Recent Advances in Pyridine Scaffold: Focus on Chemistry, Synthesis, and Antibacterial Activities.

Multidrug-resistant (MDR) pathogens have created a fatal problem for human health and antimicrobial treatment. Among the currently available antibiotics, many are inactive against MDR pathogens. In this context, heterocyclic compounds/drugs play a vital role. Thus, it is very much essential to explore new research to combat the issue. Of the available nitrogen-bearing heterocyclic compounds/drugs, pyridine derivatives are of special interest due to their solubility. Encouragingly, some of the newly synthesized pyridine compounds/drugs are found to inhibit multidrug-resistant S. aureus (MRSA). Pyridine scaffold bearing poor basicity generally improves water solubility in pharmaceutically potential molecules and has led to the discovery of numerous broad-spectrum therapeutic agents. Keeping these in mind, we have reviewed the chemistry, recent synthetic techniques, and bacterial preventative activity of pyridine derivatives since 2015. This will facilitate the development of pyridine-based novel antibiotic/drug design in the near future as a versatile scaffold with limited side effects for the next-generation therapeutics.

Optimization of Tensile Strength and Young's Modulus of CNT-CF/Epoxy Composites Using Response Surface Methodology (RSM).

Composites such as carbon fiber are used extensively by automotive, aerospace, marine, and energy industries due to their strong mechanical properties. However, there are still many areas it is lacking in testing, especially related to its electrophoretic deposition. In this research work, the tensile strength and Young's modulus of CNT-CF/epoxy composites were measured using the tensile test by varying the electrophoretic deposition (EPD) process parameters. Response surface methodology (RSM) was used to optimize the three main parameters in this EPD process: the volume ratio (water as the basis), deposition voltage, and time to obtain the maximum tensile properties of the composites. There were four volume ratios (0%, 20%, 80% and 100%) used in this design of experiment (DoE) with ratios' pairs of 0%, 100%, and 20%, 80%. For this study, water and methanol were used as the suspension medium. This design's deposition voltage and time were 10 to 20 V and 5 to 15 min. ANOVA further verified the responses' adequacy. The optimum conditions for the first Design of Experiment (DoE) (0% and 100%) were identified as a volume ratio of 99.99% water, deposition voltage of 10 V, and 12.14 min. These conditions provided the maximum strength of these composites with a tensile strength of 7.41 N/mm2 and Young's modulus of 279.9 N/mm2. Subsequently, for the second DoE (20% and 80%), tensile strength of 7.28 N/mm2 and Young's modulus of 274.1 N/mm2 were achieved with the ideal conditions: volume ratio of 44.80% water, deposition voltage of 10.04 V, and time of 6.89 min. It can be concluded that the ideal interaction between these three EPD parameters was necessary to achieve composites with good tensile properties.

Novel Galactopyranoside Esters: Synthesis, Mechanism, In Vitro Antimicrobial Evaluation and Molecular Docking Studies.

One-step direct unimolar valeroylation of methyl α-D-galactopyranoside (MDG) mainly furnished the corresponding 6-O-valeroate. However, DMAP catalyzed a similar reaction that produced 2,6-di-O-valeroate and 6-O-valeroate, with the reactivity sequence as 6-OH > 2-OH > 3-OH,4-OH. To obtain novel antimicrobial agents, 6-O- and 2,6-di-O-valeroate were converted into several 2,3,4-tri-O- and 3,4-di-O-acyl esters, respectively, with other acylating agents in good yields. The PASS activity spectra along with in vitro antimicrobial evaluation clearly indicated that these MDG esters had better antifungal activities than antibacterial agents. To rationalize higher antifungal potentiality, molecular docking was conducted with sterol 14α-demethylase (PDB ID: 4UYL, Aspergillus fumigatus), which clearly supported the in vitro antifungal results. In particular, MDG ester 7−12 showed higher binding energy than the antifungal drug, fluconazole. Additionally, these compounds were found to have more promising binding energy with the SARS-CoV-2 main protease (6LU7) than tetracycline, fluconazole, and native inhibitor N3. Detailed investigation of Ki values, absorption, distribution, metabolism, excretion, and toxicity (ADMET), and the drug-likeness profile indicated that most of these compounds satisfy the drug-likeness evaluation, bioavailability, and safety tests, and hence, these synthetic novel MDG esters could be new antifungal and antiviral drugs.

