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Pharmaceutical Chemistry: Current Research Articles

Current articles in the field of Pharmaceutical Chemistry published online in scientific journals..




The international journal is devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates.

The publisher is Springer. The copyright and publishing rights of specialized products listed below are in this publishing house. This is also responsible for the content shown.

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Additional research articles see Current Chemistry Research Articles. Magazines with similar content (pharmaceutical chemistry):

 - ArchPharm Chemistry in Life Sciences.



Pharmaceutical Chemistry: Current Research Articles - Abstracts



Enhancing the Anticonvulsant Effects of Nifedipine in Rats Through Encapsulation with Water-Soluble β-Cyclodextrin Polymer

Encapsulation is one of the efficient methods recently developed for improving drug delivery. The present study was designed to encapsulate nifedipine (NIF) by water-soluble β-cyclodextrin polymer (β-CDP) and to evaluate the effects of this carrier on NIF-induced anticonvulsant effects. Adult male Wistar rats weighting 200 – 250 g (n = 7) received NIF or encapsulated NIF (β-CDP/NIF) (5, 10 and 20 mg/kg, i.p.), diazepam (2 mg/kg, i.p.) as positive control), and vehicle. Then, pentylenetetrazol (PTZ, 80 mg/kg, i.p.) was injected about 30 min after the drug injection. Changes in the onset time of seizures and duration of their different stages (tonic and tonic-clonic) and total convulsions duration, percentage mortality and percentage of seizure protection were assessed in all test groups. Latency of the seizure onset and duration of tonic and tonic-clonic seizures were significantly decreased in β-CDP/NIF group in comparison with NIF-treated rats (p < 0.05). On the other hand, percentage mortality was significantly decreased and percentage protection was increased by β-CDP/NIF in comparison to NIF (p < 0.05). Therefore, it was concluded that the encapsulation of NIF by β-CDP led to enhancement of the anticonvulsant effects of NIF in rats.


Datum: 04.01.2022


Synthesis and Cytotoxicity Against Human Breast Carcinoma Cell Evaluation of Some New 3,4-Disubstituted Coumarin Derivatives

A novel series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction of ethyl coumarin-3-carboxylate with pyrazole-3,5-dione and condensation of ethyl 7-hydroxycoumarin-3-carboxylate with 4,6-dibromo-3-amino phenol. Acylation with acetic anhydride and condensation of coumarin derivatives with 2-hydroxybenzaldehyde yielded the corresponding acetyl derivatives and 4-substituted pyrazole derivatives. Structures of the synthesized compounds were elucidated by spectral methods and elemental analysis. All the prepared derivatives were evaluated for their cytotoxicity against human breast carcinoma cell line (MCF-7). Compound VI showed the least IC50 value in MTT colorimetric assay as compared to that of the standard marketed drug staurosporin.


Datum: 04.01.2022


Antihyperglycemic and Antihyperlipidemic Evaluation of Zingiber officinale, Anethum graveolens and Citrullus colocynthis Extracts with Different Polarities in Streptozotocin-Induced Diabetic Rats

Zingiber officinale (ginger, II), Citrullus colocynthis (CC, III) and Anethum graveolens (dill, IV) are functional medicinal plants containing beneficial compounds and some evidence exists on their anti-diabetic, anti-inflammatory and hypolipidemic activities. The objective of this study was to evaluate the antihyperglycemic and antihyperlipidemic potential of various extracts of these plants with different polarities in experiments on streptozotocin-induced diabetic rats. Test animals (n = 112) were randomly divided into control, diabetic, diabetic+chloroform extract, diabetic+carbon tetrachloride extract, diabetic+hydroalcoholic extract, and diabetic+aqueous extract groups. Rats were made diabetic by a single injection of streptozotocin (STZ, 60 mg/kg). The plant extracts were daily administered (100 mg/kg, i.p.) for 3 weeks. Serum glucose and lipid levels were measured at different weeks. All extracts of ginger and dill as well as carbon tetrachloride and hydroalcoholic extracts of CC significantly reduced serum glucose level in diabetic groups. In addition, some plants extracts approppriately and significantly improved serum lipid levels including triglyceride, total cholesterol, HDLcholesterol, and LDL cholesterol in diabetic rats. According to extract polarities and components, all ginger extracts exerted hypoglycemic effect, however, hydroalcoholic extract showed the best potential to appropriately modify serum lipids in diabetic condition. In addition, hydroalcoholic extracts of C. colocynthis and A. graveolens had the best anti-diabetic potential which could be related to better extraction of bioactive components by polar or non-polar organic and aqueous solvents from these medicinal herbs.


