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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

Assessment of the Acute Toxicity and Analgesic Activity of Ethyl-6-Amino-4-Aryl-5-Cyano-2,4-Dihydropyrano-2,3- C ]-Pyrazole-3-Carboxylates

The acute toxicity and analgesic activity of compounds of the ethyl-6-amino-4-aryl-5-cyano-2,4-dihydropyrano[2,3-c]pyrazole-3-carboxylate series were investigated. Study compounds were found to be essentially nontoxic and to have analgesic activity.

Datum: 13.04.2019

Design and Antitumor Activity of Platinum Complexes

This review presents the main advances in the design of antitumor platinum complexes over the last five years. Particular attention is paid to unconventional antitumor platinum compounds (complexes in the trans configuration, Pt(IV) complexes with S and P donor ligands, multinuclear complexes).

Datum: 13.04.2019

Synthesis and Antitumor and Antibacterial Activity of Novel Dihydronaphthaline and Dihydrobenzo[ H ]Quinazoline Derivatives

A method for the synthesis of 1-amino-3,3-dimethyl-3,4-dihydronaphthaline-2-carbonitrile (β-aminonitrile) was developed and used to synthesize Schiff bases, thioureide and chloracetamide derivatives. This latter was cyclized to 5,5-dimethyl-2-chloromethyl-5,6-dihydrobenzo[h]quinazoline-4(3H)-one, which was used to synthesize a series of 2-sulfanylmethyl and 2-aminomethyl derivatives. 2-Chloromethylbenzo[h]quinazoline in the presence of a base was found to form condensed heterocyclic compounds with seven rings: 1,1,11,11-tetramethyl-1,2,11,12-tetrahydropyrazino[2,1-b:5,4-b′]di(benzo[h]quinazoline)-10,16(8H,18H)-di one. The antitumor properties of the compounds synthesized here were studied in an ascites carcinoma model and the antibacterial properties were studied using the agar diffusion method.

Datum: 13.04.2019

Synthesis, Characterization and Biological Evaluations of New Imidazo[4,5- a ]Acridines as Potential Antibacterial Agents

The significance of bacterial infections and the early success achieved with some antibiotic drugs have prompted the search for new antibacterial agents. Some new derivatives of 3H-imidazo[4,5-a]acridines are introduced as new powerful antibacterial agents against Gram-positive species. The reaction of N-alkyl-5-nitrobenzimidazoles with arylacetonitriles under basic conditions led to the synthesis of 3H-imidazo[4′,5′:3,4]benzo[c]isoxazoles. Rearrangement of the latter compounds in concentrated sulfuric acid containing nitrous acid gave imidazo[4,5-a]acridones. 3H-imidazo[4,5-a]acridines were obtained by reaction of imidazo[4,5-a]acridones in boiling POCl3. Finally, new compounds were synthesized from the reaction of 3H-imidazo[4,5-a]acridine derivatives with aromatic amines in high yields. All new compounds were fully characterized by elemental analysis, IR, NMR and mass spectroscopy data. Antibacterial activity of the new compounds was tested against a panel of strains of Gram-negative and Gram-positive bacteria species and the corresponding minimum bactericidal concentration (MBC) values were determined. Results of the antimicrobial screening tests showed that new compounds are very effective against Gram-positive bacteria and their MBC values are comparable with those of well-known antibacterial agents such as cephalexin.

Datum: 13.04.2019

Synthesis and Antiarrhythmic Activity of N-[2-(Adamantan-2-YL)Aminocarbonyl-Methyl-N′-(Dialkylamino)Alkylnitrobenzamides

Novel 2-aminoadamantane derivatives, specifically N-[2-(adamant-2-yl)-aminocarbonylmethyl]-N′-(dialkylamino) alkylnitrobenzamides and their physiologically compatible salts, preferably the hydrochlorides, were synthesized and their pharmacological properties were studied. The novel derivatives were found to have marked antiarrhythmic (antifibrillatory) activity in models of calcium chloride and aconitin arrhythmia. The relationship between the chemical structures of the substances synthesized here and their pharmacological activities was studied. The highest level of antiarrhythmic activity and the lowest toxicity were obtained with compound N-[2-(adamant-2-yl)aminocarbonylmethyl]-N′-[3-diethylamino]propyl]-4-nitrobenzamide, which also had the advantage of a wider therapeutic ratio over known antiarrhythmic drugs of classes I, IV, and III (cardiocyclide).

