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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. 
  • 17.0K
  • 09 Feb 2023
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.
  • 9.7K
  • 22 Aug 2022
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. 
  • 8.9K
  • 18 Oct 2022
Topic Review
Methods of Preparation of Quinoxalines
Quinoxaline is a fused heterocycle system of a benzene ring and pyrazine ring. It has earned considerable attention due to its importance in the field of medicinal chemistry. The system is of extensive importance due to its comprehensive array of biological activities. Quinoxaline derivatives have been used as anticancer, anticonvulsant, anti-inflammatory, antidiabetic, antioxidant, antibacterial, anti-TB, antimalarial, antiviral, anti-HIV, and many other uses. Variously substituted quinoxalines are significant therapeutic agents in the pharmaceutical industry.
  • 8.5K
  • 23 Nov 2023
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.
  • 7.9K
  • 13 May 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’.
  • 6.5K
  • 10 May 2023
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. 
  • 5.9K
  • 25 Nov 2021
Topic Review
Mechanism of Action of Thiazolidin-2,4-dione
The thiazolidin-2,4-dione (TZD) moiety plays a central role in the biological functioning of several essential molecules. The availability of substitutions at the third and fifth positions of the Thiazolidin-2,4-dione (TZD) scaffold makes it a highly utilized and versatile moiety that exhibits a wide range of biological activities.
  • 5.2K
  • 18 Oct 2022
Topic Review
Natural Product Extraction Techniques
Conventional extraction techniques, including Soxhlet extraction, maceration, percolation, and decoction, are known to be time-, solvent-, and energy-intensive. In contrast, various non-conventional techniques for the extraction process, such as supercritical fluid extraction (SFE), microwave-assisted extraction (MAE), and ultrasound-assisted extraction (UAE), have been developed to increase the yield of bioactive compounds and address the aforementioned issues. These contemporary techniques have demonstrated their sustainability compared to conventional ones. Low-temperature and environmentally friendly extraction techniques have gained popularity for producing high-quality bioactive extracts. UAE, in particular, has attracted considerable interest due to its advantages over conventional extraction methods, which include greater extraction efficiency, preservation of bioactive compound stability, shorter extraction time, and industrial application. Thus, non-conventional extraction techniques like SFE, MAE, and UAE offer sustainable and efficient alternatives to conventional methods, allowing for increased bioactive compound yield, shorter extraction times, and improved stability, making them popular choices for high-quality extraction in low-temperature and environmentally friendly approaches.
  • 4.9K
  • 05 Jul 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.
  • 4.9K
  • 16 Aug 2022
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.
  • 4.8K
  • 09 Oct 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. 
  • 4.5K
  • 17 Jun 2021
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.
  • 4.5K
  • 01 Nov 2021
Topic Review
Medicinal Chemistry of Analgesic and Anti-Inflammatory Quinazoline Compounds
Quinazoline is an essential scaffold, known to be linked with various biological activities. Some of the prominent biological activities of this system are analgesic, anti-inflammatory, anti-hypertensive, anti-bacterial, anti-diabetic, anti-malarial, sedative–hypnotic, anti-histaminic, anti-cancer, anti-convulsant, anti-tubercular, and anti-viral activities. This diversity in the pharmacological response of the quinazoline system has encouraged medicinal chemists to study and discover this system and its multitude of potential against several biological activities.
  • 4.4K
  • 08 Dec 2022
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.
  • 4.4K
  • 25 Oct 2022
Topic Review
Saudi Arabian Plants
The kingdom of Saudi Arabia (SA) ranks fifth in Asia in terms of area. It features broad biodiversity, including interesting flora, and was the historical origin of Islam. It is endowed with a large variety of plants, including many herbs, shrubs, and trees. Many of these plants have a long history of use in traditional medicine.
  • 4.3K
  • 13 Jan 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.
  • 4.2K
  • 07 Apr 2023
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.
  • 4.1K
  • 23 Feb 2021
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. 
  • 4.1K
  • 22 Dec 2020
Topic Review
Thiophene-Based Compounds
Thiophene derivatives provide useful intermediaries in various areas of science and industry, with a wide range of applications, and therapeutic properties. Thiophene derivatives attract both great academic interest, and interest from the agrochemical, pharmaceutical, and dye industries, as well. As to their biological and pharmacological applications, thiophene derivatives possess remarkable properties as antipsychotic, antianxiety, antifungal, antimicrobial, antioxidant, anticancer, and anti-inflammatory agents. The present work provides an update on the role of thiophene-based derivatives in inflammation processes.
  • 3.8K
  • 09 Oct 2021
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