Datum: 04.01.2022


Synthesis, Evaluation of Anti-Toxoplasma gondii Activity in vitro and Molecular Docking of Dihydroartemisinin Derivatives

In this work, 21 dihydroartemisinin derivatives were synthesized, their chemical structures were characterized by 1H NMR, 13H NMR and high-resolution MS techniques, and anti-Toxoplasma gondii activity in vitro was evaluated using thiazole blue (MTT) assay. The selectivity index of compound (3R,5aS,6R,8aS,9R,12R,12aR)-3,6,9-trime-thyldeca-hydro-12H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-yl 4-oxo-4-(pyridin-4-ylamino)butanoate (E2) was 2.24, which showed the strongest anti-T. gondii activity. In addition, the results of molecular docking studies show that E2 can be a better inhibitor of T. gondii calcium-dependent protein kinase 1 (TgCDPK1). Therefore, compound E2 has good potential as a drug for T. gondii treatment, and further research is needed to clarify its mechanism of action.


Datum: 04.01.2022


Antimicrobial, Antifungal and Enzymatic Profiling of Newly Synthesized Heavy Metal Complexes of Gemifloxacin

Three new heavy metal complexes of gemifloxacin (GMFX) were synthesized in 2:1 (L:M) ratio having good percent yield, characterized through physico-chemical and spectroscopic parameters including UV-Vis, TLC, FT-IR, NMR, and elemental (CHN) analysis. The gemifloxacin binds with metals (As, Ag, and Pb) bi-dentately as evident from the spectroscopic studies. These newly synthesized heavy metal complexes of gemifloxacin have been evaluated for their biological activities (antimicrobial and antifungal activities). Their enzymatic profiling was also determined against urease and alpha-chymotrypsin. Results obtained were then statistically analyzed through one way ANOVA and Dunnett’s test by using SPSS version 20.0 revealing that gemifloxacin act as bidentate ligand in complexation with heavy metals, and all newly synthesized complexes possess good antibacterial activities against P.mirabilis, S. typhi, E. coli, P. aureogenosa, K. pneumonia and S. flexneri. Complexes G-M13 and G-M11 showed increased activity against Citrobacter species, while G-M12 showed increased activity against C. albicans in comparison to gemifloxacin. Against S. faetures and S. aureus, G-M13 and G-M12 showed increased activity while G-M11 showed less activity than gemifloxacin. These complexes also possess mild to moderate activity against urease, whereas synthesized complexes show reduced response against α-chymotrypsin. Further emphasis and research on these complexes may place these as urease specific inhibitors in therapeutic agents’ index.


Datum: 04.01.2022


In Vivo Investigations of Analgesic, Antipyretic and Anthelmintic Activities of Various Extracts of Fernandoa adenophylla

