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Topic Review
Anti-COVID-19 potential of Clove phytochemicals
The current COronaVIrus Disease 19 (COVID-19) pandemic caused by SARS-CoV-2 infection is enormously affecting the worldwide health and economy. In the wait for an effective global immunization, the development of a specific therapeutic protocol to treat COVID-19 patients is clearly necessary as a short-term solution of the problem. Drug repurposing and herbal medicine represent two of the most explored strategies for an anti-COVID-19 drug discovery. Clove (Syzygium aromaticum L.) is a well-known culinary spice that has been used for centuries in folk medicine in many disorders. Interestingly, traditional medicines have used clove since ancient times to treat respiratory ailments, whilst clove ingredients show antiviral and anti-inflammatory properties. Other interesting features are the clove antithrombotic, immunostimulatory, and antibacterial effects.
  • 6.5K
  • 13 May 2021
Topic Review
Applications of Heterocyclic Compounds
Fluorescently labelled heterocyclic compounds are useful in bioanalytical applications, including in vivo imaging, high throughput screening, diagnostics, and light-emitting diodes. These compounds have various therapeutic properties, including antifungal, antitumor, antimalarial, anti-inflammatory, and analgesic activities. Different neutral fluorescent markers containing nitrogen heterocycles (quinolones, azafluoranthenes, pyrazoloquinolines, etc.) have several electrochemical, biological, and nonlinear optic applications. Photodynamic therapy (PDT), which destroys tumors and keeps normal tissues safe, works in the presence of molecular oxygen with light and a photosensitizing drugs (dye) to obtain a therapeutic effect. 
  • 6.4K
  • 18 Oct 2022
Topic Review
Extraction Methods of Medicinal Plants for Antimicrobial Textiles
Medicinal plants are the product of natural drug discoveries and have gained traction due to their pharmacological activities. Pathogens are everywhere, and they thrive in ideal conditions depending on the nutrients, moisture, temperature, and pH that increase the growth of harmful pathogens on surfaces and textiles.
  • 6.3K
  • 22 Aug 2022
Topic Review
Classification of the Approved EGFR-TKIs
Targeting EGFR with small-molecule inhibitors is a valid strategy in cancer therapy. Since the approval of the first EGFR-TKI in 2003, a huge number of EGFR inhibitors were reported. Classification of these inhibitors could help the researchers to understand their structure-activity relationship. Herein, we introduce different types of classifications of the EGFR-TKIs, which received global approval for clinical use. In the following, the EGFR-targeting drugs are classified based on their chemistry, clinical use, target kinases, and the type of inhibition/interaction with EGFR. 
  • 4.2K
  • 25 Nov 2021
Topic Review
Advantages and Disadvantages of Covalent Inhibitors
The formation of covalent bonds that target proteins can offer drugs diverse advantages in terms of target selectivity, drug resistance, and administration concentration. The most important factor for covalent inhibitors is the electrophile (warhead), which dictates selectivity, reactivity, and the type of protein binding (i.e., reversible or irreversible) and can be modified/optimized through rational designs. Furthermore, covalent inhibitors are becoming more and more common in proteolysis, targeting chimeras (PROTACs) for degrading proteins, including those that are currently considered to be ‘undruggable’.
  • 3.7K
  • 10 May 2023
Topic Review
Pharmacological Applications of Piperidine Derivatives
Piperidine is a six-membered heterocycle including one nitrogen atom and five carbon atoms in the sp3-hybridized state. Piperidine-containing compounds represent one of the most important synthetic medicinal blocks for drugs construction, and their synthesis has long been widespread. It can be unequivocally stated that heterocyclic compounds play a significant part in the pharmaceutical industry, and one of the most common in their structure is the piperidine cycle. 
  • 3.0K
  • 09 Feb 2023
Topic Review
Five-Membered Heterocyclic Compounds
Heterocyclic compounds are a class of compounds of natural origin with favorable properties and hence have major pharmaceutical significance. They have an exceptional adroitness favoring their use as diverse smart biomimetics, in addition to possessing an active pharmacophore in a complex structure. This has made them an indispensable motif in the drug discovery field. Heterocyclic compounds are usually classified according to the ring size, type, and the number of heteroatoms present in the ring.
