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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

Advance on Traditional Uses, Phytochemistry and Pharmacology of Lycium ruthenicum MURR.

Lycium ruthenicum Murr. (LR) is a medicinal and edible plant in China, which has a variety of medicinal values and health benefits and is used as traditional medicine for a variety of conditions, including heart complaints, irregular menstruation, and menopause. Based on analysis over two decades of documented literature, a comprehensive up-to-date review has been compiled covering traditional and folk medicine uses, phytochemistry and pharmacology of LR, with a view to providing a scientific platform for its further development and utilization. Relevant data were obtained through systematic electronic searches into various scientific databases, including PubMed, Web of Science, Google Scholar, Science Direct, Wiley, Springer, as well as the ancient and modern literature. The chemical constituents of LR include anthocyanins, polysaccharides, flavonoids, procyanidins, phenolic acid, alkaloids and other important substances. So far, more than 90 compounds have been isolated from LR, among which the content of anthocyanins is highest and is the main component, leading to recognition of LR as “King of Anthocyanins” and “Blue Demon King”. The content of anthocyanins in LR reaches up to 387.9 mg/100 g. Modern pharmacological research has revealed multiple activities of LR, including anti-oxidant, anti-aging, blood lipid-lowering, and glucose-lowering properties. The antioxidant activity of LR is currently the most studied and the most in-depth. Reports on the chemical components of LR have mostly focused on single species, and no systematic studies have been conducted to date, the material basis related to the traditional effects has not yet been clarified. Therefore, follow-up research should focus on the relationship between pharmacology and structural characteristics of the majority of ingredients of LR, and chemical ingredients closely related to traditional functions. Systematic research on the phytochemistry and pharmacology of LR is essential to provide a basis for further development and guide in its traditional use.

Datum: 01.10.2022

Assessment of the Quality of Herbal Teas from Šabac, Serbia in Terms of the Content of Heavy Metals

Chemical components of teas have received great interest because they are related to health. In this work, data on the determination of foreign matter, loss on drying/water content, total ash and ash insoluble in hydrochloric acid are presented. The content of seven heavy metals including Cu, Fe, Mn, Zn, Ni, Cd and Pb were determined by atomic absorption spectrometry in samples of several herbal teas: Matricariae flos, Thymi herba, Menthae piperitae folium, Betulae folium, Quercus cortex, Gentianae radix, Frangulae cortex, Althaeae radix, Uvae ursi folium and Glycyrrhizae radix collected from Šabac’s market, Serbia. The sample preparation procedure involved dry digestion and dissolution of the ash in 6M HCl and then in 0.1 M HNO3. Herbal teas showed the concentration of heavy metals Cu, Fe, Mn, Zn and Ni in the range: 2.9 ± 0.1 – 22.2 ± 0.9 mg/kg, 118.5 ± 1.1 – 755.5 ± 2.5 mg/kg, 19.0 ± 5.8 – 561.0 ± 1.9 mg/kg, 6.5 ± 0.4 – 242.5 ± 1.4 mg/kg and 2.5 ± 0.1 – 10 ± 1.1 mg/kg, respectively. The level of copper in all samples was uniform. The highest content of Fe was in Thymi herba, while Mn and Zn were at maximum in Betulae folium. The levels of toxic heavy metals Cd and Pb were below the detection limit. The obtained values were compared with data available from literature. The herbal tea samples analyzed contained essential heavy metals (Cu, Fe, Mn, Zn) and probably essential in trace (Ni), and could obey the daily dietary requirements. Noncancer health risk assessment detected that the herbal teas of Betulae folium and Frangulae cortex can manifest some health risk to consumers.

Datum: 29.09.2022

Development of a Quantitative Determination Method for the Active Substances in Timogel Combined External Preparation

A quantitative determination method for metronidazole, chlorhexidine, and methylparaben in commercial Timogel gel for the treatment of wounds and burns is presented. The analyses were carried out using an HPLC method on a Hewlett Packard chromatograph with a spectrophotometric detector. The conditions for the maximum sensitivity for determining the active substances in the medical product were selected. The proposed technique could be used to estimate the quantitative content of metronidazole, chlorhexidine, and methylparaben in combined external drugs. All procedures tested on laboratory batches of gel showed reproducible results and could be recommended for inclusion in regulations on the technology and quality control of the wound-healing gel.