Fernandoa adenophylla is well-known Thai medicinal tree used for treating skin disorders, as antiviral, antihypertensive, antidiabetic, and anti-diarrheal remedies, and muscle relaxant. In the present work, anthelmintic activity was studied on Pheretima posthuma (earth worm) specie. For analgesic activity (hot plate method), three groups of mice (n = 6 per group) were taken followed by intake of 100, 200 and 300 mg/kg dose of all extracts. Tramadol (0.1 mg/kg) and normal saline (0.9 g/L) were taken as positive and negative control, respectively. For antipyretic activity (Brewer’s yeast induced pyrexia), 5 groups of mice (n = 6 per group) were kept on fasting for 5 h before activity testing, while only water intake was allowed. Doses of 100, 200 and 300 mg/kg of all three extracts were administered. Paracetamol and NaCl were administered as standard and negative control, respectively. The rectal temperature was measured every hour for 5 h after dosing to observe changes in temperature. Toxicologically, all extracts were determined up to 4 g/kg in mice. In case of anthelmintic activity, the aqueous extract (60 mg/mL) significantly caused paralysis of P. posthuma in 15.4 ± 1.9 min. The aqueous extract showed greater analgesic activity at dose of 300 mg/kg for 60 min, continued till 90 min (p < 0.001) as compared to other extracts. The antipyretic activity of aqueous extract was significantly raised at 200 mg/kg after treatment (p < 0.01) and maximum level was observed in 4th and 5th hour of treatment. As a result, the plant extract showed no toxicity during toxicological analysis in mice, the highest dose of extracts was 4 g/kg. It can be concluded that the aqueous extract of F. adenophylla leaves exhibited best pharmacological potentials against model test organisms. Clinical trials are recommended for the above mentioned pharmacological activities of the aqueous extract of F. adenophylla leaves.


Datum: 01.12.2021


NMDA-Receptor Antagonists Reduce Skin Sensitivity to the TRPV1-Receptor Agonist Capsaicin

Glutamate receptors are widely represented in the central and peripheral nervous systems, which determines their involvement in central and peripheral nociception. In particular, NMDA receptors are localized at the dermal-epidermal junction. TRPV1 receptors in skin-innervating unmyelinated nerve fibers can functionally interact with NMDA receptors in the calcium/calmodulin-dependent protein kinase II and protein kinase C cascades. Herein, the effect of noncompetitive NMDA-receptor antagonists on peripheral skin sensitization caused by subcutaneous injection of the TRPV1-receptor agonist capsaicin was evaluated using different routes of administration. The high-affinity antagonist of NMDA receptors MK-801 and the low-affinity antagonist of NMDA receptors hemantane administered to mice by cutaneous application and systemic (intraperitoneal for hemantane and subcutaneous for MK-801) and subcutaneous injection in the metatarsal region reduced the duration of the response to subcutaneous injection of capsaicin solution in the metatarsal region.


Datum: 01.12.2021


Viability of Tumor Cells (K562, Hep-2, HeLa) and Rat Fibroblasts in the Presence of Pterostilbene and Extracts of Licorice Root and Andrographis Paniculata

Results from in vitro studies of the effect of pterostilbene, licorice root extract, and Andrographis paniculata extract on the viability of rat fibroblast and tumor-cell cultures (K562, Hep-2, HeLa) are reported. The selectivity index of pterostilbene (SI = 12.8 – 2.34) indicates the presence of selective cytotoxicity against tumor cells that decreases in the order Hep-2 > K562 ≥ HeLa. Licorice root extract at a concentration of 0.00025 – 0.5 mg/mL showed no noticeable cytotoxicity against normal and tumor cells. The extract of A. paniculata suppressed the viability of human chronic myelogenous leukemia cells at a concentration of 0.2 mg/mL and of all studied normal and tumor cells at a concentration of 2 mg/mL without selectivity with respect to all studied tumor cells.


Datum: 01.12.2021


Synthesis of Quinoxaline Derivatives as Intermediates to Obtain Erdafitinib

As an important member of multi-nitrogen heterocyclic compounds, quinoxalines have various biological activities which are widely used in chemistry, biomedicine and chemical industry. In this work, quinoxaline derivative 7-bromo-2-(1-methyl-1H-pyrazol-4-yl)quinoxaline (5), which is an essential intermediate to obtain drug Erdafitinib, has been synthesized in reasonably good yield using 4-bromobenzene-1,2-diamine (4) and 2-bromo-1-(1-methyl-1H-pyrazol-4-yl)ethan-1-one (3) as raw materials, triethylene diamine (DABCO) as catalyst, and tetrahydrofuran as solvent. To the best of our knowledge, this is the first time compound 5 has been acquired by the proposed method.