Datum: 13.04.2019

Controversial Points in the Assessment of the Quality of Generic Esomeprazole Formulations

A comparative dissolution kinetics test was performed to model the actions of pathological duodenogastric reflux and therapeutic acid suppression on the stability of esomeprazole formulations from three different manufacturers. After exposure to solutions pH (1.2 ±0.05) or (4.0 ±0.05), formulations were transferred to medium pH (7.0 ±0.05), from which aliquots were collected at 0, 4, 10, 15, 20, 30, 45, and 60 min for estimation of esomeprazole concentrations. The duration of exposure of the medicinal formulation of esomeprazole to pathological duodenogastric refluxate was 4 min. In these test conditions, Generic-1 and Generic-2 were found not to be equivalent to the reference drug (RD); the medicinal formulation of the RD was probably influenced by pathological duodenogastric reflux in the stomach, while Generic-2 was completely degraded in moderately acidic medium pH 4.0, which is evidence of the possible adverse influence of its main antisecretory pharmacodynamic effect of the intragastric stability of the medicinal formulation and the active substance.

Datum: 12.04.2019

Synthesis and Analgesic and Anti-Inflammatory Activities of (3,3-Dipropyl-6,7-Dimethoxy-3,4-Dihydroisoquinolin-1(2 H )-Ylidene)-Acetamide Hydrochlorides

Cyclocondensation of 4-(3,4-dimethoxybenzyl)heptan-4-ol with N-substituted cyanoacetamide was used to synthesize (3,3-dipropyl-6,7-dimethoxy-3,4-dihydroisoquinolin-2(2H)-ylidene)acetamides. The hydrochlorides of the resulting enaminoamides exist in the imino form. All hydrochlorides displayed analgesic effects in the hotplate test at the level of sodium metamizole, and the most active were the amide with the N-substituted 2-(3,4-dimethyoxyphenyl)ethyl radical, which had greater levels of analgesic activity than metamizole and nimesulide. Many of the resulting amides displayed anti-inflammatory effects in a carragheenan model which were comparable in magnitude to those of sodium metamizole.

Datum: 12.04.2019

UHPLC Method Development for Determining Sitagliptin and Dapagliflozin in Lipid-Based Self-Nanoemulsifying Systems as Combined Dose in Commercial Products and its Application to Pharmacokinetic Study of Dapagliflozin in Rats

Anew simple, precise, selective and reproducible reversed-phase ultra-high performance liquid chromatography (RP-UHPLC) method has been developed and validated for the first time in simultaneous determination of two anti-diabetic drugs, sitagliptin (SN) and dapagliflozin (DN), in lipid-based self-nanoemulsifying formulations as a new combined preparation dose. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol–acetonitrile–water mixture at 24/18/58 (%v/v/v) ratio as the mobile phase. The isocratic flow rate was 0.4 mL/min with a run time of 6 min. The UV detection of both SN and DN was performed at 210 nm. The method was validated over a concentration range of 100 – 10000 ng/mL (r2 = 0.9997 and 0.9999 for SN and DN, respectively). The selectivity, specificity, recovery, accuracy and precision for determining SN and DN in lipid-based formulation were validated. The lower limits of detection and quantitation of the method were 27 and 89 ng mL–1 for SN and 19 and 61 ng mL–1 for DN, respectively. The intra- and inter-day coefficients of variation were less than 4%. The validated method has been successfully applied to quantify both SN and DN in self-nanoemulsifying formulation of combined dosage form. In addition, the proposed method was also applied for in vivo pharmacokinetic study using an animal model (rat) to further illustrate the scope and application of the proposed method.

