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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

Search for Selective Glua1 Ampa Receptor Antagonists in a Series of Dicationic Compounds

Homologous series of dicationic derivatives based on adamantyl and phenylcyclohexyl fragments in which the cationic groups and the distance between them were varied by using hydrocarbon chains five or six methylene units in length were synthesized. The ability of the dications to block open channels of NMDA and AMPA glutamate receptors was investigated. Pyramidal neurons isolated from the hippocampal CA1 zone were used to study the NMDA channels. Giant cholinergic interneurons of striatum were used in studies of AMPA receptors missing GluA2 subunits. An investigation of the structure—activity relationship of the dications revealed five compounds (IEM-2131, -2132, -2133, -2041, -2297) that surpassed the reference GluA1 AMPA antagonist IEM-1460 in terms of GluA1 AMPA selectivity. IEM-2131, which was an order of magnitude more active than IEM-1460 in AMPA-blocking activity (IC50 = 0.29 and 3 μM, respectively), showed the maximum AMPA activity and selectivity and had five times better AMPA selectivity (101- and 500-fold, respectively). The clinical prospects of the new GluA1 AMPA blockers were discussed.

Datum: 01.06.2022

Structure-Based Design and Structure-Activity Relationship Analysis of Small Molecules Inhibiting Bcl-2 Family Members

Based on a Mcl-1/Bcl-2 dual inhibitor (S1) previously reported by our group, structure-directed molecular design and structure-activity relationship (SAR) analysis were performed to investigate structural features contributing to the Mcl-1/Bcl-2 binding selectivity and affinity. A series of S1 derivatives with various pharmacophores were synthesized, and among these a selective Mcl-1 inhibitor A4 with 5-fold selectivity over Bcl-2 (Ki = 0.37 ± 0.07 μM vs. 1.87 ± 0.21 μM) and a dual Mcl-1/Bcl-2 inhibitor B3 with optimized affinities (Ki = 0.35 ± 0.01 μM for Mcl-1 and 0.81 ± 0.01 μM for Bcl-2) were revealed by fluorescence polarization assay (FPA). The SAR data and binding modes of A4 and B3 examined by molecular docking showed that the p1 pocket having different geometry and binding features between Mcl-1 and Bcl-2 contributed to the specific binding properties of Mcl-1, and the spatial conserved N223 on Mcl-1 and N143 on Bcl-2 were the key residues to form additional hydrogen bonds with the ester of B3. Finally, the apoptosis-inducing potencies of A4 and B3 in the μM range against K562 and MCF-7 cancer cells were consistent with their binding selectivity determined in vitro, and only weak killing was found for these compounds in the normal cells.

Datum: 01.06.2022

Quantitative Determination of Methotrexate, 7-Hydroxymethotrexate, and Methotrexate Polyglutamates in Human Erythrocytes by High-Performance Liquid Chromatography with Mass Spectrometry

Methotrexate is the drug of choice for the treatment of rheumatoid arthritis. However, some patients have no or an insufficient effect if the treatment protocol is followed. Therefore, a need exists to establish patient compliance and to develop an instrumental approach to correct drug therapy. The present work was aimed at developing quantitative determination methods for methotrexate and its metabolites such as 7-hydroxymethotrexate and polyglutamate residues in erythrocytes that possess high sensitivity, selectivity, and rapidity. The proposed quantitative determination method for methotrexate and its metabolites is based on high-performance liquid chromatography with electrospray-ionization (ESI) and mass spectrometric detection (HPLC-MS/MS). The lower limit of quantitation (LLOQ) is 0.5 nmol/L for all analytes. The calibration curve is linear in the range 0.5 – 100 nmol/L. The coefficient of approximation accuracy is no less than 0.99. Samples were prepared by precipitation of a homogenized erythrocyte mass. The method was tested in clinical study No. 0514-2018-0003 using local ethics committee protocol No. 23 of Sept. 20, 2018.

Datum: 01.06.2022

Optimization of Phenolics Extraction from Strobilanthes cusia Leaves and their Antioxidant Activity

Strobilanthes cusia (Nees) Kuntze is commonly used as a traditional medicine with widespread health benefits. This work proposed S. cusia leaves as a potential source of phenolic compounds for extraction and examined the antioxidant capacity of the phenolic-rich extract. Several solvents (ethanol, methanol, and water) were screened as extractants. Among these, methanol showed the highest extraction efficiency. Single-factor experiments and response surface methodology were then applied to optimize the extraction conditions. The maximum total phenolic content of 64.86 ± 0.32 mg GAE/g was obtained under the following extraction conditions: extraction time, 2.27 h; methanol-to-material ratio, 9.55 mL/g; aqueous methanol concentration, 63.54%. The phenolic-rich extract showed potential antioxidant capacity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical at an IC50 value of 464.59 μg/mL. This study shows that S. cusia leaves are rich in phenolic constituents and suggests S. cusia leaf extracts as promising antioxidant agents for future applications.

