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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Entries
Topic Review
Synthetic Organic Antimicrobial Agents
Synthetic organic antimicrobial agents are organic compounds and polymers that exhibit antimicrobial activity, which is self-activated through the aforementioned mode of action. Their chemical structure is critical for their categorisation. Recently, a huge number of antimicrobial polymers were synthesized. These species could be quaternary ammonium compounds (QACs), halogen-containing compounds (molecules containing fluorine or chlorine, N-halamines or triclosan), guanidine-containing polymers (polyhexamethylene vinyguanide), polymers containing phospho- and sulpho-derivatives, polymers of phenol and benzoic acid derivatives, nitro compounds, urea, amines, formaldehyde, organometallic polymers and others.
  • 369
  • 17 Apr 2023
Topic Review
Silver and Zinc Oxide Nanoparticles
The versatility of Ag-NPs and zinc oxide NPs (ZnO-NPs) in rendering themselves to many applications, including in sensors, renewable energies, environmental remediation, bio-therapeutic devices, clothing, antimicrobial is currently being explored.
  • 395
  • 17 Apr 2023
Topic Review
Synthesis of the 1,2,3-Dithiazole Scaffold
The 1,2,3-dithiazole is an underappreciated scaffold in medicinal chemistry despite possessing a wide variety of nascent pharmacological activities. The scaffold has a potential wealth of opportunities within these activities and further afield. The synthesis of Appel salt 1 acted as a catalyst to the field and granted access to many 1,2,3-dithiazole derivatives, and to other heterocycles incorporating sulfur and nitrogen atoms.
  • 317
  • 12 Apr 2023
Topic Review
Oxidative Catalytic Processes for APIs and Precursors Preparation
Active pharmaceutical ingredients (APIs) can be defined as those biological compounds used for the detection, prevention, and treatment of different types of diseases. Asymmetric oxidation processes have constituted a valuable tool for the synthesis of APIs, especially for the preparation of optically active sulfoxides, compounds with interesting biological properties. Biocatalyzed reactions usually occur with high efficiency, excellent selectivity, good yields, environmental sustainability, and lower costs, which make them more attractive from an industrial perspective. However, it must be taken into account that these procedures also present some drawbacks, such as the (relatively) high substrate specificity of biocatalysts or the low substrate loadings required due to their generally low solubility in water.
  • 571
  • 10 Apr 2023
Topic Review
Papaverine and Its Mechanism of Action
Papaverine has been proven to be a high-value opioid alkaloid in the field of therapeutics either in solitude or in combination with other metabolites/molecules. Pharmacological research has revealed that papaverine demonstrates a variety of biological activities, including activity against erectile dysfunction, postoperative vasospasms, and pulmonary vasoconstriction, as well as antiviral, cardioprotective, anti-inflammatory, anticancer, neuroprotective, and gestational actions.
  • 857
  • 07 Apr 2023
Topic Review
Organic Electronic Devices and Assessment Parameters
Organic electronic devices have gained popularity because of their promising tunable electronic properties, flexibility, low-cost, versatile functionalization, and processability. Organic field effect transistors (OFETs) are not only the fundamental building blocks of flexible and large-area electronic devices but are also a useful tool for measuring charge-carrier mobilities of newly organic semiconductors.
  • 371
  • 06 Apr 2023
Topic Review
Acyl Oxime Ester
The synthetic strategies of oxime derivatives participating in radical-type reactions have been rapidly developed in the last few decades. Among them, the N–O bond cleavage of oxime esters leading to formation of nitrogen-centered radicals triggers adjacent C–C bond cleavage to produce carbon-centered free radicals, which has been virtually used in organic synthesis in recent years.
  • 556
  • 29 Mar 2023
Topic Review
Phosphorus-Substituted Pyridines
Phosphorus(V)-substituted pyridine was first synthesized by Plazek’s research group in 1936 by a reaction of 2-dimethylaminopyridine with phosphorus trichloride under oxidative conditions. Later, related compounds were obtained by reactions of metalated pyridines with phosphorus-halogen compounds, of pyridinediazonium tetrafluoroborate with phosphorus trichloride, of N-alkoxypyridines with sodium diethyl phosphite and phosphines, and of N-pyridylpyridines with phosphonic acid, by the Michaelis–Arbuzov reaction, Pd(II)-catalyzed phosphorylation of halopyridines, cyclization of phosphorus-containing 3-azatrienes, and the Diels–Alder reaction involving 3-phosphoryl-1-azadienes.
  • 539
  • 20 Mar 2023
Topic Review
Direct Amidations of Carboxylic Acids with Amines
The prevalence of amides in biological systems and chemical fields such as polymers, materials and natural products drives continuous research on novel procedures to obtain these ubiquitous functional groups. Efforts to this purpose are mainly focused around the discovery of direct and catalytic methods that are more atom economic, safe and practical for diversified applications (e.g., organic, medicinal and peptide chemistries, material and polymer purposes, etc.), in accordance with green chemistry principles. 
  • 1.0K
  • 22 Feb 2023
Topic Review
Sugar Based Surfactants
Sugar-based surfactants are a class of surfactants derived from natural sugars, such as glucose, sucrose, and maltose. These surfactants have gained significant interest in recent years due to their biodegradability, low toxicity, and high compatibility with biological systems. Sugar-based surfactants are classified into two main groups: alkyl polyglucosides (APGs) and saccharide fatty acid esters (SFAEs). APGs are produced by reacting a fatty alcohol with glucose, while SFAEs are produced by esterifying a sugar molecule with a fatty acid. APGs have excellent cleaning and foaming properties and are used in a variety of personal care and household products, including shampoos, body washes, and dishwashing detergents. SFAEs are mainly used in the food industry as emulsifiers and stabilizers. One of the main advantages of sugar-based surfactants is their biodegradability, which means that they break down into harmless substances when exposed to environmental conditions such as sunlight, water, and microorganisms. This makes them an attractive alternative to synthetic surfactants, which can persist in the environment for a long time and have negative impacts on ecosystems.
  • 2.1K
  • 24 Mar 2023
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