one, and Isoquinolin-1(2H)-one

“…Substituted isoquinolinones and naphthyridinones form an important class of compounds in the pharmaceutical industry. , Particularly, substituted isoquinolin-1­(2 H )-one, which constitutes the core scaffold of marketed or reported small molecular inhibitors, such as Duvelisib, compound 4 , and Eganelisib, made this heterocycle a popular pharmacophore for synthetic chemists (Scheme , compounds 1 , 3 , and 4 ). − Naphthyridinone also acted as a small molecular inhibitor against some medicinal targets (compounds 2 , 5 , 6 ). − The Ullmann coupling reaction or multistep cyclization are commonly used to construct N -phenyl-isoquinolinone segments. , However, these suffer from several limitations, such as expensive copper salts, air-sensitive ligands, and harsh reaction conditions, thus hampering the application of conventional synthetic methods…”

“… 3 − 5 Naphthyridinone also acted as a small molecular inhibitor against some medicinal targets (compounds 2 , 5 , 6 ). 6 − 8 The Ullmann coupling reaction or multistep cyclization are commonly used to construct N -phenyl-isoquinolinone segments. 9 , 10 However, these suffer from several limitations, such as expensive copper salts, air-sensitive ligands, and harsh reaction conditions, thus hampering the application of conventional synthetic methods.…”

Kinetic Characteristics of Curcumin and Germacrone in Rat and Human Liver Microsomes: Involvement of CYP Enzymes

“…The liver microsomes are rich in CYP, associating with drug metabolism and biotransformation [ 15 , 16 ]. The candidate drugs pharmacokinetic properties and characteristics in vivo can be predicted through detecting the metabolic rates and enzyme kinetics characteristics in vitro [ 17 , 18 , 19 ]. It is of great significance to clarify the metabolic enzyme subtypes of drugs in liver microsomal metabolism in vitro, and the mechanisms of drugs combine to achieve synergistic effects and detoxification [ 20 , 21 , 22 ].…”

“…It is of great significance to clarify the metabolic enzyme subtypes of drugs in liver microsomal metabolism in vitro, and the mechanisms of drugs combine to achieve synergistic effects and detoxification [20][21][22]. According to the literatures, curcumin has been evaluated the metabolites with an 18 O isotope labeling strategy in HLMs [23]. The interaction of zederone and germacrone with the main human liver CYPs, the sensor regulators, and the potential protected effect for liver were explored [24].…”

Visible Light-Promoted Radical Relay Cyclization/C–C Bond Formation of N-Allylbromodifluoroacetamides with Quinoxalin-2(1H)-ones

“…We envisaged that the radical intermediate generated from the visible light-promoted cyclization of allylbromodifluoroacetamides could be captured by quinoxalin-2­(1 H )-ones via a radical relay addition process. It is worth noting that molecular hybridization is a frequently employed strategy in medicinal chemistry for designing multitarget drug candidates for complex diseases in which two pharmacophoric moieties were combined to produce a new hybrid compound with improved affinity and efficacy . Following this rationale, it is quite appealing and interesting to rationally merge the pharmaceutically important partners quinoxalin-2­(1 H )-ones and γ-lactams into one molecule through an efficient synthetic method, which may result in attractive properties for drug discovery.…”