Summary

Organic synthesis is the tool for the preparation of small molecules with interesting biological and medicinal properties—new compounds with activity against diseases affecting humankind today such as cancer, metabolic disorders, neurodegenerative disorders or infectious diseases, as well as new syntheses of known drugs. New bioactive compounds are designed and synthesized to target key metabolic reactions in pathological processes as the first steps toward drug discovery. The crosstalk between synthetic and medicinal chemists enable a high impact of new synthetic methodologies in drug discovery. The aim is to highlight the role that organic synthesis plays in developing methods that may be exploited for finding lead compounds and drugs by the pharmaceutical industry.

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Topic Review
Ivacaftor (VX-770)
Ivacaftor possesses a molecular structure characterized by the presence of an N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxamide moiety. The quinolone scaffold within its composition is a crucial pharmacophore, significantly influencing drug discovery. This scaffold holds prominence as one of the primary classes of nitrogen-containing heterocycles found in various biologically active compounds and blockbuster drugs, as highlighted in the literature. The amide group serves as a crucial link between the “privileged building block” and the di-tert-butylphenol in ivacaftor’s structure. This linkage is of considerable importance in medicinal chemistry due to its multifaceted role.
  • 250
  • 17 Feb 2024
Topic Review
Industrial Applications of Microfluidic Systems
With the proliferation of microelectromechanical systems (MEMS) technology, the syntheses of microfluidic devices or microdroplets have become increasingly important as tools for chemical analysis and synthesis. Microfluidic devices (microreactors, microchemical chips, etc.) that integrate the functions of chemical synthesis, analysis equipment, and chemical plants in a compact form are being investigated.
  • 335
  • 26 Jan 2024
Topic Review
Green Synthesis of Nanoparticles from WPCBs
Waste printed circuit boards (WPCBs), constituting approximately 10% of all electronic waste (e-waste), are particularly intriguing due to their high content of valuable metals and rare earth elements.
  • 223
  • 15 Jan 2024
Topic Review
Flavonoids as Visible Light Photoinitiators
The design of biosourced and/or bioinspired photoinitiators is an active research field as it offers a unique opportunity to develop photoinitiating systems exhibiting better biocompatibility as well as reduced toxicity. In this field, flavonoids can be found in numerous fruits and vegetables so these structures can be of interest for developing, in the future, polymerization processes, offering a reduced environmental impact but also better biocompatibility of the polymers.
  • 233
  • 29 Dec 2023
Topic Review
Methods of Preparation of Quinoxalines
Quinoxaline is a fused heterocycle system of a benzene ring and pyrazine ring. It has earned considerable attention due to its importance in the field of medicinal chemistry. The system is of extensive importance due to its comprehensive array of biological activities. Quinoxaline derivatives have been used as anticancer, anticonvulsant, anti-inflammatory, antidiabetic, antioxidant, antibacterial, anti-TB, antimalarial, antiviral, anti-HIV, and many other uses. Variously substituted quinoxalines are significant therapeutic agents in the pharmaceutical industry.
  • 810
  • 23 Nov 2023
Topic Review
Molecular Hybridization of Alkaloids Using 1,2,3-Triazole-Based Click Chemistry
Alkaloids found in multiple species, known as ‘driver species’, are more likely to be included in early-stage drug development due to their high biodiversity compared to rare alkaloids. Many synthetic approaches have been employed to hybridize the natural alkaloids in drug development. Click chemistry is a highly efficient and versatile reaction targeting specific areas, making it a valuable tool for creating complex natural products and diverse molecular structures. It has been used to create hybrid alkaloids that address their limitations and serve as potential drugs that mimic natural products.
  • 342
  • 22 Nov 2023
Topic Review
C–H Functionalisation
C–H bond functionalisation describes the transformation of a C-H bonds into a C-X bonds (X = C, N, O, B, halides, among many others). The term is typically associated with transition metals in processes like C-H activation. However, other methods such as nitrene/carbene insertion and hydrogen atom transfer (HAT) can also be used to functionalise C-H bonds with varying selectivity and ability to introduce different functional groups depending on the method used. 
  • 326
  • 09 Nov 2023
Topic Review
Synthesis of Monoterpene Thiols
Thiols are one of the most convenient synthons in the synthesis of organosulfur compounds. The typical methods to prepare monoterpene thiols include the electrophilic addition of H2S or dithiols to the double bond of monoterpenes; nucleophilic substitution of halides; tosylates/mesylates obtained from corresponding monoterpene alcohols; thia-Michael addition of S-nucleophiles to α,β-unsaturated ketones; nucleophilic epoxide ring opening; nucleophilic substitution of the activated methylene protons; and reduction of sulfochlorides, dithiolanes, thiiranes, and sultones.
  • 399
  • 07 Nov 2023
Topic Review
Biosynthesis of Aurones
Natural products are a boundless source for the development of pharmaceutical agents against a wide range of human diseases. Accordingly, naturally occurring aurones possess various biological benefits, such as anticancer, antioxidant, antimicrobial, antidiabetic, anti-inflammatory, antiviral and neuroprotective effects. In addition, various studies have revealed that aurones are potential templates for the regulation of diabetes mellitus and its associated complications. Likewise, certain aurones and their analogues have been found to be remarkable kinase inhibitors of DARK2, PPAR-γ, PTPM1, AGE, α-amylase and α-glucosidase, which represents a promising approach for the treatment of chronic metabolic disorders such as diabetes. 
  • 472
  • 01 Nov 2023
Topic Review
Covalent Organic Frameworks Solid-State Electrolytes
Covalent organic frameworks (COFs) have emerged as a promising platform of materials for solid-state battery electrolytes due to their porous and robust structures, and their special spaces such as 1D and 3D, as well as their ability to be modified with functional groups. 
  • 439
  • 16 Oct 2023
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