Datum: 22.09.2022

New Water-Soluble IR Photosensitizer in the Bacteriochlorophyll a Series

Chlorin and bacteriochlorin derivatives are at present the most promising compounds used in photodynamic therapy. However, the use of these photosensitizers (PSs) in clinical practice is limited because of their low solubility in biological fluids. A water-soluble dipropoxybacteriopurpurinimide (DPBI) conjugate with Pluronic F-127 was synthesized in the present work. It was shown that conjugation with the poloxamer did not affect the physicochemical and photophysical properties of the starting PS. It was found during biological tests that the resulting conjugate had photodynamic and pharmacokinetic properties similar to those of the original DPBI pigment. The advantages of the proposed PS were demonstrated in an acute toxicity study. Intravenous administration of the PS at 10 times the therapeutic dose did not cause the death of test animals, in contrast to a DPBI emulsion in water.

Datum: 21.09.2022

In Vitro Cytotoxicity of Methano[1,2,4]Triazolo-[1,5-C][1,3,5]Benzoxadiazocine Derivatives and Their Effects on Nitrite and Prostaglandin E2 (PGE2) Levels

Biological activity of the Biginelli type heterocycles is extremely broad and provides a suitable platform for the discovery of potent small drug-like molecules. Such activity of 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives is widely known, whereas their oxygen-bridged analogs, benzoxadiazocines, are presented quite rarely in the literature. In this study, a series of new methano[1,2,4]triazolo[1,5-c][1,3,5]benzoxadiazocine derivatives (3a-3j) were evaluated in vitro for their activities and molecular docking features. According to the molecular docking study, COX-2 and PGE2S appeared as likely targets responsible for the reduced PGE2 levels caused by the title compounds. The cytotoxicity of compounds 3a-3g, 3j was evaluated on RAW 264.7 murine macrophage cell line by MTT assay after treatment for 24 h with various doses (25, 50, 100 μM) of these compounds. Then, compounds admitting cell viability higher than 70% were tested for their anti-inflammatory activity at non-toxic doses by evaluating the nitrite level of cell supernatants with the Griess reagent. Compounds 3c and 3f demonstrated significant inhibition of nitrite production (by 29 and 25%, respectively) at 100 μM (p < 0.05). These compounds significantly inhibited PGE2 production, thus suggesting analgesic activity.

Datum: 21.09.2022

Synthesis and In-Vitro Evaluation of Raloxifene–Oxalyl Chloride Conjugate Targeting Breast Cancer

Anticancer drugs mostly produce minimal to severe side effects due to lack of selectivity. The present work envisaged selective targeting of MCF-7 breast cancer cells by synthesizing an ester conjugate using oxalyl chloride of drug raloxifene targeted for steroidal estrogen receptor alpha. The objective was to synthesize and evaluate raloxifene–oxalyl chloride conjugate as anticancer drug with side effects reduced by increasing selectivity. Synthesis of the conjugate was carried out by reflux condensation of acid chloride of oxalyl chloride with raloxifene. In vitro methods viz. lipophilicity, solubility, protein binding, drug release and permeation, hydrolysis, and cytotoxicity were employed for characterization and evaluation of the drug conjugate. The solubility and partition coefficient studies had an outcome of better solubility and lipophilicity while protein binding studies revealed a low protein binding capacity of the drug conjugate. The hemolytic study showed lesser RBC lysis with significant cytotoxicity compared to the parent drug and a selective diffusion at the pH of cancer cells rather than pH of normal cells, and hence increasing the specificity and minimizing the adverse effects. Hydrolytic study of the conjugate signified minimal hydrolysis of the conjugate at various pH, simulated gastric fluid, and simulated intestinal fluid. The synthesized conjugate thus ratifies to be a useful prodrug in reducing the systemic toxicity of raloxifene as well as selectively targeting the cancerous cells.

Datum: 21.09.2022

Synthesis and Evaluation of New 5,15-Diarylporphyrin Derivatives for Photodynamic Therapy

Two new 5,15-diarylporphyrin derivatives (L1 and L2) were designed and synthesized and their anti-esophageal cancer effects as photosensitizers were evaluated. Both compounds have strong absorption band at 645 – 655 nm in UV-Vis spectra, obvious singlet oxygen generation ability, and fluorescence emission around 657 – 674 nm under laser excitation. Under photodynamic therapy (PDT) conditions, they could significantly inhibit the growth of Eca-109 tumor cells. In particular, compound L1 exhibited excellent photodynamic antiproliferative effect and is worthy of further development.

Datum: 20.09.2022

Method for Obtaining and Hypolipidemic Activity Assay of a Lipolytic Enzyme from Nigella sativa Seeds

A lipolytic enzyme was isolated from seeds of Nigella sativa after pressing the oil to develop a waste-free technology. An enzyme with a maximum lipolytic activity of 150,000 U/g was obtained by selecting the optimum temperature (37°C) and pH (10.5). A comparative study of the lipolytic enzyme and sebelipase alfa in the Tween hyperlipidemia model in rats showed that the former decreased the concentration of total cholesterol by 19.6%, which indicated the expediency of using this enzyme to improve absorption processes in the gastrointestinal tract.

