Recent Advances in the Application of Barbituric Acid Derivatives in Multicomponent Reactions

Barbituric acid is a pyrimidine heterocyclic organic compound, which is pharmacologically active. It is important to build structures containing various medicinal activities. This compound attracts the scientific research community in organic synthesis. It can be used in the synthesis of polyheterocyclic, natural, medicinal compounds, and organic sensors. Herein, the utilization of barbituric or thiobarbituric acid in multicomponent reactions is reported from 2016-2021 in this manuscript.

Bioinformatic Analysis of Antiviral Medicinal Compounds Against Sars Cov-2 Proteases

The world is under siege from a global pandemic caused by a novel class of coronaviruses called severe acute respiratory syndrome coronavirus-2 (SARS CoV-2). These viruses cause severe respiratory illness leading to death. Molecular studies reveal that SARS CoV-2 proteases are involved in the processing of viral polyproteins. This study was conducted to obtain antiviral agents for SARS CoV-2 proteases. An extensive library of antiviral medicinal compounds was scrutinized to determine the probable interaction with both main and 3-chymotrypsin like proteases. Six antiviral compounds (Abietic Acid, Gallic Acid, Piceatannol, Piperine, Sinomenine, and Triptolide) were capable of establishing hydrogen bonds with the active pocket residues of the viral proteases, with appreciable binding energy. These compounds were subjected to root mean square analysis and tested not only for acute toxicity, but also for absorption, distribution, metabolism, excretion, and toxicity properties. Results were favourable for use in the treatment of SARS COV-2 infection.

The physicochemical and DNA binding studies of some medicinal compounds in solutions

To understand the expected mode of action, the physicochemical study on the solution properties of medicinal compounds and their interaction with deoxyribonucleic acid (DNA), under varying experimental conditions, is of prime importance. The present research work illustrates the physicochemical study and interaction of certain medicinal compounds such as; Levofloxacin, Ciprofloxacin, and Ibuprofen with DNA. Density, viscosity and surface tension measurements have been performed in order to determine, in a systematic manner, the physicochemical, volumetric and thermodynamic properties of these compounds; and most of these parameters have shown different behavior with varying concentration of solution, temperature of the medium and chemical nature/structure of the compound. In addition, these drugs showed a spontaneous surface-active and association behavior in aqueous solutions. The flow behavior, surface properties, volumetric behavior and solute–solvent interaction of these drugs were prominently influenced by experimental variables and addition of DNA to their solutions. UV–Visible spectroscopy was also used to examine the interaction of these drugs with DNA in aqueous media in detail. Calculated values of binding constants (Kb) for all complexes of drug-DNA are positive, indicating a fruitful binding process. It is seen that a smaller Kb value reflects weaker binding of the drug with DNA and vise versa. Due to the difference in the chemical structure of drugs the values of binding constant are different for various drug-DNA complexes and follow the order Kb(Levofloxacin-DNA) > Kb(Ciprofloxacin-DNA) > Kb(Ibuprofen-DNA). On the basis of spectral changes and Kb it can be said that the binding of all these drugs with DNA may be of physicochemical nature and the dominating binding force be of hydrogen bonding between oxygen of drugs and hydrogen of DNA units and the drug having more oxygen atoms showed stronger binding ability. The data further suggest a limited possibility of chemical type attachment of these drugs with DNA.

Exploring Aromatic Medicinal Compounds for the Treatment of Amyotrophic Lateral Sclerosis

Purpose: Amyotrophic lateral sclerosis (ALS) is a lethal neurodegenerative condition, in which motor neurons start to degenerate due to the accumulation of protein aggregates in the neuron cytoplasm. The formation of aggregates causes neurotoxicity, facilitated by the N-terminal domain (NTD) of the transactive response DNA-binding protein-43 (TDP-43). Therapies used to treat ALS manage secondary symptoms, but do not stop the activity of the rogue NTD domain of TDP-43. Therefore, new drug candidates should be designed to deal efficiently with this disease by inhibiting the domains involved in the development of ALS. This study determined the chemical affinity of aromatic medicinal compounds with NTD. Screening of 1323 medicinal compounds was conducted with PYRX 0.9 software against NTD. Compounds obtained from this analysis were further used to predict absorption, distribution, metabolism, excretion, and toxic (ADMET) properties and their effect on major gene targets of ALS. Results: From 1300 + compounds, acetovanillone showed binding affinity for NTD and had good ADMET and drug likeness attributes. This compound reduced the expression of CXCL2, NOP56, and SOD1 genes implicated in ALS pathogenesis. Conclusion: These results concluded that acetovanillone is a candidate drug for in vitro and clinical studies into the exploitation of drugs within ALS therapeutics.