Datum: 12.04.2019

Bismuth Oxide Nanoparticles in Drug Delivery Systems

The paper presents the overlook on bismuth oxide nanoparticles as a potential material applied in medicine-related fields of science. First, the types of drug delivery systems are described. General properties of bismuth oxide are considered as well. The main part of article is devoted to bismuth oxide-based systems intended for drug delivery and medical imaging purposes. It has been confirmed by many scientists that bismuth oxide nanoparticles are a promising material for drug delivery systems and for enhancing the properties of other products in medical applications.

Datum: 12.04.2019

Use of Gas Chromatomass Spectroscopy for Analysis of Salicylate Contents in Plasma from Patients with Cerebrovascular Diseases Taking Aspirin as Antiaggregant Therapy

A chromatomass spectrometric method for assay of salicylic and acetylsalicylic acids in human plasma was developed and metrologically validated. The method measured salicylic and acetylsalicylic acid contents in plasma samples from 26 patients with cerebrovascular diseases (CVD) taking aspirin constantly at doses of 75 – 100 mg/day as antiaggregant therapy for primary or secondary prophylaxis of vascular events. Patients whose samples contained acetylsalicylic acid demonstrated more marked pharmacological responses to antiaggregant therapy.

Datum: 12.04.2019

Synthesis, Characterization and Antimicrobial Activity of Bis (Phthalimido)Piperazine and its Derivatives: a New Class of Bioactive Molecules with Enhanced Safety and Efficacy

Piperazine rings are important heterocyclic targets in organic synthesis and are useful synthetic intermediates or intricate parts of biologically active molecules. In our efforts, a series of piperazine derivatives has been prepared discovering new classes of antimicrobial agents, including bis(phthalimido)piperazine, bis(3-aminopropyl) piperazine, 2,3-dihydro-phthalazine-1,4-dione, and bis(3,4-aminophenol)piperazine. The synthesized antimicrobial agents have been studied using various spectroscopic techniques. Furthermore, these compounds have been screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. Three compounds exhibited mild to good antibacterial activity, but somewhat lower antifungal activity against tested microbial strains.

Datum: 12.04.2019

Physicochemical Properties of the Original Antidepressant GSB-106 and Development of a Method for the Analysis of GSB-106 Substance

Studies at the V. V. Zakusov Science Research Institute of Pharmacology have worked on the basis of the β-pleated structure of loop 4 of brain-derived neurotrophic factor (BDNF) to construct its dimeric peptide mimetic - GSB-106, bis-(N-monosuccinyl-L-serine-L-lysine) hexamethylenediamide. GSB-106 is being developed as an antidepressant with a BDNF-ergic mechanism of action. We report here studies of the physicochemical properties of GSB-106 and development of a method for analysis of GSB-106 substance. The main pharmacopeia quality indicators were determined and IR and NMR spectra were obtained from samples of substance. A method was developed for detecting contaminants in substance using TLC and HPLC.

Datum: 12.04.2019

Synthesis and Pharmacological Properties of 1-(6-Aminohexylamino)-1-Phenylcyclohexyl Dihydrochloride (IEM-2062) as Compared with Memantine

1-(6-Aminohexylamino)-1-phenylcyclohexyl dihydrochloride (IEM-2062) had significantly greater antihypoxic, anticonvulsant, antidepressant, and analgesic activity than memantine and similar antiparkinsonism activity as memantine; it had low toxicity and was safer for use. IEM-2062 produced significant pharmacological effects in the dose range 0.3 – 3 mg/kg.

Datum: 12.04.2019

Preparation of a Horse Chestnut Extract with a 50% Content of Escin and its Actions on Tumor Cell Proliferation and Isolated Mitochondria