Datum: 01.06.2022

Antioxidant and Genoprotective Properties of α-Lipoic (Thioctic) Acid in Blood Serum Under X-Ray Exposure

α-Lipoic (thioctic) acid (ALA), which is used as a drug for the treatment of diabetic and alcoholic neuropathy and several other diseases, was found to be an effective antioxidant that effectively neutralized the products of water radiolysis and reduced oxidative damage to DNA and proteins caused by x-ray exposure. ALA had different effects on the formation and decay of long-lived reactive species of albumin and globulin in blood serum. This process was accompanied by the generation of hydrogen peroxide and prolongation of post-exposure oxidative stress. ALA in the concentration range 0.05 – 0.4 nM eliminated oxidative damage of DNA in vitro although the efficiency decreased with increasing concentration. ALA also exhibited genoprotective and radiomitigatory properties in vivo by reducing the formation of micronuclei in polychromatophilic erythrocytes of red bone marrow in mice after irradiation. The obtained results and available literature data indicate that ALA in the effective pharmaceutical window is a promising therapeutic radiomitigator capable of preventing harmful consequences caused by the disturbance of redox homeostasis due to radiation-induced oxidative stress.

Datum: 01.06.2022

Synthesis and Biological Activity of 5-alkoxy- and 5-amino-substituted 3-bromo-4-nitro-1-(thietan-3-yl)-1H-pyrazoles

5-Alkoxy- and 5-amino-substituted 3-bromo-4-nitro-1-(thietan-3-yl)-1H-pyrazoles were synthesized by reactions of 3,5-dibromo-4-nitro-1-(thietan-3-yl)-1H-pyrazole with sodium alcoholates and primary amines. The structures of the synthesized compounds were established by IR, PMR, and 13C NMR spectroscopy. In vitro studies of the antiplatelet, anticoagulant, and antioxidant activity revealed promising compounds, including 3-bromo-5-methoxy-4-nitro-1-(thietan-3-yl)-1H-pyrazole with antioxidant action and 2-{[3-bromo-4-nitro-1-(thietan-3-yl)-1H-pyrazol-5-yl]amino}ethan-1-ol with an antiplatelet effect. Results of in silico calculations predicted the absence of toxic risks (mutagenicity, oncogenicity, reproductive toxicity, local irritation) and acceptable bioavailability (in terms of the topological polar surface area).

Datum: 01.06.2022

Synthesis and Antinociceptive Activity of GABA and Pyroglutamic Acid Short Peptides

The antinociceptive activity of new synthesized short peptides of γ-aminobutyric acid (GABA) with pyroglutamate (pGlu) – pyroglutamyl GABA (pGlu-GABA), pyroglutamyl GABA ethyl ester (pGlu-GABA ethyl ester), and pyroglutamyl diGABA (pGlu-GABA-GABA) – has been investigated. The peptides were administered to rats in a dose of 20 mg/kg separately and in combination with pregabalin, in the same dose. Results of the tail flick test demonstrated that intraperitoneal administration of all the investigated substances exhibited antinociceptive activity, leading to increase in the tail flick latency time. The maximum value of the tail flick latency for all peptides was manifested after 90 min of administration and was higher compared to the same characteristics in the control group as follows: for pGlu-GABA, 20.5%; for pGlu-GABA ethyl ester, 40.99%; and for pGlu-diGABA, 33,23%. In addition to the own antinociceptive activity of investigated peptides, the ability to potentiate the analgesic efficacy of pregabalin was revealed.