Datum: 20.09.2022

Using a Conductometric Method in Microbiological Control of Natural Excipients

The “microbiological purity” criterion is an important quality attribute of non-sterile drugs and excipients in the pharmaceutical industry. The impedance conductometry method of microbiological analysis (ICMMA) is based on monitoring of changes in the impedance (resistance to alternating electric current) of liquid growth medium resulting from the living activity of microorganisms contained in the analyzed sample. The aim of this work was to determine the possibility of using ICMMA for determining the total number (TN) of aerobic microorganisms in natural excipients. As a result, the TNs determined by conductometric and pharmacopoeial two-layer agar methods converged with a correlation coefficient of 0.95. This allowed the conductometric method to be recommended as a routine method for determining the TN of aerobic microorganisms when analyzing the microbiological purity of excipients intended for pharmaceutical production.

Datum: 20.09.2022

Analysis of Eleutherosides by Tandem Mass Spectrometry: Possibilities of Standardizing a Multi-Phytoadaptogen Formulation for Preventive Oncology

The major bioactive constituents in extracts from roots of Eleutherococcus senticosus (Rupr. & Maxim) (Araliaceae) and in a multi-adaptogen herbal formulation (Multiphytoadaptogen) were analyzed using high-performance liquid chromatography (HPLC) in combination with tandem mass spectrometry. Chromatography was performed on an ACQUITY UPLC BEH C18 column in gradient mode. A TSQ Vantage triple quadrupole mass spectrometer with electrospray ionization was used for the analysis. Eleutherosides B (syringin, a phenylpropanoid) and E (syringaresinol diglucoside, a lignan) were identified in both the multi-adaptogen herbal formulation and E. senticosus root extract. The results could be used for standardization and quality testing of herbal formulations including eleutherosides B and E and for justification of the biological action of Multiphytoadaptogen and studies of its new properties considering the identified bioactive constituents. The probable mechanisms of the antitumor and additive/synergistic effects of eleutherosides B and E were established by in silico analysis of their biological activity profiles.

Datum: 20.09.2022

Relevance of Using Platinum-Containing Antitumor Compounds (A Review)

This review describes various platinum complexes including heterocyclic fragments such as gemcitabine, satraplatin, fuplatin, etc. and covers data published over the last 20 years concerning the effectiveness of using platinum-containing drugs in antitumor therapy. Preparations of various genesis, structure, and intracellular conformations and possible mechanisms of action, biochemical properties, and some physicochemical parameters of these compounds are considered. Adducts of different nature and geometric structure have different intracellular repair reactions, cleavage of functional groups, and interaction with untwisted DNA in affected cells. In turn, molecules capable of targeted drug delivery of substances such as fullerenes and their water-soluble derivatives fullerenols as well as polymeric compounds (in particular, cucurbituril) used in the synthesis of platinum-containing biologically active compounds are gaining increased interest. Thus, research is also being conducted on selective targeted delivery of platinum-containing series with reduced toxicity in parallel with the search for the most effective compounds. This review cites data on biological modeling of the effectiveness, mechanism, and kinetics of active platinum-containing drugs. An important aspect is that all antitumor substances are synthesized under rational accessible conditions and have logical pathways for continuing work on the synthesis of analogs capable of stimulating the apoptosis of cancer cells.

Datum: 20.09.2022

Interaction of Imidazo[4,5-a]Acridines with Acetylcholinesterase

The present work deals with the synthesis, spectral characterization and the interaction of new tetracyclic imidazo[4,5-a]acridines with acetylcholinesterase (AChE) enzyme. This compound was obtained via hydrolysis in the CN group of 8-methoxy-3-methyl-3H-imidazo[4,5-a]acridine-11-carbonitrile in high yield. The target compound was synthesized from the reaction of 1-methyl-5-nitro-1H-benzo[d]imidazole with 2-(4-methoxyphenyl)acetonitrile in basic medium. The catalytic activity of AChE was investigated in the presence of title compound and inhibition constants were determined for the reversible enzyme–inhibitor complex. Based on the mixed inhibition model, inhibition constant for the title compound was 0.097 mM. Molecular modeling of the complex (ligand–enzyme) was used to determine amino acid residues of the active site involved in the interaction. In the presence of the ligand in some regions, such as residues 80 – 87, 328 – 347, 433 – 440, 484 – 492 and the N-terminal residues, the flexibility of the AChE residues has decreased. Also, the calculations show that the new ligand interacts with the active site of AChE. The Trp84, Phe330, and His440 residues play a role in this interaction. These residues are located in the cavity of the AChE binding site. Trp84 and His440 are located at the bottom of the cavity, and Phe330 occurs in the middle of the cavity. These residues exhibit hydrophobic interaction with the new ligand. Also, the ligand has altered the secondary structure of AChE. The helical secondary structure of AChE is most affected by the ligand.

