Design, synthesis and evaluation of benzofuran-acetamide scaffold as potential anticonvulsant agent

A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran-3-yl)-2-(substituted) acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All the synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg–1 body mass during 0.5–4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, compounds 5i [N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(cyclohexyl(methyl)amino)-acetamide] and 5c [N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(4-methylpiperidin-1-yl)acetamide] demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas compound 5f [(N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(4-(furan-2-carbonyl)-piperazin-1-yl) acetamide] exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg–1 body mass. The ED50 of synthesized compounds ranged from 0.055 to 0.259 mmol kg–1 (~23.4 to 127.6 mg kg–1) body mass. The pharmacophore mapping of the examined compounds on standard drugs (phenobarbital, phenytoin, ralitolin and carbamazepine) strongly suggests that these compounds may exert their anticonvulsant activity via the same established mechanism as that of known drugs

Therapeutic Strategies in the Management of COVID-19

Since December 2019, SARS-CoV-2 (COVID-19), novel corona virus has caused pandemic globally, with rise in the number of cases and death of the patients. Vast majority of the countries that are dealing with rise in the active cases and death of patients suffering from novel corona viruses COVID-19 are trying to content the virus by isolating the patients and treating them with the approved antiviral that have been previously used in treating SARS, MERS, and drugs that are used to treat other viral infections. Some of these are under clinical trials. At present there are no therapeutically effective antiviral present and there are no vaccines or drugs available that are clinically approved for treating the corona virus. The current strategy is to re-purpose the available drugs or antiviral that can minimise or reduce the burden of the health care emergencies. In this article the reuse of antiviral, US-FDA approved drugs, plant based therapeutic, anti-malarial, anti-parasitic, anti–HIV drugs and the traditional medicines that are being currently used in treating the symptoms of COVID–19 patients is discussed emphasis is also given on the treatment using monoclonal antibodies. The present article provides the therapeutic strategies that will qualify as one of the best available treatment for the better management of the COVID–19 patients in order to achieve medical benefits

Metal–Polymer Nanocomposites: A Promising Approach to Antibacterial Materials

There has been a new approach in the development of antibacterials in order to enhance the antibacterial potential. The nanoparticles are tagged on to the surface of other metals or metal oxides and polymers to achieve nanocomposites. These have shown significant antibacterial properties when compared to nanoparticles. In this article we explore the antibacterial potentials of metal-based and metal–polymer-based nanocomposites, various techniques which are involved in the synthesis of the metal–polymer, nanocomposites, mechanisms of action, and their advantages, disadvantages, and applications

GC-MS Analysis and Biological activity of Essential Oil of Fruits, Needles and Bark of Pinus pinea grown wildly in Jordan

Essential oils from needles, fruits and bark was extracted from Pinus pinea L. (stone pine) grown wildly in Jordan. The chemical composition, antibacterial activity, antioxidant activity of essential oils was evaluated. The chemical compositions were identified using Gas-Chromatography-Mass spectrometry (GC-MS) and retention Indices (Van den Dool & Kratz). The results show that the essential oil obtained from needles composed mainly of Guaiol (12.7%), limonene (11.42%), and β-caryophyllene (7.61%), while fruit contains limonene (32.56%), and α-pinene (6.78%). The essential oils from barks were rich in β-caryophyllene (16.51%), limonene (14.83%), caryophyllene oxide (11.83%), and longifolene (7.51%). In vitro, antibacterial activity of the essential oil samples was evaluated using agar-well diffusion method against three different strains of bacteria (Gram¬-positive bacteria: Staphylococcus aureus and Gram-negative bacteria: Klebsiella pneumoniae and Escherichia coli). The results showed that essential oil showed appreciable antibacterial activity against S. aureus. The essential oil from fruit exhibited weak antibacterial activity against E. coli and K. pneumoniae. Essential oils of P. pinea showed appreciable antioxidant activity in-vitro

Microwave-Assisted Synthesis of Schiff Bases of Isoniazid and Evaluation of Their Anti-Proliferative and Antibacterial Activities