  • 2.9K
  • 16 Aug 2022
Topic Review
Ultra-High-Purity Aluminum
Properties of high-purity aluminum are the low magnetic permeability, the absence of low-temperature brittleness, as well as the increased strength and plasticity at low temperatures. These explain the classical application of high- to ultra-high-purity aluminum for the stabilization of superconductors running at cryogenic temperatures as low as −269 °C.
  • 2.9K
  • 01 Nov 2021
Topic Review
Xanthones
Xanthone is an aromatic oxygenated heterocyclic molecule, with a dibenzo-γ-pirone scaffold, known as 9H-xanthen-9-one, with the molecular formula of C13H8O2.
  • 2.6K
  • 23 Feb 2021
Topic Review
Epoxide Synthesis and Ring-Opening Reactions
This entry concentrates on some examples of success stories from the synthesis of approved medicines and drug candidates using epoxide chemistry in the development of robust and efficient syntheses at large scale. The focus is on those parts of each synthesis related to the substrate-controlled/diastereoselective and catalytic asymmetric synthesis of epoxide intermediates and their subsequent ring-opening reactions with various nucleophiles. These are described in the form of case studies of high profile pharmaceuticals spanning a diverse range of indications and molecular scaffolds such as heterocycles, terpenes, steroids, peptidomimetics, alkaloids and main stream small molecules. Representative examples include, but are not limited to the antihypertensive diltiazem, the antidepressant reboxetine, the HIV protease inhibitors atazanavir and indinavir, efinaconazole and related triazole antifungals, tasimelteon for sleep disorders, the anticancer agent carfilzomib, the anticoagulant rivaroxaban the antibiotic linezolid and the antiviral oseltamivir. Emphasis is given on aspects of catalytic asymmetric epoxidation employing metals with chiral ligands particularly with the Sharpless and Jacobsen–Katsuki methods as well as organocatalysts such as the chiral ketones of Shi and Yang, Pages's chiral iminium salts and typical chiral phase transfer agents.
  • 2.6K
  • 09 Oct 2020
Topic Review
Zinc Complexes as Anticancer Agents
The search for anticancer metal-based drugs alternative to platinum derivatives could not exclude zinc derivatives due to the importance of this metal for the correct functioning of the human body. Zinc, the second most abundant trace element in the human body, is one of the most important micro-elements essential for human physiology. Its ubiquity in thousands of proteins and enzymes is related to its chemical features, in particular, its lack of redox activity and its ability to support different coordination geometries and to promote fast ligands exchange. Analogously to other trace elements, the impairment of its homeostasis can lead to various diseases and in some cases can be also related to cancer development. However, zinc complexes generally exert lower toxicity in comparison to other metal-based drugs and many zinc derivatives have been proposed as antitumor agents. Among them zinc complexes  comprising  N-donor ligands have been surveyed and analyzed. 
  • 2.5K
  • 22 Dec 2020
Topic Review
Ginger
Ginger in its many forms, from juices of the fresh rhizome, to ginger powder and ginger essential oil, is growing in popularity for claimed universal health benefits. Nevertheless, and contrarily to the common notion of the public, ginger is not devoid of side effects, especially interactions with other drugs, and many of the claimed benefits remain to be substantiated. 
  • 2.4K
  • 17 Jun 2021
Topic Review
Chemistry of Chalcone and Its Derivatives
Chalcone is a collective group of ketones (flavonoids) that has a three-carbon α,β-unsaturated carbonyl group attached to two aromatic rings. Other chemical names of chalcone include benzyl acetophenone or benzylideneacetophenone. They are produced by certain plant species such as Angelica, Glycyrrhiza, Humulus, and Scutellaria as precursors to the biosynthesis of flavonoids and isoflavonoids and intermediates to the synthesis of heterocyclic compounds with biologically interesting properties such as pyrazolines, isoxazoles, cyanopyridines and pyrimidines.
  • 2.4K
  • 25 Oct 2022
Topic Review
Phlorotannins
Phlorotannins represent an important group of phenolic compounds, exclusively occurring in brown algae that can form simple structures of 126 Da to very large and complex polymers. Although the biosynthetic pathway of these compounds is still not consensual, it is known that they are formed via C–C and/or C–O–C oxidative coupling of several monomeric units of phloroglucinol, which in turn is known to be biosynthesized through the acetate–malonate pathway. According to the type of linkage formed between these units and the number of hydroxyl groups, phlorotannins can be classified in four sub-classes, namely phlorethols and fuhalols (ether linkages), fucols (aryl-aryl linkages), fucophlorethols (aryl-aryl and ether linkages), and eckols and carmalols (dibenzodoxine linkage).