Datum: 01.06.2022

Design, Synthesis and Antifungal Activity of Phloroglucinol Derivatives

Phloroglucinols of Dryopteris fragrans (L.) Schott plant show strong antifungal activity. In previous work, we isolated a wide range of phloroglucinols from the plant and found that pseudoaspidinol of D. fragrans and its structural modifications (methylphloroglucinol derivatives) showed stronger antifungal activity and confirmed that the butyryl group of these compounds accounted for this activity. In this study, we designed a series of phloroglucinol derivatives (A1–A9) and methylphloroglucinol derivatives (B1–B9) by introducing acyl groups with diverse carbon numbers in the C-2 position, synthesized these compounds, and evaluated the anti-dermatophyte activity of compounds A1–A5 and B1–B5 on Trichophyton rubrum and Trichophyton mentagrophytes fungal species. The results showed that compound A5 exhibited the strongest activity. These compounds can be used as leads for the development of new antifungal agents.

Datum: 01.06.2022

A New Reverse-Phase High Performance Liquid Chromatography Method for Simultaneous Estimation of Fimasartan, Rosuvastatin Calcium, and Amlodipine Besylate in Combination

A reverse-phase high performance liquid chromatography (RP-HPLC) method was developed and validated for simultaneous estimation of fimasartan (FIM), amlodipine besylate (AML) and rosuvastatin calcium (ROS) in combination for the treatment of hypertension with dyslipidemia presenting a major risk factor for cardiovascular diseases. Chromatographic separation was performed on stationary reverse-phase inert sustain-swift C18 100A° (250 mm × 4.6 mm, 5 μm i.d.) column. The optimized mobile phase acetonitrile – methanol – water (15:15:70, v/v, at pH 3.5 adjusted with 0.1% ortho-phosphoric acid) was pumped at a flow rate of 1.0 mL/min and the effluent spectrum was monitored at 230 nm. Calibration graphs of drugs constructed at their wavelengths of determination were linear in a concentration range of 10 – 100 μg/mL for all three components. The retention times for FIM, ROS calcium, and AML peaks at 230 nm were found to be 4.6, 6.4, and 10.8 min respectively. The method suggested usefulness of a unique mobile phase during the estimation of two or more multicomponent dosage forms. Due to its simplicity, rapidness, high precision, and accuracy, the proposed RP-HPLC method can be applied for simultaneous determination of FIM, ROS and AML in bulk mixture.

Datum: 01.06.2022

(S)-(–)-N-[2-(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide Inhibits Neuroglioma Cell Growth Through Inducing Apoptosis

Neuroglioma is an aggressive type of cancer in the central nervous system without effective treatments. (S)-()-N-[2-(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide (SNA) is a new compound isolated from Selaginella pulvinata plant with potent inhibitory activity against melanoma cell proliferation through increasing apoptosis. This study further investigated effects of SNA against neuroglioma and explored the underlying mechanisms. Neuroglioma H4 cells were treated with various SNA concentrations and MTT assay was used to detect the SNA effects on cell proliferation. Wound healing and cell invasion assays were used to measure the cell migration, Annexin V/PI staining was used to detect apoptosis. Western blot was used to detect the expression of proteins. SNA significantly inhibited the proliferation of H4 cells and suppressed the cell migration. Moreover, SNA increased cell cycle arrest and induced the apoptosis. Our data demonstrated that SNA could be a potential anti-tumor drug against neuroglioma.

Datum: 01.06.2022

Synthesis and Antiproliferative Activity of 2-oxo-1,2-dihydropyridine-3,4-dicarbonitriles

A series of 2-oxo-1,2-dihydropyridine-3,4-dicarbonitriles were synthesized. Their antiproliferative activity was studied. Substituents in the pyridine ring 5- and 6-positions influenced the activity of the molecules. 2-Oxo-2,5,6,7-tetrahydro-1H-cyclopenta[b]pyridine-3,4-dicarbonitrile and 2-oxo-6-tert-butyl-1,2,5,6,7,8-hexahydroquinoline-3,4-dicarbonitrile slightly inhibited the growth of leukemia (with a tendency to a greater degree for K-562 and SR), brain cancer (with a tendency to a greater degree for SNB-75), prostate cancer (with a tendency to a greater degree of PC-3), and breast cancer cell lines (with a tendency to a greater degree for MCF-7).

