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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

Chemical Composition of Menyanthes trifoliata L. Leaves

The trace mineral composition of marsh trefoil at different plant-formation periods was studied by atomic absorption spectrometry. The bioaccumulation of Fe, Cu, and Zn was insignificant during flowering. Also, the contents of physiologically active compounds (iridoids, polyphenols, ascorbic acid) increased slightly during the plant-formation period. The contents of iridoids and ascorbic acid were higher in marsh trefoil samples growing in an environmentally pristine area. The high contents of polyphenolic compounds in the samples were likely due to the presence of biophilic elements such as Cu, Zn, Mn, and Fe.

Datum: 15.06.2021

Experimental Study of Local Anesthetic Activity and Acute Toxicity of a Combined Gel

Results from studies of the local anesthetic activity of a gel for surface anesthesia that was developed at A. S. Sadykov Institute of Bioorganic Chemistry of the Academy of Sciences of the Republic of Uzbekistan are presented. DF Skincaine gel (Korea) and 5% lidocaine solution were used as reference drugs. A model of terminal anesthesia of rabbit-eye cornea showed that the test gel had a local anesthetic effect with a Rainier index of 950; DF Skincaine gel, 680; 5% lidocaine solution, 480. The new gel had a longer anesthetic effect than DF Skincaine (75 ± 6.4 and 45 ± 3.8 mins or 66.7% longer) and shorter latent period (4 and 6 min or 37% less). The studies showed that instillation into the conjunctival sac of the anesthetic gel did not cause adverse local reactions. Conversely, use of 5% lidocaine solution as an anesthetic agent led to the appearance of signs of local irritation as hyperemia of the conjunctivae and edge of the eyelids. Results of acute toxicity tests after subcutaneous injection to mice showed that the anesthetic gel was seven times less toxic than 5% lidocaine solution. The LD50 values of the compounds were lidocaine 274.6 ± 7.4 mg/kg; DF Skincaine, ≥2000; and the new anesthetic gel, ≥2500.

Datum: 15.06.2021

Experimental Assessment of Additional Hormonal Activity of the Pregnane-Steroid Gestagen Gestobutanoyl

The ability of gestobutanoyl, a pregnane steroid with progestogenic activity, to exhibit additional glucocorticoid, mineralocorticoid, antiandrogenic, and estrogenic effects in rats has been studied. It was found that gestobutanoyl did not have estrogenic activity because it did not increase the weight of the uterus with prolonged (30 d) administration at a therapeutic dose of 0.25 mg/kg and doses 10 and 100 times higher. Gestobutanoyl at a dose of 2.5 mg/kg for 30 d did not show glucocorticoid activity because the thymus mass did not change. However, the thymus mass decreased by 25% (p ≤ 0.05) when gestobutanoyl was administered at a dose 100 times higher (25 mg/kg) than the therapeutic dose. Gestobutanoyl at a dose of 2.5 mg/kg reduced the expression of androgen receptor (AR) mRNA in the rat uterus by 3 times and, as previously shown, did not increase the weight of the prostate and levator ani muscle. The mineralocorticoid activity of gestobutanoyl tablets was studied using peroral administration for 14 d to female rats at doses 100 and 1000 times (2.5 and 25 mg/kg, respectively) the therapeutic dose. Diuresis did not decrease, water was not retained in the rat body, and electrolytes were excreted in the urine and were present in the urine at constant concentrations in all experimental groups, indicating the absence of side mineralocorticoid effects of gestobutanoyl tablets.

Datum: 15.06.2021

Application of the SeDeM Method for Optimization of Tablet Formulations (A Review)

A new method of mathematical modeling called Sediment Delivery Model (SeDeM) is reviewed. This method is a convenient tool for determining the suitability of powdered material for direct compression. The method identifies unsatisfactory properties of the material and also determines the type and amount of excipients that should be added to the tablet formulation to neutralize the unsatisfactory properties of the active pharmaceutical ingredient (API). The principles of application of the SeDeM method are considered. The parameters to be determined for application of this method, the equations for calculations, and the constructed diagrams are presented. The methods for application of SeDeM to the pharmaceutical industry and the advantages of such use of the system are described. The SeDeM method is used to optimize and calculate the composition of tablets obtained by direct compression. This system takes into account all the characteristics of the bulk material and provides recommendations for the selection of excipients. The method makes it easier to develop a new drug and simplifies the manufacturing process by eliminating unnecessary excipients. In addition, the method is used for quality control of single APIs and excipients.