Datum: 20.09.2022

Bactericidal and Fungicidal Properties of Some Antiseptic Drugs and Disinfectants

Analytical results for the bactericidal and fungicidal properties of some antiseptic drugs and disinfectants are presented. Regulatory and pharmacopoeial documentation concerning these issues was compared. Differences were revealed among the test microorganisms, conditions of procedures, methods of assessment, and quality requirements. Within the framework of this study, a general approach to the analysis has been formulated, a technique was developed and verified, and the applicability of the proposed method of sample neutralization by membrane filtration of antiseptic drugs and disinfectants was proven.

Datum: 20.09.2022

In-Silico Study, Preparation and Biological Evaluation of 99MTC-Mesalamine Complex as Radiotracer for Diagnostics and Monitoring of Ulcerative Colitis in Mice

This work centralizes on pursuit ulcerative colitis localized in mice. High radiolabeling and purity were ensured during the formation of a radiotracer, [99mTc]nitrido-mesalamine complex, due to inspecting many parameters under optimum conditions including pH of the reaction mixture (pH 6), reducing agent content (tin(II), 50 μg), reaction time (30 min), mesalamine content (200 μg), Tc-99m (200 – 350 MBq), stability in rat serum (24 h), and reaction temperature (37°C) giving high radiolabeling yield of 98%. In silico molecular docking study was performed to evaluate the possible mechanism of action on the target peroxisome proliferator-activated receptor gamma (PPARγ). Results of biological studies obtained in this work illuminate the usefulness of [99mTc]nitrido-mesalamine complex as a radiotracer that can be used for ulcerative colitis imaging up to 24 h in microbial model (76% dose/g organ (ID/g)) as monitored in mice.

Datum: 20.09.2022

Synthesis and Cytotoxic Activity on Cell Cultures of New Azolotriazines

Results from studies of the cytotoxic activity of new azolo[5,1-c][1,2,4]triazine derivatives to establish the potential of using them as antitumor agents, including for breast cancer chemotherapy, are presented. The spectral characteristics confirmed that the obtained compounds were highly pure and stable on storage. The cytotoxicity was determined using the methyltetrazolium (MTT) test against MCF-7 and CHO cell lines. The compounds were used at final concentrations from 0.25 to 10.0 μM. Two imidazo[5,1-c][1, 2, 4] triazines (5a and 5d) had calculated half-maximal inhibitory concentrations (IC50) for MCF-7 several times lower than the reference drug epirubicin. The cytotoxicity of all newly synthesized derivatives was lower than that of epirubicin with respect to untransformed CHO cells. This further indicated the potential of these compounds. The results can be used as a basis for selecting compounds 5a and 5d as substances with potential antitumor activity for further studies of their genotoxic and metabolic properties on cell models and laboratory animals.

Datum: 20.09.2022

Radiocomplexation, Chromatographic Separation and Bioevaluation of [99mTc]Dithiocarbamate of Procainamide as Selective Labeled Compound for Myocardial Perfusion Imaging

Cardiac imaging is one of the most important tools for diagnosing many diseases related to the heart. This work was devoted to developing this method using experiments on mice. The formation of a complex of [99mTc]dithiocarbamate of procainamide under optimum conditions of reaction temperature (37°C), reaction time (30 min), pH of the reaction mixture (8), amount of substrate (100 μg), amount of reducing agent tin(II) (content, 50 μg), and stability in rat serum (8 h) was achieved using radioactive Tc-99m (300 – 500 MBq) to give high labeling yield (98.5%) and radiochemical purity. Procainamide works through sodium channel blocker. Normal mice were used in biodistribution investigations. High absorption uptake of the [99mTc]dithiocarbamate of procainamide complex was found to be 33.47 ± 0.83% injected dose/g organ (ID/g) as observed in mice for up to 5 min, which demonstrated its usefulness as a radiotracer for heart imaging.