Escin-containing horse chestnut extracts and various medicinal formulations are widely used as venotonic agents whose mechanisms of action and intracellular targets remain unknown. Escin is used as an active substance to increase membrane permeability in experiments, and it has more recently been shown to have cytotoxic effects on a number of tumor cell lines. With the aim of increasing the percentage content of active pharmaceutical escin substance in medicinal formulations and studying its mechanism of action, we prepared a horse chestnut extract (HCE) with a 50% escin content. Comparison of the cytotoxic action on HeLa tumor cell cultures showed that at identical concentrations by weight, HCE and reference agent escin had identical cytotoxic effects. At a concentration of 0.003 mg/ml, both substances inhibited HeLa cell viability by more than 80% at 24 h. The cytotoxic effect was not seen when the concentration was reduced four-fold. At equivalent cytotoxic concentrations, the actions of escin in HCE were studied on isolated mitochondria. Both substances were found to increase mitochondrial membrane permeability, to induce mitochondrial swelling, to decrease mitochondrial calcium capacity, and to induce the opening of mitochondrial pores (MPTP). MPTP opening leads to cell death. Escin induced slow and irreversible swelling of mitochondria, while HCE produced rapid and reversible swelling. The MPTP inhibitor cyclosporin completely eliminated the actions of both substances, pointing to the involvement of mitochondria in the pharmacological actions of escin and HCE.

Datum: 12.04.2019

Joint Mechanical Processing of a Drug Substance with Enterosorbent

A selective enterosorbent (ES) based on natural silk fibroin with detoxification properties superior to those of traditional carbon sorbents (SKN-2K, SKN-4M) was proposed. The ES could be used as a matrix for drugs and a platform for new dosage forms to enhance the sanitizing effect of the proposed ES. Inclusion complexes of the ES with benzimidazolyl-2-methylcarbamate hydrochloride (I) were obtained and investigated. H-bonds were shown to form during the reaction of ES with I.

Datum: 01.03.2019

Development of the Optimal Diphilic Emulsion Compositions for Phytoextract Suppositories

Six compositions with various quantities of lipophilic and hydrophilic phases and different emulsifiers were developed. The suppository lipophilic component was type A solid fat; hydrophilic, poly (ethylene glycol) molecules with varying chain lengths and molecular masses. Comprehensive theoretical and experimental results led to formulation of the optimal composition with 35% marigold CO2 extract. The processing parameters for producing such suppositories were optimized.

Datum: 01.03.2019

Validation of a GC-MS Method for Quantitative Determination of Cyclohexanone by Oxidative Cleavage

A GC method for quantitative determination of cyclohexanone by oxidative cleavage was proposed. The research was aimed at the development of a simple, rapid, and effective GC method for quantitative analysis of cyclohexanone in a reaction mixture. Chlorobenzene was used as an internal standard. Qualitative analysis compared mass spectra obtained for each component with mass spectra from the National Institute of Standards and Technology (NIST) database. The method was validated for specificity, linearity, accuracy, robustness, repeatability, and intralaboratory precision.

Datum: 01.03.2019

In Vitro Evaluation of Drug Content in and Drug Release Kinetics from Stents with Different Types of Polymer Coating

Drug elution profiles must be studied in vitro to optimize a polymer-drug formulation during development of drug-eluting stents (DESs). Results from HPLC assays of drug contents and elution kinetics from a biodegradable sirolimus coating and a stable zotarolimus coating on coronary DESs are presented. Drug contents were assessed for crimped stents on the delivery system and expanded stents. The drug coating morphology and elution kinetics were demonstrated to be associated. Significant coating morphological defects were shown to cause deviations in the drug elution profile.

Datum: 01.03.2019

R-Benzylidenehydrazides of NH-Furoyl-5-Iodoanthranilic Acids: Synthesis, Properties, and Analgesic and Antibacterial Activity

A series of R-benzylidenehydrazides of NH-furoyl-5-iodoanthranilic acid were synthesized by condensing NH-furoyl-5-iodoanthranilic acid hydrazide with aromatic aldehydes. Their structures were confirmed using IR and PMR spectroscopy. Their analgesic and antibacterial activities were studied.

Datum: 01.03.2019

Antiarrhythmic Activity of the Flavonoid Fraction of Plantago Major L. Extract

Antiarrhythmic activity of the flavonoid fraction of Plantago major L. extract (0.05 mg/mL) was studied. The studied fractions were found to lower the frequency of rat cardiac papillary muscle contractions with aconitine-induced (1 μM) arrythmia in vitro. An analysis of literature and experimental data suggested that the antiarrhythmic effects of the studied flavonoid fractions may have been related to functional modulation of Na+- and Ca2+-channels in cardiomyocytes.

Datum: 01.03.2019


Category: Current Chemistry Research

Last update: 11.04.2018.

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