Datum: 15.06.2021

Estrogen-Like Substances from the Aerial Part of Ferula tschimganica

The optimal parameters influencing the extraction of the sum of terpenoid alcohol esters from the aerial part of Ferula tschimganica and purification of the obtained extract were found and made it possible to produce a final substance without green coloration. The technology for producing the sum of terpenoid alcohol esters from the aerial part of F. tschimganica was developed. Aspectrophotometric method for quantitative determination of the sum of terpenoid alcohol esters in chimphestrol substance (working name of the created agent) was proposed. Pharmacological studies found that terpenoid alcohol esters from the aerial part of F. tschimganica at a dose of 1 mg/kg exhibited a pronounced estrogenic effect in experiments on both immature and ovariectomized rats that was comparable to that of tefestrol and slightly inferior to that of the synthetic estrogenic drug Synestrol.

Datum: 15.06.2021

Effect of Solvents on Extraction of Bioactive Substances from CITRULLUS COLOCYNTHIS and Their Antioxidant, Antimicrobial and Antiglycation Activities

Citrullus colocynthis has been used for treating ailments since ages. The ability of plant extracts obtained using various solvents to exhibit pharmacological effects was evaluated. To check for the antioxidant potential of whole plant and fruits of C. colocynthis, conventional antioxidant assays such as DPPH radical scavenging capacity were carried out, total content of flavonoids and phenolics was determined, and reducing power was estimated. The antimicrobial activity was evaluated using 96-well plate technique and Alamar Blue assay and the potential of plant extracts as antioxidant agents was evaluated using oxidative burst assay with chemiluminescent indicators. The highest phenolic content was obtained using 50% ethyl acetate, while highest total flavonoid content was provided by extraction with methanol. Aqueous extracts showed highest DPPH radical scavenging activity, while methanolic extracts showed maximum reducing power potential at different concentrations. Whole plant extracts of C. colocynthis showed higher antioxidant potential than fruit extracts only. For both in-vitro and in-vivo anti-inflammatory activity, the maximum inhibition of reactive oxygen species (ROS) was produced by 50% methanol whole plant extract. Among the five test bacterial strains used, namely Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi, the antibacterial activity of extracts showed more pronounced growth inhibition of S. aureus and minimum effect upon E. coli. All extracts tested rendered zero potential as antiglycation agents.

Datum: 15.06.2021

Synthesis and Anti-Proliferative Activity of New α-Amino Phosphonate Derivatives Bearing Heterocyclic Moiety

Condensation of 4-chloroacetophenone 1 with phenyl hydrazine 2 afforded hydrazone 3. Further reaction of 3 with Vilsmeier reagent yielded the pyrazolaldehyde 4 in excellent yield. A one-pot, three-component reaction between aldehyde 4, triphenylphosphite 5, and appropriate amines in the presence of lithium perchlorate as Lewis acid catalyst gave the corresponding α-amino phosphonates 7-12(a-d) in good yields. The chemical structures of all new compounds were established by IR, 1H NMR, and mass spectroscopy analysis. The anti-proliferative activity of the synthesized compounds against HCT-116, HepG2 and MCF-7 human cancer cells using the MTT assay was evaluated, and revealed higher anticancer activity when compared with reference drug doxorubicin. Among the tested compounds, pyrazole derivatives 4 and 9 exhibited the highest anticancer activity against breast (MCF-7), and colon (HCT-116) cancer cell lines with IC50 = 2.7 and 3.3 μM, respectively.