Datum: 01.06.2022

Antibacterial, Antioxidant and DNA Cleavage Activity Evaluation of Substituted Phenylureido Sulfaguanidine and Sulfamethazine Derivatives

A series of six N-carbamimidoyl-4-(3-substituted phenylureido) benzenesulfonamides (SG1-SG6) and six N-(4,6-dimethylpyrimidin-2-yl)-4-(3-substituted phenylureido) benzenesulfonamides (SM1-SM6) were successfully re-synthesized to determine their antibacterial, antioxidant, and DNA cleavage activities. In general, all compounds showed moderate to good activity against Gram-positive strains (S. aureus and E. faecalis) and Gram-negative strains (P. aeruginosa and E. coli). More specifically, compound SM6 showed great potency against all the tested bacterial strains. One compound (SM5) among the series tested, showed great potency against P. aeruginosa strain (minimal inhibitory concentration, MIC = 7.8 μg/mL), which was comparable with MICs of the standard drugs ampicillin and ceftriaxon (3.9 and 15.6 μg/mL, respectively). On the other hand, a weak antioxidant activity was observed using DPPH free radical scavenging assay. Taken together, several compounds from the current series might be interesting lead derivatives to develop more potent compounds against the test bacterial strains.

Datum: 01.06.2022

Skin Wound Healing Potential and Antioxidant Effect of Hyaluronic Acid Extracted from Mytilus galloprovincialis and Crassostrea gigas

This research work was devoted to studying the ability of hyaluronic acid (HA) to treat skin wounds in rats. HA, an immune-neutral polysaccharide, is widespread in the human body as it is necessary for several tissues and cellular functions and has been used in the clinical practice for more than three decades. For this purpose, we attempted to obtain and enrich HA-containing extracts from two species of molluscs collected at Bizerte lagoon, namely Mytilus galloprovincialis and Crassostrea gigas. Then, the wound healing potential of purified HA (hyaluronan) was tested on Wistar rats which were separated into 4 groups: control, treated with a marketed healing cream “Avene Cicalfate”, treated with HA isolated from M. galloprovincialis, and treated with HA isolated from C. gigas. After anesthesia, rats were submitted to back skin lesions (diameter 2 cm) and then treated daily until recovery. During the experiment, variation of the wound area was monitored. Results showed that the obtained net yield of HA was 3.8 mg/g dry weight and 1.9 mg/g dry weight for M. galloprovincialis and C. gigas respectively. Morphological analysis demonstrated that HA significantly accelerated wound repair through reepithelization. The mean wound surface was completely absent after 15 days of treatment with C. gigas hyaluronan. Based on these findings, it appears that mollusc HA has an obvious healing activity completely in accordance with its recognized effectiveness in dermo-cosmetology.

Datum: 01.06.2022

Simultaneous Estimation of Acetaminophen, Chlorpheniramine Maleate, Methyl Paraben, Propyl Paraben, Sodium Benzoate and Related Impurities in Over-the-Counter Syrup Formulation

Acetaminophen, chlorpheniramine maleate syrup is an over-the-counter (OTC) non-compendial syrup dosage form. Compendial monograph methods are not available for this product. Therefore, a single stability indicating method for the estimation of acetaminophen, chlorpheniramine maleate and possible degradation products has been developed and validated. The chromatographic separation was achieved on Phenomenex Phenyl Hexyl, (150 × 4.6 mm, 5.0 μm) HPLC column at a mobile phase flow rate of 1.0 mL/min and the detection was made at 225 nm wavelength. The correlation coefficient (r) for each analyte was more than 0.99. The reported method is precise, accurate, and robust in estimating active substances, preservatives, and related impurities. To the best of authors’ knowledge, the proposed method is the first report of a single stability-indicating HPLC method for the simultaneous determination of active substances, preservatives and impurities in Acetaminophen, Chlorpheniramine Maleate OTC syrup formulation throughout the product shelf-life.

Datum: 01.06.2022

Physicochemical and Bioassay Directed GC-MS Analyses of Chloroform Extract of Pteris cretica L.

This study was aimed to explore the potential of Pteris cretica L. to be used as herbal remedy. The P. cretica dried plant powder was subjected to a standard physicochemical (proximate analysis) protocol, which showed promising results and was consistent with the WHO recommended ranges that are required to use the plant as a remedy. To identify the bioactive chemical constituents of chloroform extract, the extract was subjected to a series of column chromatography and p-HPLC through the antibacterial and antioxidant bioassays guidance. The two most bioactive sub-fractions of chloroform extract were subjected to GC-MS analysis which revealed the presence of seventeen compounds, the major constituents being eicosane (16.8%), hexadecane (14.1%), methyl hexadecanoate (11.2%), 3,3,8-trimethyldecane (9.1%), 2,6,10-trimethyldodecane (7.8%), tricosane (5.1%) and tetradecane (3.86%). Proximate analysis results show that P. cretica plant is good for herbal remedy, and the bioassay results on chloroform fractions and sub-fractions show that this plant has significant antibacterial and antioxidant potentials. To use this plant as herbal remedy, there is need in further exploration.