Antimicrobial Activity of Medicinal Compounds Produced by Fungal Degradation of Soybean Oil Using Lignocellulose Biomass as Surface

Methyl esters were produced by fungal degradation of soybean oil using banana leaves as surface. Analysis of the products also revealed medicinal compounds (Benzyl Benzoate obtained from the banana leaves used as surface for the fungal degradation of the soybean oil and 1, 2-Benzene dicarboxylic acid dioctyl ester obtained from the soybean oil impurities). Microorganism activity test was carried out on the medicinal compounds to confirm their antibacterial and antifungal activity. The result showed that both had antibacterial and antifungal activity as shown by the zones of inhibition and as a result can find useful applications in food processing and preservation as well as agriculture as pest/disease control agents.

Hydrogels are promising considering their incredible capacity to modify, encapsulate and co-deliver medicinal compounds, cells, biomolecules, and nanomaterials

As many medications are administered jointly, they often give larger benefits, counteract disadvantages, and enhance treatment results compared to monotherapy. Whether natural or synthetic, injectable biomaterials can form degradable networks in situ, decreasing patient pain and cost while presenting new and promising possibilities for minimally invasive surgery. Biomaterials' ability to create and manufacture injectable systems is strongly impacted by their physicochemical and mechanical properties. The design and manufacture of injectable systems containing cells, therapeutic molecules, particles, and biomolecules that can be injected into geometrically complex body tissue regions poses a significant challenge as they must ensure drug/biomolecule/material bioactivity, cell survival and retention. Hydrogels are a promising choice in this case given their amazing ability to manipulate, encapsulate and co-deliver pharmaceutical chemicals, cells, biomolecules, and nanomaterials. Hydrogels can alter their mechanical and deteriorating qualities by adjusting the cross-linking technique and chemical composition. The ability to modify IH's mechanical strength permits co-encapsulation of medicinal compounds, cells, nanomaterials, and growth factors in the matrix in situ, allowing for multimodal synergistic therapies.To boost the prospects of translating IHs into normal clinics, various barriers and outstanding scientific issues must be tackled in the future. Future investigations, including the application of IHs in multimodal synergistic treatment, should start with large animal models such as monkeys and dogs or even ex vivo human tissue models. In addition, the period of in vivo evaluations should be prolonged from weeks to months for trustworthy and accurate data to be translated to clinical trials. On the one hand, the toxicity of certain crosslinking agents used in IH synthesis must be considered, as the residues will cause unwanted in vivo reactions.Toxic crosslinkers, on the other hand, may interact with therapeutic molecules/biomolecules or nanomaterials trapped in the hydrogel matrix, causing loss of bioactivity. Similarly, IHs' sol–gel transition is a vital issue requiring much investigation. A quick sol–gel transition of precursor solutions might cause the fluid to be caught in the needle, whereas high-viscosity precursor solutions need high injection force, resulting in physician hand fatigue and patient annoyance. Other concerns for clinical IH translation include fast release and rate of degradation. Degradation rate is critical in controlling therapeutic drug release and tissue regeneration. Fast hydrogel breakdown may trigger early inflammatory reaction due to breakdown products, whereas delayed degradation may result in insufficient release of therapeutic drugs. Changing the composition, structure, and crystallinity of polymers must be employed to customize the breakdown rate. Expert researchers will be better equipped to tackle these challenges if they have a deeper knowledge of polymers' physiochemical features. Overall, future IH design should focus on building simple, well-defined 3D networks with low toxicity, high biodegradation rate, and acceptable functionality.

Therapeutic potential of seaweeds

Seaweeds in general are known to contribute to the maintenance of health through their nutritional and medicinal properties and are served in soups and salads, cooked with grains, legumes or miso-soup broth, vegetable pies, stews and even consumed dried. The medicinal properties of seaweeds or vegetables have long been known in many cultures of people particularly those living in the coastal regions who are consuming these from centuries. Traditional Chinese dietotherapy (TCD) makes good use of natural marine nutrients and food to preserve health. Koreans wrap their bodies in seaweeds to get rid of deadly body toxins and Japanese who eat large quantities of seaweeds have very low incidence of cancers. The compounds with diverse biological activities such as antioxidant, antiviral, antifungal, antineoplastic, antimicrobial etc. have been isolated from the flora in the sea. A score of these bio-medicinal compounds are in different stages of clinical trials & analysis and are the focus of this article.

MEDICINAL IMPORTANCE OF MOLLUGO VERTICILLATA (MOLLUGINACEAE): A REVIEW

Over the years, the world has become common to pandemic diseases in humans with lot of ailments and untreated infectious disorders. Most of the laboratories across the globe run in with under developed vaccines and drugs for many diseases for its procurement and prevention. But the bioavailability of the drug in the market is less reached due to high cost and etc. In the current situation, plant saps and its extracts are used to counteract with the pathogens based on the information in traditional medicine. Most of the phytochemical enriched herb, weed or plants available commonly are used for treatments of various diseases. One of the herbs found is Mollugo verticillata (commonly known as ‘green carpet weed’). It is commonly used in treating fever, aches and other various ailments and it shows promising activity in pharmacological properties due to the presence of phytoconstituents like terpenoids, saponins and flavonoids. Finally, the plant extract has enormous medicinal importance. This review is a collection of overall research work on Mollugo verticillata plant and their medicinal compounds present.