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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.
13 May 2021
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.
09 Oct 2020
Small Molecules for Corneal Neovascularization
Multiple natural-source and synthetic small molecules have been tested preclinical for treating corneal neovascularization. Such small molecules include synthetic inhibitors of the vascular endothelial growth factor (VEGF) receptor and other tyrosine kinases, plus repurposed antimicrobials, as well as natural source-derived flavonoid and non-flavonoid phytochemicals, immunosuppressants, vitamins, and histone deacetylase inhibitors.
17 Aug 2020
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.
06 Aug 2020
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.
25 Nov 2021
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.
07 Dec 2020
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.
26 Aug 2020
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.
23 Feb 2021
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.
08 Jun 2021
Drug Delivery for Cardiovascular Diseases
Cardiovascular diseases (CVDs) are the leading cause of death globally, taking an estimated 17.9 million lives each year, representing one third of global mortality. As existing therapies still have limited success, due to the inability to control the biodistribution of the currently approved drugs, the quality of life of these patients is modest. The advent of nanomedicine has brought new insights in innovative treatment strategies.
08 Dec 2020
Featured Entry Collections
Encyclopedia of Social Sciences
Encyclopedia of ZEMCH Research and Development
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Encyclopedia of Piezoelectrics
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