Datum: 01.12.2021


Optimized Synthesis of the O-Benzoylaminobenzoic Acid Derivative 2-Benzoylamino-N-[4-(4,6-Dimethylpyrimidin-2-Ylsulfamoyl)Phenyl]Benzamide Possessing Anxiolytic Activity

An optimized multi-step synthesis of a new highly effective and low-toxicity derivative of o-benzoylaminobenzoic acid amides possessing anxiolytic activity is presented. Anthranylamide and propionic anhydride instead of acetic anhydride were used as starting materials. The number of synthetic steps did not increase as compared to the known method because the hydrolysis of anthranylamide proceeded in an alkaline medium, in which the Schotten–Bauman acylation was carried out. The preparation of 2-benzoylamino-N-[4-(4,6-dimethylpyrimidin-2-ylsulfamoyl)phenyl]benzamide in the final step was modified by replacing the polar aprotic solvent DMF by the less toxic and more environmentally friendly DMSO. Use of more accessible and cost-effective starting materials in combination with Schotten–Bauman acylation, which eliminated environmentally hazardous benzene, was advisable for production of the active pharmaceutical ingredient. The developed laboratory procedure could be successfully used to obtain other biologically active compounds of o-benzoylaminobenzoic acid and their cyclic derivatives.


Datum: 01.12.2021


Sodium Diclofenac Encapsulation: Optimization of Encapsulation Efficiency and Particle Size Using Response Surface Methodology

This study was carried out to optimize conditions for diclofenac microencapsulation using response surface methodology (RSM). The paper describes preparation, characterization and the microencapsulation optimization of diclofenac-loaded pectin-gelatin beads prepared by method of complex coacervation. The obtained particles exhibit the drug encapsulation efficiency varying within 96.79 to 99.55% and the average microparticle size varying from 25.54 to 57.35 μm. The particle surface morphology was analyzed by SEM and the drug–polymer interaction in the particle matrix was studied by FTIR spectroscopy. Statistical analysis reveals that the concentration of carboxymethylcellulose (CMC) is the most important factor influencing the particle size variation while the diclofenac concentration is the most important factor determining the drug encapsulation efficiency. The RSM study gives an experimental domain that allows elaboration of the smallest particles and highest encapsulation efficiency with a desirability of 0.88.


Datum: 01.12.2021


Design, Synthesis and In Vivo Anxiolytic Activity of Novel Flavonoids

Worldwide millions of peoples are suffering from psychological disorders of which anxiety is one of the major and common problems. Knowing statistical reports of anxiety, the present research focused on design of new flavonoid derivatives through molecular docking by using Schrödinger (Maestro 10.5 v), the well-known computational software on the basis of ligand – protein interaction. The most effective flavonoid derivatives with potent Glide score (IC50) values – compounds 3a (–6.824), 3b (–7.215), 3e (–6.239), 3f (-6.679), and 3j (–7.123) – were selected for the synthesis under microwave irradiation in two-step reaction involving the Claisen-Schmidth condensation to form chalcones and oxidative cyclization to form flavonoids. Then, in vivo anxiolytic activity of synthesized derivatives was studied in adult Swiss albino mice using the elevated plus-maze test model. Diazepam (2 mg/kg, IP) was used as standard drug. Compound 3b exhibited most significant anxiolytic activity against GABAA receptor, but other compounds also showed significant anxiolytic effect in mice at 100 and 200 mg/kg doses when compared to Diazepam.


Datum: 01.12.2021


Microspheres Based on a Protein Matrix and Dipyridamole with Possible Inhalation Administration

Inhalation delivery is a promising way of administration of antiplatelet drugs for the prevention of stroke. The bioavailability of drugs poorly soluble in water can be increased if microspheres based on protein molecules are used. Spray drying was used in the present work to obtain sodium caseinate microspheres with an average aerodynamic diameter of 2.8 μm containing a model hydrophobic antithrombotic drug (dipyridamole). The rate of dipyridamole dissolution and its concentration in aqueous solution could be increased if sodium caseinate was used. The obtained results made it possible to develop a strategy for creating systems based on a protein matrix for inhalation delivery of poorly soluble drugs.