Datum: 15.06.2021

The Ameliorative Effect of Monomethyl Fumarate and Silymarin Against Valproic Acid Induced Hepatotoxicity in Rats

Valproic acid (VPA) is a widely-used antiepileptic drug that has been extensively reported to cause hepatotoxicity. Monomethyl fumarate (MMF) is a compound that has been reported to produce hepatoprotective and antioxidant effects. This study was aimed at studying the alleviative effects of MMF on VPA-induced hepatotoxicity in rats. The test animals were divided into nine groups, each of six rats, as different cases and one group as control. VPA was intraperitoneally administered (500 mg/kg) once daily for 7 days. The VPA-exposed rats were then treated with two doses (25 and 50 mg/kg) of MMF and silymarin. Biochemical parameters and oxidative stress markers as well as histopathological examination were employed to evaluate the effect of these compounds on VPAhepatotoxicity. VPAadministration caused hepatotoxicity in rats as evidenced by significant increase in the levels of aminotransferase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), liver malondialdehyde (MDA), and significant reduction in glutathione (GSH) content compared to values in the control group. The administration of MMF or silymarin attenuated VPA-induced oxidative hepatotoxicity as evidenced by significant decrease in serum liver function tests together with marked improvement in oxidative stress markers. Thus, the treatment with MMF and/or silymarin improved histopathological patterns of liver tissue to a considerable degree. MMF treatment can exert protective effects (similar to those of silymarin) against VPA-induced hepatotoxicity. This amelioration can result from a considerable reduction of the oxidative stress. Moreover, a combination therapy was more effective than MMF or silymarin monotherapy alone. A dose of 25 mg/kg was as effective as 50 mg/kg for either MMF or silymarin.

Datum: 15.06.2021

Phytochemical Analysis of Polyphenol Secondary Metabolites in Cloudberry (Rubus Chamaemorus L.) Leaves

Phytochemical analysis of cloudberry leaves isolated one new (1) and four well-known compounds (2-5) and established their structures. Compounds 1 (4-O-α-L-arabinofuranosylellagic acid) and 2 [(–)-epicatechin] belonged to the tannin class. The rest of the isolated compounds were the flavonoid glucuronic glycosides quercetin 3-O-β-D-glucuronide (3), quercetin 3-O-β-D-2′′-galloylglucuronide (4), and kaempferol 3-O-β-D-glucuronide (5). Compounds 4 and 5 were isolated from Rubus chamaemorus L. for the first time. Predictions of the biological activity spectra for isolated 1-5 using the PASS program provided insights regarding the most promising directions for studying their biological activity.

Datum: 15.06.2021

New Potential Monotherapeutic Candidates for Helicobacter pylori: Some Pyridinazo Compounds Having Both Urease Enzyme Inhibition and Anti-Helicobacter pylori Effectiveness

To contribute to the monotherapeutic approach to Helicobacter pylori, some new pyridinazo compounds containing natural phenols such as eugenol and guaiacol were synthesized and their antioxidant capacities, urease enzyme inhibition and anti-Helicobacter pylori effect were investigated. This monotherapeutic approach suggests that a single synthetic drug with both a strong urease enzyme inhibitor and effective antibiotic properties can be used to treat Helicobacter pylori infection As expected, all newly obtained pyridinazo compounds have been found to have both urease enzyme inhibitor properties and anti-Helicobacter pylori activity.

Datum: 14.06.2021

Molecular Weight Characteristics and Anticoagulant Activity of Low-Molecular-Weight Heparin Obtained By Nitrous Acid Depolymerization

Low-molecular-weight heparin was synthesized by depolymerization of high-molecular-weight heparin with nitrous acid. Preparative chromatography was used to isolate low-molecular-weight heparins with narrow molecular-weight distributions, as confirmed by size-exclusion HPLC. The average molecular weight of the products according to capillary viscometry decreased with synthesis time (4 h) from 14.0 to 3.4 kDa. Fractions with molecular-weight characteristics, ratios of sulfo- to carboxyl groups, and specific activities corresponding to those of low-molecular-weight heparin isolated from commercially available Fragmin® were isolated among the products. Low-molecular-weight heparins with characteristics analogous to those of Dalteparin and Nadroparin substances could be obtained depending on the treatment time of high-molecular- weight heparin with nitrous acid in acidic medium.

