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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.
  • 2.1K
  • 10 Aug 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.
  • 2.1K
  • 17 May 2022
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.
  • 2.1K
  • 24 Dec 2021
Topic Review
Organoboron Compounds
The unique electron deficiency and coordination property of boron led to a wide range of applications in chemistry, energy research, materials science and the life sciences. The use of boron-containing compounds as pharmaceutical agents has a long history, and recent developments have produced encouraging strides. Boron agents have been used for both radiotherapy and chemotherapy. In radiotherapy, boron neutron capture therapy (BNCT) has been investigated to treat various types of tumors, such as glioblastoma multiforme (GBM) of brain, head and neck tumors, etc. Boron agents playing essential roles in such treatments and other well-established areas have been discussed elsewhere. Organoboron compounds used to treat various diseases besides tumor treatments through BNCT technology have also marked an important milestone. Following the clinical introduction of bortezomib as an anti-cancer agent, benzoxaborole drugs, tavaborole and crisaborole, have been approved for clinical use in the treatments of onychomycosis and atopic dermatitis. Some heterocyclic organoboron compounds represent potentially promising candidates for anti-infective drugs.
  • 2.1K
  • 25 Jun 2021
Topic Review
DNA Origami Nanostructures
Rapid breakthroughs in nucleic acid nanotechnology have always driven the creation of nano-assemblies with programmable design, potent functionality, good biocompatibility, and remarkable biosafety during the last few decades. Researchers are constantly looking for more powerful techniques that provide enhanced accuracy with greater resolution. The self-assembly of rationally designed nanostructures is now possible because of bottom-up structural nucleic acid (DNA and RNA) nanotechnology, notably DNA origami. Because DNA origami nanostructures can be organized precisely with nanoscale accuracy, they serve as a solid foundation for the exact arrangement of other functional materials for use in a number of applications in structural biology, biophysics, renewable energy, photonics, electronics, medicine, etc. DNA origami facilitates the creation of next-generation drug vectors to help in the solving of the rising demand on disease detection and therapy, as well as other biomedicine-related strategies in the real world. These DNA nanostructures, generated using Watson–Crick base pairing, exhibit a wide variety of properties, including great adaptability, precise programmability, and exceptionally low cytotoxicity in vitro and in vivo. 
  • 2.1K
  • 08 May 2023
Topic Review
Heterocyclic Anticancer Compounds
Heterocyclic organic compounds are designated as integral components on a wide array of structures with both pharmacological and biological importance. They constitute a large cohort of structures with immense importance in the life sciences. 
  • 2.1K
  • 29 Mar 2022
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. 
  • 2.0K
  • 19 Jan 2021
Topic Review
Sensing Tyrosinase Activity
Tyrosinase (TYR, E.C. 1.14.18.1), a critical enzyme participating in melanogenesis, catalyzes the first two steps in melanin biosynthesis including the ortho-hydroxylation of L-tyrosine and the oxidation of L-DOPA. Previous pharmacological investigations have revealed that an abnormal level of TYR is tightly associated with various dermatoses, including albinism, age spots, and malignant melanoma.
  • 2.0K
  • 08 Sep 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.
  • 2.0K
  • 28 Feb 2022
Topic Review
Synthetic Imidazopyridine-Based Derivatives
Fused pyridines are reported to display various pharmacological activities, such as antipyretic, analgesic, antiprotozoal, antibacterial, antitumor, antifungal, anti-inflammatory, and antiapoptotic. They are widely used in the field of medicinal chemistry. Imidazopyridines (IZPs) are crucial classes of fused heterocycles that are expansively reported on in the literature. Evidence suggests that IZPs, as fused scaffolds, possess more diverse profiles than individual imidazole and pyridine moieties. Bacterial infections and antibacterial resistance are ever-growing risks in the 21st century. Only one IZP, i.e., rifaximin, is available on the market as an antibiotic
  • 2.0K
  • 02 Feb 2023
Topic Review
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.
  • 2.0K
  • 08 Dec 2020
Topic Review
Riboflavin-Induced Photochemistry
Riboflavin (RF), which is also known as vitamin B2, is a water-soluble vitamin. RF is a nontoxic and biocompatible natural substance. It absorbs light (at wavelengths of 380 and 450 nm) in the presence of oxygen to form reactive singlet oxygen (1O2). The generated singlet oxygen acts as a photoinitiator to induce the oxidation of biomolecules, such as amino acids, proteins, and nucleotides, or to initiate chemical reactions, such as the thiol-ene reaction and crosslinking of tyramine and furfuryl groups. 
  • 2.0K
  • 23 Feb 2023
Topic Review
Antimicrobial Activity of Nitroaromatic Derivatives
Searching for new and efficient pharmaceuticals is a constant struggle for medicinal chemists. New substances are needed in order to treat different pathologies affecting the health of humans and animals, and these new compounds should be safe, effective and have the fewest side effects possible. Some functional groups are known for having biological activity; in this matter, the nitro group (NO2) is an efficient scaffold when synthesizing new bioactive molecules. Nitro compounds display a wide spectrum of activities that include antineoplastic, antibiotic, antihypertensive, antiparasitic, tranquilizers and even herbicides, among others.
  • 1.9K
  • 14 Jun 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).
  • 1.9K
  • 24 Feb 2021
Topic Review
PDE4 Inhibitors
Cyclic nucleotide phosphodiesterases 4 (PDE4) are a family of enzymes which specifically promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been widely investigated as a possible alternative strategy for the treatment of a variety of respiratory diseases, including chronic obstructive pulmonary disease and asthma, as well as psoriasis and other autoimmune disorders.
  • 1.9K
  • 21 Jul 2023
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.
  • 1.9K
  • 27 Oct 2020
Topic Review
Deep Eutectic Solvents in Pharmaceutical Industry
Neoteric solvents emerged as an alternative to organic solvents and are commonly called green solvents, since they have low toxicity, are biodegradable, are made with accessible and low-cost materials, and are quite easy to produce. Deep eutectic solvents (DESs) are defined as a mixture of two or more pure compounds, which, when combined in an appropriate ratio, give rise to a eutectic mixture that deviates from the ideal thermodynamic behaviour. This deviation is due to strong interactions between the initial components that act as hydrogen bond donors (HBDs) and hydrogen bond acceptors (HBAs). The HBDs and HBAs interact in the DESs to form a dense network of molecules that give them remarkably interesting physical and chemical properties. 
  • 1.9K
  • 23 Jan 2024
Topic Review
Antibacterial Activity of Heterocyclic Compounds
Heterocyclic compounds are cyclic compounds which contain the atoms of two discrete elements as representative of their ring(s). They belong to one of the larger classes of organic compounds and also appear more valuable in different fields of chemistry.
  • 1.9K
  • 19 Dec 2022
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
  • 1.9K
  • 26 Oct 2020
Topic Review
The Insulin Receptor
The insulin receptor (IR) is a transmembrane protein that is activated by ligands in insulin signaling pathways. The IR has been considered as a novel therapeutic target for clinical intervention, considering the overexpression of its protein and A-isoform in multiple cancers, Alzheimer’s disease, and Type 2 diabetes mellitus in humans. Meanwhile, it may also serve as a potential target in pest management due to its multiple physiological influences in insects.
  • 1.9K
  • 01 Aug 2022
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