Datum: 01.12.2021


Determination of Paclitaxel Solubility and Stability in the Presence of Injectable Excipients

Due to poor aqueous solubility of paclitaxel, cremophor is one of the excipients used to improve solubility in Taxol while it is responsible for a number of adverse effects such as anaphylactic shock. This research was aimed to determine the solubility and stability of paclitaxel in the presence of intravenous injectable excipients. For this purpose, the solubility of paclitaxel was measured in PEG 400, ethanol, miglyol 812, octanoic acid and oleic acid using the shake flask method. Paclitaxel showed the highest solubility in PEG 400 because of possible hydrophobic interaction of the drug with polyethylene chains. The solubility of paclitaxel in ethanol was higher than its aqueous solubility, accentuating the importance of hydrogen bonding. The solubility of paclitaxel was slightly improved in octanoic acid, oleic acid and miglyol 812, presumably for less matching hydrophobic-hydrophilic balance of their molecules with paclitaxel. The stability of paclitaxel was examined in PEG 400, ethanol, and their binary mixture. Paclitaxel exhibited highest stability in the latter case. Probably, this is because of the matching polarity of PEG 400–ethanol mixture with paclitaxel. The effect of anhydrous citric acid on the stability of paclitaxel was also studied. Citric acid significantly improved the stability because it set pH of the prepared compositions in the range of 3 – 5, where paclitaxel exhibited the slowest rate of degradation. The prepared compositions were introduced in aqueous media in various concentrations to study precipitation due to dilution. Precipitation has been observed at all concentrations because paclitaxel is greatly insoluble in water and resists re-dissolving.


Datum: 01.12.2021


HPLC Determination of Myricitrin in Juglans nigra L. Bark

An HPLC method for quantitative determination of myricitrin in black walnut (Julgans nigra L.) bark was developed. The content of the dominant flavonoid myricitrin (myricetin-3-O-α-L-rhamnopyranoside) in J. nigra bark varied from (3.10 ± 0.18) to (3.18 ± 0.14)%. The error of a single determination of myricitrin in the bark was ±5.81% with a confidence probability of 95%.


Datum: 01.12.2021


Potential for the Development of a New Generation of Aminoglycoside Antibiotics

The present review summarizes recent publications devoted to aminoglycosides that study the main types of resistance to antibiotics of this class and the main directions of chemical modification aimed at overcoming the resistance or changing the spectrum of biological activity. Conjugates of aminoglycosides with various pharmacophores including amino acids, peptides, peptide nucleic acids, nucleic bases, and several other biologically active molecules and modifications resulting in other types of biological activity of this class of antibiotics are described. It is concluded that a promising research direction aimed at increasing the activity of antibiotics against resistant strains is the search for selective inhibitors of aminoglycoside-modifying enzymes. This would allow renewal of the use of antibiotics already meeting widespread resistance and would increase the potential of a new generation of antibiotics.


Datum: 01.12.2021


Simultaneous Estimation of Diphenoxylate HCL and Atropine Sulphate in Solid Dosage Forms by High Performance Liquid Chromatography

An easy, precise and specific high performance liquid chromatography (HPLC) method has been developed and validated for the simultaneous estimation of diphenoxylate hydrochloride (HCl) and atropine sulphate in pure raw materials and tablet dosage forms. Various parameters were modified according to column and equipment available and a new method has been developed. An isocratic HPLC SPD-10A system equipped with quaternary pump and a UV detector were used for analysis on C18 (150 mm × 4.6 mm; 50 μm) column eluted with triethylamine buffer (pH 2.7) mixture with acetonitrile at 50:50 (v/v) ratio as a mobile phase. The flow rate was kept at 1.0 mL/min and the detection wavelength was selected at 220 nm. The retention times of atropine sulphate and diphenoxylate HC1 were found to be 1.58 and 4.79 min, respectively for a total runtime of 6 min. The method was validated for linearity, precision, accuracy, specificity, LOQ and LOD parameters and showed linear response in concentration range of 10-60 μg/mL for both drugs with a regression coefficient of 0.995 for diphenoxylate HC1 and 0.996 for atropine sulphate. The prosed method is accurate with percentage recovery of 100.66% for diphenoxylate HC1 and 100.68% for atropine sulphate. The Limit of detection (LOD) was 2.79 mg/mL for diphenoxylate HC1 and 1.884 mg/mL for atropine sulphate; the limit of quantitation (LOQ) was 8.474 mg/mL for diphenoxylate HCI and 5.714 mg/mL for atropine sulphate; and the calculated % assay was 99.57% for diphenoxylate HC1 and 99.71% for atropine sulphate. The method has also proved to be reproducible, robust, less time consuming, accurate and cheap.


