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
Acyclic Nucleic Acids with Phosphodiester Linkages
The pseudo-rotational flexibility of the ribonucleotide is considerably limited due to the anomeric effect, and RNA/RNA and RNA/DNA duplexes are generally more thermally stable than DNA/DNA duplexes. The rigidity of the cyclic scaffold has been considered important for the formation of thermally stable duplexes, and the unexpectedly high thermal stability of duplexes formed with the participation of LNA oligomers could serve as an excellent justification for this point of view. However, this generalization is not consistent with the behavior of Peptide Nucleic Acids (PNA), in which the heterocyclic bases are attached to a linear peptide-like backbone, since duplexes composed of RNA or DNA and PNA strands are far more stable than RNA/RNA and DNA/DNA ones. This phenomenon may be attributed to the absence of a negative charge in the backbone, such that the absence of repulsive interactions balances the entropic cost of proper spatial organization of the flexible PNA scaffolds. Nonetheless, the widely accepted importance of the cyclic sugar components for the stability of the duplexes could be questioned. There is another perspective that can be applied to the acyclic analogs of nucleic acids that is related to the origin of life. The synthetic efforts on acyclic analogs of nucleic acids and provides information on the most interesting features of selected classes of such compounds, are here described. The selection includes the following types of analogs: Flexible (FNA), Unlocked (UNA), Glycol (GNA), Butyl (BuNA), Threoninol (TNA) and Serinol Nucleic Acids (SNA). These classes of analogs are discussed in terms of their synthetic methods, the thermal stability of their homo- and hetero-duplexes and their applicability in biological and biochemical research and nanotechnology.
  • 1.4K
  • 10 Feb 2022
Topic Review
Catalytic Synthesis of Glycerol Carbonate
Glycerol carbonate (GC) belongs to the family of organic carbonates that are regarded as very typical “green chemistry” products for their unique advantages in many fields, such as high boiling point solvents, pharmaceutical intermediates, and material intermediates.
  • 3.5K
  • 10 Feb 2022
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.
  • 1.3K
  • 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.
  • 1.5K
  • 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.
  • 3.4K
  • 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.
  • 2.4K
  • 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.
  • 1.0K
  • 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.
  • 1.7K
  • 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.
  • 4.0K
  • 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.
  • 4.3K
  • 12 Jan 2022
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