Datum: 20.09.2022

Synthesis of 3,3-Dimethyl- and 3,3-Diethyl-Substituted 2-(3,4-Dihydroisoquinolin-1-yl)Carboxylic Acid Amide Hydrochlorides and Their Anti-Arrhythmic, Hemostatic, Anthelmintic, and Larvicidal Activity

Series of 3,3-dimethyl- and 3,3-diethyl-substituted 2-R-(3,4-dihydroisoquinolin-1-yl)acetamides were synthesized via Ritter reactions of 1-(3,4-dimethoxyphenyl)-2-methylpropanol-2 and 1-phenyl-2-ethylbutanol-2 with 2-R-cyanoacetamides (R = Et, n-Pr, i-Pr, n-Bu, n-Am, and i-Am). The hydrochlorides of the obtained compounds were tested for anti-arrhythmic activity using the CaCl2 model. Three of ten compounds showed anti-arrhythmic activity with a maximum anti-arrhythmic index (AI) of 3.9.With respect to blood clotting, all compounds proved to be hemostatics. The most active compound increased the blood coagulation index up to 37.9%. Eight compounds exceeded pyrantel and two compounds exceeded levamisole with respect to anthelmintic activity. Larvicidal (insecticidal) effects were observed for nine compounds, two of which reduced the larvae life span to 10.6 and 10.4 min, thus exceeding the effect of diazinon (17.0 min).

Datum: 20.09.2022

Inhibitory Potential of Chemical Constituents from Paeonia suffruticosa Against α-Glucosidase and α-Amylase

Phytochemical study of the root bark of Paeonia suffruticosa plant led to the isolation and characterization of paeoniflorigenone (1), benzoylpaeoniflorin (2), betulinic acid (3), oleanolic acid (4), β-sitosterol (5), and caffeic acid octadecyl ester (6). The enzymatic activities of compounds 1-6 were evaluated by in vitro inhibition assay of α-glucosidase and α-amylase. Compounds 1-6 with IC50 values ranging from 30 to 180 μM inhibited α-glucosidase more efficiently than the standard compound acarbose (IC50 = 1463.0 ± 29.5 μM). Conversely, these compounds (with IC50 values ranging from 40 to 200 μM) were less potent against α-amylase compared to acarbose (IC50 = 16.6 ± 0.9 μM). Kinetic analysis showed that compound 1 was a mixed-type inhibitor, compounds 3 and 4 were noncompetitive inhibitors, while compound 6 was an uncompetitive inhibitor of glucosidase.

Datum: 20.09.2022

Design and Preparation of Iodinated Brucea Javanica Oil as Dual Functional Anti-Tumor Agent for Treating Hepatocellular Carcinoma

Brucea javanica oil (BJO), a traditional herbal medicine extracted from the seeds of Brucea javanica plant, has been used in the treatment of cancer in China. In order to develop high-efficiency embolic agents with additional anti-cancer effects applied in transarterial chemoembolization (TACE), iodinated Brucea javanica oil (IBJO) has been prepared and investigated. IBJO was successfully synthesized by a facile method that gradually injected hydrogen iodide into BJO. In addition, antiproliferative activity of IBJO and BJO were determined by MTT assay on human hepatocellular cancer cell line HepG2 and by flow cytometry analysis. The results demonstrated the activity of BJO without significant effect after iodination. More importantly, the results of embolic simulative model in vitro revealed that IBJO exhibited excellent embolization effect. These phenomena indicate that IBJO can induce embolism in capillaries, which is consistent with the goal of BJO iodination. It is our hope that the results obtained in these studies would support the development of dual functional agent which can be used in TACE treatment of hepatocellular carcinoma.

Datum: 20.09.2022

Quantitative Analysis of Tranexamic Acid Using 2,6-Dichloroquinone-4-Chlorimide as Chromogen: Kinetic Approach

Coupling of 2,6-dichloroquinone-4-chlorimide (DCQ) with tranexamic acid (TA) resulted in a greenish-brown colored complex which absorbed at λmax = 670 nm. It was found that the color intensity of the coupling product changes with time. The present work was aimed at studying the kinetics of this absorbance variation as function of the time at room temperature so as to provide a new colorimetric method for the quantitative determination of TA. To this end, four kinetic methods were conducted and the corresponding calibration curves were constructed. Based on analysis of the correlation coefficients, the fixed time method proved to be the best one (R = 0.996). Nonetheless, the method appeared to suffer from lengthy time and lower sensitivity. Therefore, attempts were made to eliminate these drawbacks. Accordingly, the analysis was conducted using non-kinetically fixed time method with sample heating for three minutes. The obtained limit of detection (LOD) and limit of quantification (LOQ) for the non-kinetic method were found to be 24.01 and 80.04 μg/ml, respectively. The proposed colorimetric method proved to have no significance difference with the official titrimetric method in terms of accuracy and precision.

Datum: 20.09.2022


Category: Current Chemistry Research

Last update: 11.04.2018.

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