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Topic Review
Rhenium(I) Tricarbonyl Complexes As Photosensitisers
Photodynamic therapy (PDT) is emerging as a significant complementary or alternative approach for cancer treatment. Re(I) tricarbonyl complexes is a new generation of metal-based photosensitisers for PDT that are of great interest in multidisciplinary research.
  • 1.4K
  • 27 Oct 2020
Topic Review
Nanotechnology for Eye Topical Drug Delivery
Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. Drug-loaded nanoparticles/hydrogels do not enter cells via diffusion. The endocytosis pathway is related to the penetration of drug-loaded nanoparticles/hydrogels into the cell. The interactions between the nanoparticles and the cell membrane generate forces of different origins and lead to the membrane wrapping of the nanoparticles followed by cellular uptake.
  • 1.4K
  • 24 Dec 2021
Topic Review
Hyaluronic Acid for Tissue Engineering
Polysaccharides such as hyaluronic acid (HA) which is omnipresent in the human body and exert pleiotropic biological functions such as tissue repair and tissue regeneration, may be exploited for cosmetics development, esthetic medicine, tissue engineering and regenerative medicine. In this work, the authors describe the excellent biocompatibility and biodegradability of HA-derived hydrogels with make them ideal materials for tissue engineering applications.
  • 1.4K
  • 27 May 2021
Topic Review
SARS-CoV-2 Main Protease
The main protease (Mpro) of the newly emerged severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was subjected to hyphenated pharmacophoric-based and structural-based virtual screenings using a library of microbial natural products (>24,000 compounds). Subsequent filtering of the resulted hits according to Lipinski’s rules was applied to select only the drug-like molecules. Top-scoring hits were further filtered out depending on their ability to show constant good binding affinities towards the molecular dynamic simulation (MDS)-derived enzyme’s conformers. Final MDS experiments were performed on the ligand-protein complexes to verify their binding modes and calculate their binding free energy. Consequently, a final selection of six compounds of microbial origin was proposed to possess high potential as anti-SARS-CoV-2 drug candidates. Our study provides insight into the role of the Mpro structural flexibility during interactions with the possible inhibitors and sheds light on the structure-based design of anti-coronavirus disease 2019 (COVID-19) therapeutics targeting SARS-CoV-2
  • 1.3K
  • 26 Oct 2020
Topic Review
Naphthoquinone and Anthraquinone
Naphthoquinone (NQ) and Anthraquinone (AQ) compounds have gained considerable interest from researchers in diverse pharmacological settings due to their biological activities, making them attractive building blocks for drug development. The literature contains many examples of NQ and AQ-based compounds, mainly derived from natural sources or synthetic, that also demonstrated promising properties against diverse AD targets. The NQ or AQ scaffolds may contribute to the biological effect against AD as main units or significant substructures. In particular, hybrid- and fragment-based drug design strategies allowed the identification of multifunctional NQ and AQ molecules, which displayed antioxidant activity and the ability to inhibit ChEs, BACE, Aβ and tau aggregation. 
  • 1.3K
  • 19 Jan 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.
  • 1.3K
  • 18 Oct 2022
Topic Review
2021 Peptides and Oligonucleotides Harvest
From the medical, pharmaceutical, and social perspectives, 2021 has been a year dominated by the COVID-19 pandemic. However, despite this global health crisis, the pharmaceutical industry has continued its endeavors, and 2021 could be considered an excellent year in terms of the drugs accepted by the US Food and Drug Administration (FDA). Thus, during this year, the FDA has approved 50 novel drugs, of which 36 are new chemical entities and 14 biologics. It has also authorized 10 TIDES (8 peptides, 2 oligonucleotides), in addition to 2 antibody-drug conjugates (ADCs) whose structures contain peptides.
  • 1.3K
  • 17 Feb 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.
  • 1.3K
  • 23 Nov 2023
Topic Review
Computational Drug Design of TB
Developing new, more effective antibiotics against resistant Mycobacterium tuberculosis that inhibit its essential proteins is an appealing strategy for combating the global tuberculosis (TB) epidemic. Finding a compound that can target a particular cavity in a protein and interrupt its enzymatic activity is the crucial objective of drug design and discovery. Such a compound is then subjected to different tests, including clinical trials, to study its effectiveness against the pathogen in the host. In recent times, new techniques, which involve computational and analytical methods, enhanced the chances of drug development, as opposed to traditional drug design methods, which are laborious and time-consuming. The computational techniques in drug design have been improved with a new generation of software used to develop and optimize active compounds that can be used in future chemotherapeutic development to combat global tuberculosis resistance.
