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
Ni-Based Bimetallic Catalysts
Metallic Ni shows high activity for a variety of hydrogenation reactions due to its intrinsically high capability for H2 activation, but it suffers from low chemoselectivity for target products when two or more reactive functional groups are present on one molecule. Modification by other metals changes the geometric and electronic structures of the monometallic Ni catalyst, providing an opportunity to design Ni-based bimetallic catalysts with improved activity, chemoselectivity, and durability.
  • 635
  • 07 Feb 2022
Topic Review
Luminescent Micelles for Sensing Nitroaromatic and Nitramine Explosives
Luminescent micelles are extensively studied molecular scaffolds used in applied supramolecular chemistry.
  • 617
  • 28 Jan 2022
Topic Review
Heterocyclic Crown Ethers
Crown ethers are heterocyclic compounds present as cyclic oligomers in their simple form. These are extremely versatile compounds exhibiting higher binding affinity towards metal ions, including s-block and transition metal ions. For example, 18-crown-6 has a cavity that fits the size of 4f transition metal ions and has reflected exceptional attraction for complexation with the lanthanide ions.
  • 1.3K
  • 27 Jan 2022
Topic Review
The Rearrangement of Alkylallenes to 1,3-Dienes
1,3-Dienes are vital building blocks in organic synthesis. They underpin many fundamental synthetic transformations and are present in numerous natural products and drug candidate molecules.
  • 691
  • 19 Jan 2022
Topic Review
New Antimicrobial Oleanonic Acid Polyamine Conjugates
The series of 21 oleanolic acid derivatives containing di- and polyamine fragments at position C3 and C28 was synthesized and evaluated for their antimicrobial activities against both Gram-positive and Gram-negative bacterial. Almost all series presented good to moderate Minimum Inhibitory Concentrations (MIC) against Gram-positive S. aureus, S. faecalis and B. cereus bacteria, moreover compounds possess important antimicrobial activities against Gram-negative E. coli, P. aeruginosa, S. enterica, and EA289 bacteria with MICs ranging from 6.25 to 200 µg/mL. The SAR data showed that the nature of the polyamine fragment, as well as differences in the structure of oleanolic acid plays an important role in the potential activities of tested compounds. The testing of the ability to restore the antibiotic activity of doxycycline and erythromycin at a 2 µg/mL concentration in a synergistic assay showed that only Mannich base with spermine fragment 6 lead to a moderate improvement in terms of antimicrobial activities of the different selected combinations against both P. aeruginosa and E. coli. The study of the mechanism of action of the most important compound in this series (amide 2i derived from N-methyl-norspermidine) showed the effect of disruption of the outer bacterial membrane of P. aeruginosa PA01 cells. Computational ADMET profiling renders compound 2i as a suitable starting point for pharmacokinetic optimization.
  • 433
  • 19 Jan 2022
Topic Review
Small-Molecule Semiconductor-Based OFET Temperature Sensors
Organic small-molecule semiconductors offer many benefits over their polymer equivalents, including ease of production, greater purity, and increased charge carrier mobility. OFETs based on small-molecule semiconductors have been intensively investigated as sensors for a variety of applications, including gas sensing, chemical sensing, biosensors, and pressure sensing.
  • 762
  • 17 Jan 2022
Topic Review
Thienopyrimidine
Thienopyrimidine emerges as an attractive scaffold in medicinal chemistry with a wide array of pharmacological properties, such as antibacterial, antifungal, antiparasitic and antiviral. Considering the fusion between pyrimidine and thiophene rings, three different thienopyrimidines can be obtained, namely thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines. Different synthetic pathways involving the construction of the pyrimidine or the thiophene ring were reported in the literature to access polysubstituted thienopyrimidines. In these approaches, the synthetic strategies mostly involved the synthesis of a thienopyrimidin-4-one derivative, where position 4 could be modified via further functionalization.
  • 817
  • 13 Jan 2022
Topic Review
Commercial Polymeric Membrane for Gas Separation
CO2 has been highly emitted to the environment, with the distribution of 25% being from electricity and heat production, 24% from agriculture, forestry, and other land usages, 21% by industry, 14% from transportation, 10% by other energies, and 6% from building. CO2 removal from natural gas is needed due to issues such as corrosion, catalyst poisoning and its effects on lowering the heating value of fuel. Several mass-transfer technologies can be used for this purpose, namely, membrane, absorption, adsorption and cryogenic. Membrane-based separation methods are more energy-efficient than heat-driven separations. Membrane-based separation uses 90% less energy than its distillation counterpart.
  • 1.7K
  • 12 Jan 2022
Topic Review
Polymers Modifications through Ultraviolet Absorbers Addition
The photooxidative degradation process of plastics caused by ultraviolet irradiation leads to bond breaking, crosslinking, the elimination of volatiles, formation of free radicals, and decreases in weight and molecular weight. Photodegradation deteriorates both the mechanical and physical properties of plastics and affects their predicted life use, in particular for applications in harsh environments. Plastics have many benefits, while on the other hand, they have numerous disadvantages, such as photodegradation and photooxidation in harsh environments and the release of toxic substances due to the leaching of some components, which have a negative effect on living organisms. Therefore, attention is paid to the design and use of safe, plastic, ultraviolet stabilizers that do not pose a danger to the environment if released. Plastic ultraviolet photostabilizers act as efficient light screeners (absorbers or pigments), excited-state deactivators (quenchers), hydroperoxide decomposers, and radical scavengers. Ultraviolet absorbers are cheap to produce, can be used in low concentrations, mix well with polymers to produce a homogenous matrix, and do not alter the color of polymers.
  • 2.0K
  • 10 Jan 2022
Topic Review
Palladium-Catalyzed Carboxylation Reactions
The efficient incorporation of carbon dioxide into an organic substrate (carboxylation) under catalytic conditions to give high value added molecules is one of the most important and fascinating areas of current organic synthesis. Carbon dioxide is a nonflammable, inexpensive and largely available C-1 feedstock. In fact, it allows converting an important waste (it is well known that carbon dioxide is produced in enormous amounts from the combustion of fossil fuels for the production of energy) into a variety of useful compounds, which can find application as fuels or in the pharmaceutical or material fields.
  • 860
  • 06 Jan 2022
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