Datum: 01.12.2021


Solid-Phase Fluorimetric Determination of Some Nonsteroidal Anti-Inflammatory Drugs in Medicines with the Aid of a Smartphone

A fast and simple method for determining the active ingredients of non-steroidal anti-inflammatory drugs (NSAIDs) meloxicam and tolfenamic, mefenamic, and niflumic acids using digital colorimetry of solid-state fluorescence was developed. The fluorescence of europium and terbium sensitized by the NSAIDs on cellulose paper and in a thin layer of silica gel was studied. Spots of NSAID solutions applied to the matrix exhibited green fluorescence for tolfenamic, mefenamic, and niflumic acids and red fluorescence for meloxicam upon exposure to UV light (365 nm). The fluorescence intensity on the matrix surface was measured using a smartphone. The colorimetric parameters in the RGB system were used as the analytical signal (Ar). The limits of detection and quantitation were 1 – 5 and 3 – 17 μg/mL, respectively, for all considered analytes. The range of determined concentrations was 3 – 500 μg/mL. The proposed method was tested on medicinal products. The relative standard deviation of the analytical results was ≤0.08.


Datum: 01.12.2021


Beneficial Effects of Punica granatum L. Juice and Gallic Acid Against Kidney Oxidative Damage Caused by Sodium Fluoride

The present work was undertaken to study the effect of sodium fluoride (NaF) exposure on renal oxidative stress status in rats and to evaluate the protective effects of both Punica granatum L. (PGJ) juice and gallic acid (GA). Thirty-six maleWistar rats were divided into six groups: C (n = 6) served as a control; NaF (n = 6) were treated with NaF at 100 ppm; NaF+GA(n = 6) were administered NaF at 100 ppm plus 20 mg/kg of GA; NaF+PGJ (n = 6) were treated by both NaF (100 ppm) and PGJ (1 mL); NaF+GA+PGJ (n = 6) were treated with NaF at 100 ppm plus both GA(20 mg/kg) and PGJ (1 ml); and PGJ (n = 6): received 1 mL of PGJ. After three weeks, data showed that NaF administration caused a rise in urea, creatinine, uric acid, and malondialdehyde (MDA) levels and a decrease in glutathione peroxidase (GPx), catalase (CAT), superoxide dismutase (SOD) activities as well as reduced glutathione level. Furthermore, histological examination revealed a moderate inflammatory infiltration. However, supplementation of GA and/or PGJ improved both the renal histological structure and all other studied parameters. The obtained results clearly showed the ability of P. granatum juice and gallic acid to protect renal tissues from oxidative damage caused by sodium fluoride.


Datum: 01.12.2021


On the Possibility of Reducing the Sample Size for Microbiological Examination of Some Pharmaceutical Substances

The possibility of reducing the sample size for microbiological examination of some pharmaceutical substances is considered. Trypticase-soy agar was evaluated for the ability to detect yeast and mold fungi and to isolate the minimal amount of certain types of microorganisms. The minimal sample size for microbiological examination was 0.2 g (mL) for synthetic substances intended for the production of non-sterile drugs and 1.2 g (mL), for sterile drugs. Based on the experimental results, a scheme has been developed for microbiological examination of particular pharmaceutical substances using a reduced sample size


Datum: 01.12.2021


 


Category: Current Chemistry Research

Last update: 11.04.2018.






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