  • 1.3K
  • 17 Dec 2021
Topic Review
Various Uses of Lycopene
Lycopene is a carotenoid abundantly found in red vegetables. This natural pigment displays an important role in human biological systems due to its excellent antioxidant and health-supporting functions, which show a protective effect against cardiovascular diseases, hypertension, cancers, and diabetes.
  • 1.3K
  • 28 Feb 2022
Topic Review
Dapsone Imine Derivatives
Dapsone (DDS) is an antibacterial drug with well-known antioxidant properties. However, the antioxidant behavior of its derivatives has not been well explored. In the present work, the antioxidant activity of 10 dapsone derivatives 4-substituted was determined by an evaluation in two in vitro models (DPPH radical scavenging assay and ferric reducing antioxidant power). These imine derivatives 1–10 were obtained through condensation between DDS and the corresponding aromatic aldehydes 4-substuited. Three derivatives presented better results than DDS in the determination of DPPH (2, 9, and 10). Likewise, we have three compounds with better reducing activity than dapsone (4, 9, and 10). In order to be more insight, the redox process, a conceptual DFT analysis was carried out. Molecular descriptors such as electronic distribution, the total charge accepting/donating capacity (I/A), and the partial charge accepting/donating capacity (ω+/ω−) were calculated to analyze the relative donor-acceptor capacity through employing a donor acceptor map (DAM). The DFT calculation allowed us to establish a relationship between GAPHOMO-LUMO and DAM with the observed antioxidant effects. According to the results, we concluded that compounds 2 and 3 have the lowest Ra values, representing a good antioxidant behavior observed experimentally in DPPH radical capturing. On the other hand, derivatives 4, 9, and 10 display the best reducing capacity activity with the highest ω− and Rd values. Consequently, we propose these compounds as the best antireductants in our DDS imine derivative series.
  • 1.3K
  • 08 Oct 2021
Topic Review
Fludeoxyglucose (18F)
Fluorodeoxyglucose (18F) (INN), or fluorodeoxyglucose F 18 (USAN and USP), also commonly called fluorodeoxyglucose and abbreviated [18F]FDG, 18F-FDG or FDG, is a radiopharmaceutical used in the medical imaging modality positron emission tomography (PET). Chemically, it is 2-deoxy-2-[18F]fluoro-D-glucose, a glucose analog, with the positron-emitting radionuclide fluorine-18 substituted for the normal hydroxyl group at the C-2 position in the glucose molecule. The uptake of 18F-FDG by tissues is a marker for the tissue uptake of glucose, which in turn is closely correlated with certain types of tissue metabolism. After 18F-FDG is injected into a patient, a PET scanner can form two-dimensional or three-dimensional images of the distribution of 18F-FDG within the body. Since its development in 1976, 18F-FDG had a profound influence on research in the neurosciences. The subsequent discovery in 1980 that 18F-FDG accumulates in tumors underpins the evolution of PET as a major clinical tool in cancer diagnosis. 18F-FDG is now the standard radiotracer used for PET neuroimaging and cancer patient management. The images can be assessed by a nuclear medicine physician or radiologist to provide diagnoses of various medical conditions.
  • 1.3K
  • 10 Oct 2022
Topic Review
Gemcitabine Peptide-Based Conjugates
Gemcitabine is an anticancer drug used to treat a wide range of solid tumors and is a first-line treatment for pancreatic cancer. The effect of gemcitabine is significantly weakened by its rapid plasma degradation. In addition, the systemic toxicity and drug resistance significantly reduce its chemotherapeutic efficacy. Up to now, many approaches have been made to improve the therapeutic index of gemcitabine. One of the recently developed approaches to improve conventional chemotherapy is based on the direct targeting of chemotherapeutics to cancer cells using the peptide-drug conjugates (PDCs).
  • 1.3K
  • 24 Feb 2021
Topic Review
Development of CDK4/6 Inhibitors
CDKs, a family of serine/threonine kinases, regulate cell cycle progression into the four distinct phases G1, S (DNA synthesis), G2 and M, and are crucially involved in the regulation of cell division and proliferation.