Three new Schiff bases of isoniazid were synthesized using microwave-assisted synthesis and conventional condensation with aromatic aldehydes. Synthesized compounds were characterized using elemental analysis, IR, NMR, and Mass spectroscopy. Synthesized compounds were evaluated for antiproliferative activity against MCF-7 cell line. The IC50 values were from 125 to 276 µM. The compounds were also evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli. Results showed that the synthesized compounds produce significant antibacterial activity in vitro. Inhibition of compounds ranged from 13 to 18 mm

Awareness of Cosmetic Procedures among Adults Seeking to Enhance Their Physical Appearance: A Cross-Sectional Pilot Study in Central Jordan

The increase in urban society in the use of cosmetic practices to rejuvenate oneself or obtain a more appealing appearance has influenced the practices of cosmetic dermatologists, general medical practitioners, plastic surgeons, and dental practitioners, among others. The pharmaceutical industry has evolved to meet customers’ desire to be more physically attractive irrespectively of age and gender. This study aimed to preliminarily explore Jordanian adults’ awareness of dental, facial, and other cosmetic procedures. The reasons for undergoing such cosmetic procedures and self-reported knowledge of the side effects or risks associated with these interventions were also explored. The results show that the participants had undergone various procedures to enhance their looks, attractiveness, and confidence. None of the female participants wanted to emulate a celebrity. Most participants were aware of the side effects associated with cosmetic procedures, which may be attributed to their educational backgrounds, as the participants’ minimum qualification was 12th grade and their easy access to information services such as electronic media. A multicenter, large-scale, regional study is required to determine the associations, correlations, and recommendations for individuals seeking cosmetic treatment, cosmetic health providers, and policymakers

Awareness of Cosmetic Procedures among Adults Seeking to Enhance Their Physical Appearance: A Cross-Sectional Pilot Study in Central Jordan

The increase in urban society in the use of cosmetic practices to rejuvenate oneself or obtain a more appealing appearance has influenced the practices of cosmetic dermatologists, general medical practitioners, plastic surgeons, and dental practitioners, among others. The pharmaceutical industry has evolved to meet customers’ desire to be more physically attractive irrespectively of age and gender. This study aimed to preliminarily explore Jordanian adults’ awareness of dental, facial, and other cosmetic procedures. The reasons for undergoing such cosmetic procedures and self-reported knowledge of the side effects or risks associated with these interventions were also explored. The results show that the participants had undergone various procedures to enhance their looks, attractiveness, and confidence. None of the female participants wanted to emulate a celebrity. Most participants were aware of the side effects associated with cosmetic procedures, which may be attributed to their educational backgrounds, as the participants’ minimum qualification was 12th grade and their easy access to information services such as electronic media. A multicenter, large-scale, regional study is required to determine the associations, correlations, and recommendations for individuals seeking cosmetic treatment, cosmetic health providers, and policymakers

Molecular modeling, synthesis, characterization and pharmacological evaluation of benzo[d]oxazole derivatives as non-steroidal anti-inflammatory agents

A series of N-(2-(4-chlorobenzyl)benzo[d]oxazol-5-yl)-3-substituted-propanamide (3a–3n) were synthesized and evaluated for their acute and chronic anti-inflammatory potential. The structure of the compounds was elucidated by elemental and spectral (IR, 1H NMR and MS) analysis. The synthesized compounds (at a dose of 20 mg/kg b.wt. p.o.) have shown their ability to provide 45.1–81.7% protection against carrageenan-induced paw edema, in comparison with diclofenac sodium (69.5%) and ibuprofen (64.7%). The most active compounds 3a, 3l and 3n were screened for chronic anti-inflammatory activity (cotton-pellet-induced granuloma) and to study their ulcerogenic activity. Compounds 3a, 3l and 3n showed 48.4%, 39.3% and 44.0% protection against cotton pellets-induced granuloma compared to diclofenac sodium (60.2%). The tested compounds were less ulcerogenic than the ibuprofen. Molecular modeling studies suggest that these compounds have strong interaction with the COX-2 enzyme, which is responsible for the activity

