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
Synthesis of 3,4-Dihydropyrimidin(thio)one Containing Scaffold
The interest in 3,4-dihydropyrimidine-2(1H)-(thio)ones is increasing every day, mainly due to their paramount biological relevance. The Biginelli reaction is the classical approach to reaching these scaffolds, although the product diversity suffers from some limitations. In order to overcome these restrictions, two main approaches have been devised. The first one involves the modification of the conventional components of the Biginelli reaction and the second one refers to the postmodification of the Biginelli products. Both strategies have been extensively revised in this manuscript. Regarding the first one, initially, the modification of one of the components was covered. Although examples of modifications of the three of them were described, by far the modification of the keto ester counterpart was the most popular approach, and a wide variety of different enolizable carbonylic compounds were used; moreover, changes in two or the three components were also described, broadening the substitution of the final dihydropyrimidines. Together with these modifications, the use of Biginelli adducts as a starting point for further modification was also a very useful strategy to decorate the final heterocyclic structure.
  • 1.3K
  • 15 Aug 2022
Topic Review
Nanostructured Antibiotics
Bacterial strains resistant to antimicrobial treatments, such as antibiotics, have emerged as serious clinical problems, necessitating the development of novel bactericidal materials. Nanostructures with particle sizes ranging from 1 to 100 nanometers have appeared recently as novel antibacterial agents, which are also known as “nanoantibiotics”. Nanomaterials have been shown to exert greater antibacterial effects on Gram-positive and Gram-negative bacteria across several studies. Antibacterial nanofilms for medical implants and restorative matters to prevent bacterial harm and antibacterial vaccinations to control bacterial infections are examples of nanoparticle applications in the biomedical sectors. The development of unique nanostructures, such as nanocrystals and nanostructured materials, is an exciting step in alternative efforts to manage microorganisms because these materials provide disrupted antibacterial effects, including better biocompatibility, as opposed to minor molecular antimicrobial systems, which have short-term functions and are poisonous.
  • 1.0K
  • 10 Nov 2022
Topic Review
Targeting p53-MDM2 Interaction for Cancer Drug Discovery
Named as the guardian of the genome, p53 is a tumor suppressor that regulates cell function, often through many different mechanisms such as DNA repair, apoptosis, cell cycle arrest, senescence, metabolism, and autophagy. One of the genes that p53 activates is MDM2, which forms a negative feedback loop since MDM2 induces the degradation of p53. When p53 activity is inhibited, damaged cells do not undergo cell cycle arrest or apoptosis. As 50% of human cancers inactivate p53 by mutation, current research focuses on reactivating p53 by developing drugs that target the p53-MDM2 interaction, which includes the binding of MDM2 and phosphorylation of p53.
  • 1.2K
  • 22 Jul 2022
Topic Review
Copper-Catalyzed Intramolecular Borylative Coupling with Imines
Copper-catalyzed enantioselective borylative cyclization with various electrophiles via difunctionalization of unsaturated hydrocarbons is a powerful tool for the generation of interesting boron-containing carbocycles and heterocycles processes involving a chiral organocopper intermediate. Alkenes, allenes, and alkynes are versatile and easily accessible substrates that can be subjected to a wide range of reactions to produce densely functionalized, enantioenriched products.
  • 1.0K
  • 17 Jul 2022
Topic Review
Biocatalyzed Redox Processes Employing Green Reaction Media
Biocatalysis can be defined in a broad sense as the mediation of chemical reactions by means of biological systems, including isolated enzymes, whole cells or cell-free extracts. In some circumstances, the aqueous buffer medium normally employed in biocatalytic procedures is not the best option to develop these processes, due to solubility and/or inhibition issues, requiring biocatalyzed redox procedures to circumvent these drawbacks, by developing novel green non-conventional media, including the use of biobased solvents, reactions conducted in neat conditions and the application of neoteric solvents such as deep eutectic solvents. 
  • 738
  • 05 Jul 2022
Topic Review
Recent Advances in A3 Coupling with Metal Salts
Recent advances in the metal salt catalysed multicomponent reaction of aldehydes, amines, and alkynes, known as A3 coupling, which yields propargylamines, a valuable organic scaffold.
  • 1.4K
  • 04 Jul 2022
Topic Review
Metal-Catalyzed Synthesis of the OSe Compounds
Organoselenium (OSe) compounds have recently gained considerable interest as a potential class of organic motifs due to their outstanding applications in synthetic organic and medicinal chemistry and their possible properties in materials science. These are attributed to the exceptional properties of the selenium (Se) element.
  • 833
  • 02 Jun 2022
Topic Review
Cross-Coupling-Reaction of Copper Carbene Intermediate with Terminal Alkyne
Copper-catalyzed cross-coupling reaction of a copper carbene intermediate with terminal alkynes was one of the most powerful protocols for the construction of C–C bonds. However, in early works, a mixture of alkynoates and allenoates was generated in combined moderate yields under harsh reaction conditions. Until 2004, Fu reported the first example of the copper-catalyzed coupling reaction of terminal alkynes with diazo esters or diazo amides to yield 3-alkynoate or 3-butynamide products selectively with minimal amount of allene byproducts under no-basic conditions. Consequently, a variety of copper-catalyzed coupling reactions of terminal alkynes with various carbene precursors have been developed independently.
  • 1.3K
  • 30 May 2022
Topic Review
Theranostic Radiopharmaceuticals
Theranostic Radiopharmaceuticals (Radiotheranostics) is a term in the medical field to define the combination of therapeutic and diagnostic techniques by a suitable radiopharmaceutical agent. Radionuclides are isotopes that emit radiation or have excess nuclear energy, making them chemically unstable and tend to change into another atom. Various types of radiation can be emitted by radionuclides e.g. alpha particles, beta particles, and gamma energy. In radiotheranostics, a pharmaceutical agent (drug) is needed to be a carrier molecule that introduces the radionuclide to its target. Radionuclides are then used as a source of radiation in radiotheranostics that are responsible for diagnosing or treating various diseases.
  • 1.8K
  • 24 May 2022
Topic Review
Heteroaromatic N-Oxides in Asymmetric Catalysis
Chiral heteroaromatic N-oxides can work as powerful electron-pair donors, providing suitable electronic environments in the transition state formed within the reaction. The nucleophilicity of the oxygen atom in N-oxides, coupled with a high affinity of silicon to oxygen, represent ideal properties for the development of synthetic methodology based on nucleophilic activation of organosilicon reagents.
  • 774
  • 28 Apr 2022
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