  • 1.3K
  • 23 Apr 2021
Topic Review
Pyrazino[1,2-a]Indoles
The pyrazino[1,2-a]indole unit is a tricyclic aromatic nucleus combining an indole and a pyrazine linked by the N5 and C9a atoms. The Synthesis and Biological Activities of Pyrazino[1,2-a]Indole and Pyrazino[1,2-a]Indol-1-One Derivatives is presented.
  • 1.3K
  • 10 Aug 2021
Topic Review
Alzheimer's disease
Alzheimer's disease (AD) is a multifactorial disease and the most common neurodegenerative disorder affecting the elderly population world-wide.The used medications treat the symptoms of AD, but without any delay on the progression of the disease. Curcumin presented favorable effects on AD. In the last decade curcumin analogues and derivatives have been synthesized in an attempt to optimize the beneficial properties of curcumin and improve its absorbance and  distribution per os as a therapeutic agent. Reviewing the bibliographical data of the last decade, information on the structures and / or chemical groups that are associated with specific action against AD, was gathered, derived from docking studies, (Q)SAR from vitro and in vivo tests. Phenolic hydroxyl groups might contribute to the anti-amyloidogenic activity. Phenyl methoxy groups seems to contribute to the suppression of Aβ42 and to the suppression of APP. Hydrophobic interactions revealed to be important. The presence of flexible moieties at the linker are crucial for the inhibition of Aβ aggregation. The inhibitory activity of derivatives is increased with the expansion of the aromatic rings. The keto-enol tautomer form offers as a new modification for the design of amyloid-binding agents. Taking the above under consideration  innovative design  and synthesis will lead to more potent and specific curcumin analogues and derivatives against AD.
  • 1.3K
  • 30 Oct 2020
Topic Review
Chemical Enzymology of Monoamine Oxidase
Monoamine oxidase (E.C. 1.4.3.4) enzymes MAO A and MAO B are FAD-containing proteins located on the outer face of the mitochondrial inner membrane, retained there by hydrophobic interactions and a transmembrane helix. The redox co-factor (FAD) is covalently attached to a cysteine and buried deep inside the protein behind an aromatic cage that aligns substrates towards the flavin. MAO metabolizes neurotransmitters such as dopamine and serotonin in the nervous system so is a target for drugs to modify amine levels. MAO also metabolizes a wide range of biogenic amines in all tissues. Current accumulated evidence, particularly from theoretical modelling, supports hydride transfer as the chemical mechanism. The long active site cavity accommodates a wide chemical variety of small molecules designed as inhibitors, including coumarins, chromones, triazoles, and more. Inactivators that bind covalently to MAO include hydrazines, cyclopropylamines and propargylamines. This entry is an extract adapted from a review outlining the remaining uncertainties in the understanding of this key drug target.
  • 1.3K
  • 19 Oct 2021
Topic Review
Chronic Wounds
The chronicity of wounds is affected by several contributory factors, including hormonal imbalances, cytokines, invasive microbial infections, and growth factors. More importantly, bacterial infections have been implicated as the predominant feature in most chronic wound microenvironments, including Staphylococcus aureus and Pseudomonas aeruginosa. These bacteria exist in polymicrobial forms forming biofilms that afford them protection against the host’s immunity and conventional antibiotics. S. aureus biofilms are sometimes present close to the surface of chronic wounds, while P. aeruginosa biofilms appear deep within wound tissue. The recalcitrant disposition of these microbes has been implicated as one of the causalities of antimicrobial resistance.
  • 1.3K
  • 17 May 2022
Topic Review
Tragia L. Genus
Tragia L. is a genus of plants belonging to the Euphorbiaceae family with worldwide intertropical distribution, composed of more than 150 species.
  • 1.2K
  • 16 May 2022
Topic Review
The Medicinal Chemistry of Artificial Nucleic Acids
Nucleic acids play a central role in human biology, making them suitable and attractive tools for therapeutic applications. While conventional drugs generally target proteins and induce transient therapeutic effects, nucleic acid medicines can achieve long-lasting or curative effects by targeting the genetic bases of diseases.
  • 1.2K
  • 05 Aug 2022
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