  • 2.4K
  • 13 Oct 2023
Topic Review
Bee-Products in Male Reproductive Impairment
Bee products are sources of functional food that have been used in complementary medicine to treat a variety of acute and chronic illnesses in many parts of the world. The products vary from location to location as well as country to country. 
  • 2.3K
  • 08 Jun 2021
Topic Review
Molecular Dynamics Simulations
Molecular dynamics (MD) is a simulation technique that aims at deriving statements about the structural, dynamical, and thermodynamical properties of a molecular system. MD simulations have become increasingly useful in the modern drug development process. For example, in the lead discovery and lead optimization phases, MD facilitates the evaluation of the binding energetics and kinetics of the ligand-receptor interactions, therefore guiding the choice of the best candidate molecules for further development. in the future, the role of MD simulations in facilitating the drug development process is likely to grow substantially with the increasing computer power and advancements in the development of force fields and enhanced MD methodologies.
  • 2.1K
  • 20 Jan 2021
Topic Review
Red Macroalgae
Red Seaweed “Rhodophyta” are an important group of macroalgae that include approximately 7000 species. They are a rich source of structurally diverse bioactive constituents, including protein, sulfated polysaccharides, pigments, polyunsaturated fatty acids, vitamins, minerals, and phenolic compounds with nutritional, medical, and industrial importance. Polysaccharides are the main components in the cell wall of red algae and represent about 40–50% of the dry weight, which are extensively utilized in industry and pharmaceutical compounds, due to their thickening and gelling properties. The hydrocolloids galactans carrageenans and agars are the main red seaweed cell wall polysaccharides, which had broad-spectrum therapeutic characters. Generally, the chemical contents of seaweed are different according to the algal species, growth stage, environment, and external conditions, e.g., the temperature of the water, light intensity, nutrient concentrations in the ecosystem. Economically, they can be recommended as a substitute source for natural ingredients that contribute to a broad range of bioactivities like cancer therapy, anti-inflammatory agents, and acetylcholinesterase inhibitory. This entry touches on the mainpoints of the pharmaceutical applications of red seaweed, as well as the exploitation of their specific compounds and secondary metabolites with vital roles.
  • 2.0K
  • 07 Dec 2020
Topic Review
Taxol Biosynthetic Pathway
Taxol is one of the most effective anticancer drugs in the world that is widely used in the treatment of several cancers. The elucidation of the taxol biosynthetic pathway is the key to solve the problem of taxol supply. So far, the taxol biosynthetic pathway has been reported to require an estimated 20 steps of enzymatic reactions, and most of enzymes involved have been well characterized. In details, the source and formation of the taxane core and the process of the downstream synthetic pathway have been basically depicted, while the modification of the core taxane skeleton has not been fully reported, mainly concerning the developments from diol intermediates to 2-debenzoyltaxane. 
  • 2.0K
  • 01 Jun 2021
Topic Review
Synthesis of nucleobase-modified RNA oligonucleotides
The review summarizes the methods of site-specific incorporation of nucleobase-modified units into RNA oligomers via the post-synthetic strategy including recently discovered native hypermodified functional groups, fluorescent dyes, photoreactive groups, disulfide crosslinks, and nitroxide spin labels.
  • 2.0K
  • 06 Aug 2020
Topic Review
Natural sulfur containing compounds
The present review aims to characterize the general characteristics, physicochemical properties,and health-related studies of onion, garlic, and cruciferous vegetable consumption, as well as theinfluence of food processing on their content of active substances. The review combines distinctchapters where information relevant for nutraceutical and functional food engineers, medical doctors,as well as consumers can be obtained. We believe that the review will stimulate further studies relatedto the implementation of the most accurate sources of sulfur compounds from chosen plants whichcould support the therapy of cancer patients. Moreover, the review aims to present cost-e ectiveanti-tumor means that would include the implementation in the diet of sulfur-based compoundsin foods.
  • 1.9K
  • 26 Aug 2020
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