Datum: 14.06.2021

Cytotoxic Activity of Perfluoroalkyl-Substituted Imidazoindazoles and Imidazobenzisoxazoles

The cytotoxic activity of perfluoroalkyl imidazoindazoles and imidazobenzisoxazoles with respect to MCF-7 (human breast carcinoma) and HepG2 cell lines (human hepatocellular carcinoma) was studied. The imidazoindazoles exhibited significant cytotoxicity against MCF-7 and HepG2 cell lines. 2,6-bis(4-Fluorophenyl)-4,4-dimethyl-8-trifluoromethyl-3,4,5,6-tetrahydroimidazo[4,5-e]indazole displayed the most pronounced cytotoxic action. Regioisomeric imidazobenzisoxazoles inhibited extensively growth of HepG2 cells. The mechanism of cytotoxic action can be related to the induction of apoptosis as a result of disruption of the cell cycle, in particular, arrest of HepG2 cells in the G2 phase and MCF-7 cells in the G1 phase.

Datum: 14.06.2021

Development of a Quantitative Determination Method for a Benzimidazole Derivative with Laboratory Code RU-31 and Antimigraine Activity in Biological Samples

A quantitative determination method for drug substance RU-31, a derivative of a methoxyphenylimidazo - [1,2-α]benzimidazole possessing antimigraine activity, in biological samples was developed. This method has selectivity and high sensitivity sufficient to allow its use for pharmacokinetic studies of RU-31. The sensitivity of the method (detection limit) for RU-31 is 100 ng/mL; limit of quantitation, 500 ng/mL. The average measurement error is ≤15%.

Datum: 14.06.2021

Synthesis of Glycyrrhizic Acid Conjugates with S-Benzyl-L-Cysteine and Their Antiviral Activity

A new method for the synthesis of glycyrrhizic acid (GA) conjugates with S-benzyl-L-cysteine using 1-ethyl-3-(3-dimethylaminoproopyl)carbodiimide is proposed. It is established that 3-O-{2-O-[N-(β-D-glucopyranosyluronyl)-L-cysteine-S-benzyl]-N-(β-D-glucopyranosyluronyl)-L-cysteine-S-benzyl}-(3β,20β)-11-oxo-30-(N-carbonyl-L-cysteine-S-benzyl)-30-norolean-12-ene is superior to GA in inhibiting the accumulation of HIV-I virus-specific protein p24 (viral antigen) in MT-4 cell culture (IC50 3 μg/mL, SI 90) and is 50 – 55 times less toxic to cells than azidothymidine.

Datum: 14.06.2021

Analgesic Activity and Acute Toxicity of Dihydrotetrazolo[1,5-a]Pyrimidine Derivatives

Aseries of dihydrotetrazolo[1,5-a]pyrimidine derivatives were synthesized via a three-component reaction of benzoylacetone with aromatic aldehydes and 5-aminotetrazole monohydrate. The obtained compounds were tested for analgesic activity using the acetic acid-induced writhing test. Their acute toxicities were determined. (7-Aryl-5-methyl-4,7-dihydrotetrazolo[1,5-a]pyrimidin-6-yl)(phenyl)methanones were found to exhibit analgesic activity comparable to that of the reference drug metamizole sodium and were low-toxicity compounds. The obtained results were indicative of good prospects for further investigation of analgesic properties in this series of compounds.

Datum: 14.06.2021

Solid-Phase Fluorimetric Determination of Tetracyclines in Medicinal Preparations on Cellulose Paper and in Thin-Layer Silica Gel Using a Smartphone

The possibility of determining the active substances of antibacterial drugs of the tetracycline series (tetracycline, doxycycline, oxytetracycline, demeclocycline, metacycline, and chlortetracycline) using solid-phase fluorescence digital colorimetry is considered. The intrinsic fluorescence of tetracyclines and tetracycline-sensitized fluorescence of europium on cellulose paper and a thin layer of silica gel was studied. Yellow-green (tetracyclines) and pink (europium) fluorescence were observed upon irradiation with UV light (365 nm) of spots of tetracycline solutions applied to the matrix. The fluorescence intensity on the matrix surface was measured using a smartphone. Values of colorimetric parameters in the RGB system were used as the analytical signals (Ar). The limits of detection and quantitation were 1 – 5 and 3 – 17 μg/mL, respectively, for all analytes. The ranges of the determined concentrations were 3 – 500 μg/mL. The technique was tested for medicinal products. The relative standard deviation of the analytical results was ≤0.06.

