Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.

/pdf/chalcone-a-privileged-structure-in-medicinal-chemistry-2glhtivnj7.pdf

Chalcone: A Privileged Structure in Medicinal Chemistry.

The analogs of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The number of novel N-heterocyclic moieties with significant physiological properties and promising applications in medicinal chemistry is ever-growing. In this review, we consolidate the recent advances on novel nitrogen-containing heterocycles and their distinct biological activities, reported over the past one year (2019 to early 2020). This review highlights the trends in the use of nitrogen-based moieties in drug design and the development of different potent and competent candidates against various diseases.

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications.

Nitrogen-containing heterocyclic compounds and their derivatives have historically been invaluable as a source of therapeutic agents. Pyrazole, which has two nitrogen atoms and aromatic character, provides diverse functionality and stereochemical complexity in a five-membered ring structure. In the past decade, studies have reported a growing body of data on different pyrazole derivatives and their innumerable physiological and pharmacological activities. In part, such studies attempted to reveal the wide range of drug-like properties of pyrazole derivatives along with their structure–activity relationships in order to create opportunities to harness the full potentials of these compounds. Here, we summarize strategies to synthesize pyrazole derivatives and demonstrate that this class of compounds can be targeted for the discovery of new drugs and can be readily prepared owing to recent advances in synthetic medicinal chemistry.

Review: biologically active pyrazole derivatives

"Comprehensive Heterocyclic Chemistry" was published in 1984 and is now available on CD-ROM.

Comprehensive heterocyclic chemistry on CD-ROM

The four-membered oxetane ring has been increasingly exploited for its contrasting behaviors: its influence on physicochemical properties as a stable motif in medicinal chemistry and its propensity to undergo ring-opening reactions as a synthetic intermediate. These applications have driven numerous studies into the synthesis of new oxetane derivatives. This review takes an overview of the literature for the synthesis of oxetane derivatives, concentrating on advances in the last five years up to the end of 2015. These methods are clustered by strategies for preparation of the ring and further derivatization of preformed oxetane-containing building blocks. Examples of the use of oxetanes in medicinal chemistry are reported, including a collation of oxetane derivatives appearing in recent patents for medicinal chemistry applications. Finally, examples of oxetane derivatives in ring-opening and ring-expansion reactions are described.

/pdf/oxetanes-recent-advances-in-synthesis-reactivity-and-3v6yf8rtvd.pdf

Oxetanes: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry

Arylglyoxals in synthesis of heterocyclic compounds.

Chemistry of α-oxoesters: a powerful tool for the synthesis of heterocycles.

Fe3O4@SiO2 core–shell magnetic nanoparticles (MNPs) were prepared by chemical coprecipitation of FeCl3·6H2O and FeCl2·4H2O in alkaline solution, followed by silylation using triethoxy silane, and then by treatment with 3-aminopropyltriethoxysilane. The corresponding MNPs were coated with carboxymethyl cellulose (CMC) by amide formation between carboxyl groups of CMC and amine functional groups of nanoparticles. The structure of MNPs was characterized by FT-IR, SEM, EDX, TEM, XRD, VSM and TGA analysis. CMC-coated Fe3O4@SiO2 magnetic nanoparticles were used as an efficient adsorbent for the removal of methylene blue (MB, a cationic dye) from aqueous solutions. The impact of various factors such as adsorbent dosage, pH, initial concentration of MB, temperature and contact time were investigated. The kinetic, isotherms, and thermodynamic parameters of adsorption were also studied.

Carboxymethyl cellulose coated Fe 3 O 4 @SiO 2 core–shell magnetic nanoparticles for methylene blue removal: equilibrium, kinetic, and thermodynamic studies

α-Imino esters are useful precursors for the synthesis of a variety of types of natural and unnatural α-amino acid derivatives, with a wide range of biological activities. Due to the adjacent ester group, α-imino esters are more reactive relative to other types of imines and undergo different kinds of reactions, including organometallics addition, metal catalyzed vinylation and alkynylation, aza-Henry, aza-Morita-Baylis-Hillman, imino-ene, Mannich-type, and cycloaddition reactions, as well as hydrogenation and reduction. This review discusses the mechanism, scope, and applications of the reactions of α-imino esters and related compounds in organic synthesis, covering the literature from the last 12 years.

Maryam Zirak

Papers

Arylglyoxals in synthesis of heterocyclic compounds.

Chemistry of α-oxoesters: a powerful tool for the synthesis of heterocycles.

Carboxymethyl cellulose coated Fe 3 O 4 @SiO 2 core–shell magnetic nanoparticles for methylene blue removal: equilibrium, kinetic, and thermodynamic studies

α-Imino Esters in Organic Synthesis: Recent Advances

Stereoselective synthesis of β-amino ketones via direct mannich-type reactions, catalyzed with ZrOCl2·8H2O under solvent-free conditions