Development and Validation of HPLC-FLD Analysis of Perampanel in MEPS-Processed Rat Plasma Sample

Perampanel, a novel α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist, is registered for the adjunctive treatment of patients (aged ≥ 12 years) with refractory partial-onset seizures. A simple high-performance liquid chromatographic method fluorescence detection (HPLC-FLD) was developed to analyze perampanel in rats’ plasma and validated for bioanalytical purposes. Rats’ plasma (50 µL) was processed by microextraction packed sorbent (MEPS). The analytes were separated using a Hypersil Gold octadecyl silane column (250 × 4.6 mm internal diameter, 5 μm particle size) with isocratic elution. A mobile phase consisting of acetonitrile–methanol–water (275:275:450, v/v/v; containing 50 µL triethylamine and pH adjusted to 3.25 with orthophosphoric acid) was used in this analysis. The flow rate was 1.25 mL/min. Analytes were monitored at an excitation wavelength of 285 nm and an emission wavelength of 430 nm. The linearity range for this validated method was from 3.75 to 300 ng/mL. No endogenous peaks were found in the elution of analytes in drug-free rats’ plasma. Intra- and inter-batch reproducibility studies demonstrated accuracy and precision within the acceptance criteria. The results indicate that the present method is simple, selective, reproducible, and suitable for the analysis of perampanel in small volume samples. The robustness of the method was accessed using MODDE® design of experiments software version 12.5

Fatty Acid Analysis, Chemical Constituents, Biological Activity and Pesticide Residues Screening in Jordanian Propolis

Propolis is a resinous natural product collected by honeybees (Apis mellifera and others) from tree exudates that has been widely used in folk medicine. The present study was carried out to investigate the fatty acid composition, chemical constituents, antioxidant, and xanthine oxidase (XO) inhibitory activity of Jordanian propolis, collected from Al-Ghour, Jordan. The hexane extract of Jordanian propolis contained different fatty acids, which are reported for the first time by using GC-FID. The HPLC was carried out to identify important chemical constituents such as fatty acids, polyphenols and α-tocopherol. The antioxidant and xanthine oxidase inhibitory activities were also monitored. The major fatty acid identified were palmitic acid (44.6%), oleic acid (18:1∆9cis, 24.6%), arachidic acid (7.4%), stearic acid (5.4%), linoleic acid (18:2∆9–12cis, 3.1%), caprylic acid (2.9%), lignoceric acid (2.6%), cis-11,14-eicosaldienoic acid (20:2∆11–14cis, 2.4%), palmitoleic acid (1.5%), cis-11-eicosenoic acid (1.2%), α–linolenic acid (18:3∆9–12–15cis, 1.1%), cis-13,16-docosadienoic acid (22:2∆13–16cis, 1.0%), along with other fatty acids. The major chemical constituents identified using gradient HPLC-PDA analysis were pinocembrin (2.82%), chrysin (1.83%), luteolin-7-O-glucoside (1.23%), caffeic acid (1.12%), caffeic acid phenethyl ester (CAPE, 0.79%), apigenin (0.54%), galangin (0.46%), and luteolin (0.30%); while the minor constituents were hesperidin, quercetin, rutin, and vanillic acid. The percentage of α-tocopherol was 2.01 µg/g of the lipid fraction of propolis. Antioxidant properties of the extracts were determined via DPPH radical scavenging. The DPPH radical scavenging activities (IC50) of different extracts ranged from 6.13 to 60.5 µg/mL compared to ascorbic acid (1.21 µg/mL). The xanthine oxidase inhibition (IC50) ranged from 75.11 to 250.74 µg/mL compared to allopurinol (0.38 µg/mL). The results indicate that the various flavonoids, phenolic compounds, α-tocopherol, and other constituents which are present in propolis are responsible for the antioxidant and xanthine oxidation inhibition activity. To evaluate the safety studies of propolis, the pesticide residues were also monitored by LC-MS-MS 4500 Q-Trap. Trace amounts of pesticide residue (ng/mL) were detected in the samples, which are far below the permissible limit as per international guidelines