Datum: 01.06.2022

Methodological Approaches to Standardization of Rhizomes and Roots of Eleutherococcus senticosus

Methodological approaches to the analysis of biologically active compounds in rhizomes and roots of Eleutherococcus senticosus (Rupr. et Maxim.) Maxim. [syn. Acanthopanax senticosus (Rupr. et Maxim.) Harms] were substantiated. An HPLC method for assay of eleutheroside B (syringin) and a spectrophotometric method for determination of the total content of phenylpropanoids in terms of eleutheroside B (syringin) isolated from medicinal plant raw material after preliminary purification and filtration through a layer of aluminum oxide were developed and validated. The total content of phenylpropanoids in roots and rhizomes of E. senticosus was found to vary from 0.30 ± 0.02% to 0.37 ± 0.02%; eleutheroside B, from 0.041 ± 0.002% to 0.089 ± 0.003%. Results of statistical processing indicated that the relative error of determining the mean total of phenylpropanoids and eleutheroside B (syringin) did not exceed ±5.0% at a confidence level of 95%.

Datum: 01.06.2022

Influence of Manufacturing Technology on the Properties of Active Pharmaceutical Ingredients of Prostate Extract

Important peculiarities of various technologies used for manufacturing the API of prostate extract that determine different qualitative characteristics of the final product are described. Data on the physicochemical and biological properties of APIs essential for the production of finished dosage forms possessing the desired safety and efficacy indices are presented. The key quality parameters of APIs produced by various technologies are comparatively analyzed.

Datum: 01.06.2022

Implants as Targeted Drug Delivery Systems (Review)

This review considers implants as modern drug delivery systems. Methods of their production by hot melt extrusion, direct pressing, and 3D printing are described. The advantages and disadvantages of implants produced by different methods are shown. The nomenclature and basic requirements for excipients necessary for effective use of the dosage forms are given. An assortment of polymers used to produce biodegradable and non-biodegradable implants is presented. Requirements for excipients for a particular method of producing a drug delivery system are described. The prospects and advantages of in situ implants as an alternative technology to produce drugs for targeted therapy are shown. Recent developments and drugs already approved for implants for ophthalmic, dental, and intranasal application and for targeted therapy of oncological diseases are reviewed.

Datum: 01.06.2022

Synthesis and Analgesic and Anti-Inflammatoryactivity of 5-aryl-4-acetyl-3-hydroxy-1-carboxymethyl-3-pyrrolin-2-ones

A series of 5-aryl-4-acetyl-3-hydroxy-1-carboxymethyl-3-pyrrolin-2-ones were synthesized by reacting acetylpyruvic acid methyl ester with a mixture of an aromatic aldehyde and glycine in glacial acetic acid and distilled water. The analgesic activity of the obtained compounds was studied using the hot-plate test. Their anti-inflammatory activity was determined using the model of aseptic carrageenan-induced inflammation. It was found that the synthesized compounds had pronounced analgesic activity and belonged to low-toxicity substances.

Datum: 01.06.2022

Cytotoxic Activity of Extracts from the Intact Plant and Cell Cultures of Podophyllum peltatum Against Cervical Cancer Cells

Cell cultures of the root, bud, and fruit of Podophyllum peltatum were obtained at VILAR. The cytotoxic activity of extracts from various plant organs and cell cultures was studied. The primary characteristics of the plant metabolome responsible for this activity were determined. Ultra-performance liquid chromatography identified derivatives of ellagic, caffeic, and gallic acids; flavonoids; and podophyllotoxins in Me2CO extracts of P. peltatum cell cultures. Results of the resazurin test showed that the Me2CO extracts of the plant organs reduced the viability of HeLa cells by 52 – 62%; extracts of callus cultures, by 52 – 76%; and extracts of suspension cultures, by 12 – 88%. The most stable cytotoxic activity was shown by extracts of P. peltatum rhizomes and roots (reducing test cell viability by 52 – 60%) and extracts of callus (53 – 74%) and suspension cultures (20 – 60%) obtained from the plant root. Thus, callus and suspension cell cultures of P. peltatum root can serve as inexpensive and convenient raw materials for the production of antitumor compounds, which corresponds to rational nature management as one of the priority tasks of the modern pharmaceutical industry.

Datum: 01.06.2022


Category: Current Chemistry Research

Last update: 11.04.2018.

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