Datum: 14.06.2021

Use of Surfactants in Quality Control of Solid Dosage Forms with Respect to Microbiological Indicators

The present study focuses on the use of surfactants (SA) in quality control of solid dosage forms. Features of the dissolution of solid dosage forms and factors affecting the extraction of microorganisms from drug samples are discussed. The properties of SA required to neutralize the antimicrobial activity of drugs are considered. Experimental data on the extraction of microorganisms from and the neutralization of antimicrobial action of solid dosage forms of non-sterile drugs are presented.

Datum: 14.06.2021

Synthesis of Chalcone Derivative from Clove Leaf Waste as a Natural Antioxidant

The synthesis of chalcone derivatives from clove leaf waste and their potential application as natural antioxidants have been studied. Synthesis of chalcone derivatives takes six steps: (1) distillation of clove leaf oil waste, (2) isolation of eugenol from clove leaf oil, (3) isomerization reaction of eugenol to produce isoeugenol, (4) oxidation reaction of isoeugenol to produce vanillin, (5) O-allylation reaction of vanillin to produce 4-allyloxy-3-methoxy benzaldehyde, and (6) Claisen-Schmidt condensation reaction of compound 5 with acetophenone to yield 3-(4-allyloxy-3-methoxyphenyl)-1-phenyl prop-2-en-1-one as chalcone derivative of target molecule in 97.28% yield. The antioxidant activity was evaluated in oleic acid oxidation reaction in comparison to butylated hydroxytoluene (BHT) as a standard by using ferric thiocyanate (FTC) and thiobarbituric acid (TBA) methods. The test showed that the order of antioxidant activity was as follows : BHT > 3-(4-allyloxy-3-methoxyphenyl)-1-phenyl prop-2-en-1-one > vanillin > 4-allyloxy-3-methoxy benzaldehyde.

Datum: 14.06.2021

Antibacterial and Acetylcholinesterase Inhibitory Potentials of Triazenes Containg Sulfonamide Moiety

The aim of this study was to investigate the antibacterial and acetylcholinesterase (AChE) inhibitory activities of 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl)benzenesulfonamides (compounds 1 – 12) and to find out new possible drug candidate molecules since the available agents in clinical use have some limitations. According to the results of antibacterial screening for compounds 1 – 12, most of the synthesized compounds were found to be effective against Gram-positive microorganisms while being ineffective (MIC > 1600 μg/mL) on Gram-negative microorganisms. According to the AChE inhibition results, Ki values of compounds 1 – 12 were in the range of 5 ± 1 – 34 ± 2 nMtoward AChE. Tacrine (TAC) used as a reference drug had Ki value of 4 ± 1 nM toward AChE. The non-substituted derivative compound 1 coluld be considered as a lead compound for this study in terms of AChE inhibitory activity, since its Ki value (5 ± 1 nM) was close to that of the reference drug (TAC). Thus, compound 1 was docked at the binding site of AChE and showed good interaction with the target enzyme, suggesting their possible mechanism of action.

Datum: 14.06.2021

Correction to: Standardization and Wound-Healing Activity of Petroleum, Ethanolic and Aqueous Extracts of Ficus Benghalensis Leaves

To the article “Standardization and Wound-Healing Activity of Petroleum, Ethanolic and Aqueous Extracts of Ficus Benghalensis Leaves,” by Mohd Imran, Jyoti Nanda Sharma, Mehnaz Kamal, and Mohammad Asif, Vol. 54, No. 10, pp. 1057 – 1062, January, 2021

Datum: 01.05.2021


Category: Current Chemistry Research

Last update: 11.04.2018.

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