Triazoles and Their Derivatives: Chemistry, Synthesis, and Therapeutic Applications.

Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. Structurally, there are two types of five-membered triazoles: 1,2,3-triazole and 1,2,4-triazole. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities. These are also important in organocatalysis, agrochemicals, and materials science. Thus, they have a broad range of therapeutic applications with ever-widening future scope across scientific disciplines. However, adverse events such as hepatotoxicity and hormonal problems lead to a careful revision of the azole family to obtain higher efficacy with minimum side effects. This review focuses on the structural features, synthesis, and notable therapeutic applications of triazoles and related compounds.

Physico-mechanical, thermal and morphological properties of furfuryl alcohol/2-ethylhexyl methacrylate/halloysite nanoclay wood polymer nanocomposites (WPNCs).

In this study, the physical, morphological, mechanical and thermal properties of furfuryl alcohol/2-ethylhexyl methacrylate/halloysite nanoclay wood polymer nanocomposites (FA-co-EHMA-HNC WPNCs) were investigated. FA-co-EHMA-HNC WPNCs were prepared via an impregnation method and the properties of the nanocomposites were characterized through the weight percent gain, Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), three-point flexural test, dynamic mechanical thermal analysis (DMTA), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) analysis and moisture absorption test. The weight percent gain in the 50:50 FA-co-EHMA-HNC WPNC was the highest compared with the raw wood (RW) and other WPNCs. The FT-IR results confirmed that polymerization took place in the nanocomposites, especially 50:50 FA-co-EHMA-HNC WPNC, which had a reduced amount of hydroxyl groups. The SEM results revealed that the 50:50 FA-co-EHMA-HNC WPNC had the smoothest and most uniform surface among all of the nanocomposites. The 50:50 FA-co-EHMA-HNC WPNC showed the highest flexural strength and modulus of elasticity. The results revealed that the storage modulus and loss modulus of the FA-co-EHMA-HNC WPNCs were higher and the tan δ of FA-co-EHMA-HNC WNPCs was lower compared with the RW. The FA-co-EHMA-HNC WPNCs exhibited the higher thermal stability in the TGA and DSC analysis. The 50:50 FA-co-EHMA-HNC WPNC exhibited remarkably lower moisture absorption compared with the RW. Overall, this study proved that the ratio 50:50 FA-co-EHMA ratio was the most suitable for introduction in the in the RW.

Review on the Risk Assessment of Heavy Metals in Malaysian Clams.

The current review discusses the levels of six heavy metals in different clam species from 34 sites of Malaysian coasts. The concentrations (µg/g dry weight) of these heavy metals ranged around 0.18-8.51, 0.13-17.20, 2.17-7.80, 0.84-36.00, 24.13-368.00, and 177.82-1912.00 for Cd, Pb, Ni, Cu, Zn, and Fe, respectively. It was observed that the concentrations of metals slightly depend on different clam species but mostly depend on site locations. According to Malaysian Food Regulation (1985), about 30% and more than 50% sites are safe from Cd and Pb contamination, respectively, and also the clam species from the other populations studied were safe for consumption.

Cadmium and lead in blood cockle (Anadara granosa) from Asajaya, Sarawak, Malaysia.

The concentrations were ranged from 1.35 ± 0.16 to 2.22 ± 0.34 µg/g (dry weight) and 2.65 ± 0.34 to 4.36 ± 0.53 µg/g (dry weight) for Cd and Pb, respectively, in blood cockle Anadara granosa from four sites of Sabang River, namely, Kampung Sambir, Kampung Tambirat, Beliong Temple, and Kampung Tanjung Apong, which are located at Asajaya, Sarawak, Malaysia. All values exceeded safety limits set by Malaysian Food Regulation (1985). It may be the cause of serious human health problems after long term consumption. Thus, consumer should have consciousness about such type of seafood from mentioned sites and need further investigation.