Pharmaceutical Chemistry Journal
Pharmaceutical Chemistry Journal, a peer-reviewed journal, is dedicated to scientific and technical research on the creation and manufacturing improvement of medicines and intermediates.
- Presents the full spectrum of new drug research, including synthesis methods, rational drug design and pharmacological, toxicological, modelling, docking and biochemical studies.
- Describes the properties and applications of new medicinal products, drug delivery, targeting, and multifunctional nanosystems.
- Discusses proteomics metabolonomics, and pharmacogenomics of new pharmaceutical agents, along with nanobiotechnology of SiRNA, microRNAs, antibodies, and nanoparticles.
- Applies new physicochemical methods to identification, quantitative determination, uncover molecular details of condensed media and control of solid particle surface chemistry.
- Reviews international literature to report on recent developments in the field.
Current Issue
Vol 52, No 12 (2019)
- Year: 2019
- Articles: 12
- URL: https://journals.rcsi.science/0091-150X/issue/view/15294
Search for New Drugs
R-Benzylidenehydrazides of NH-Furoyl-5-Iodoanthranilic Acids: Synthesis, Properties, and Analgesic and Antibacterial Activity
Abstract
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.
Article
Synthesis and Antimicrobial Activity of 3-Phenyl-1-Methylquinolin-2-One Derivatives
Abstract
A series of quaternary salts were obtained by reacting 3-(4-bromoacetylphenyl)-1-methylquinolin-2(1H)-one with Py, 4-methylpyridine, quinoline, benzo[f]quinoline, and triphenylphosphine. Derivatives of thiazole, imidazo[1,2-a]pyridine, and imidazo[1,2-a]pyrimidine were produced using dinucleophilic reagents. Several of the synthesized compounds possessed high antimicrobial activity, indicating that further research on this series of compounds was promising.
Computer Regression Models for P-Glycoprotein Transport of Drugs
Abstract
Regression models of the cellular substrate specificity of 177 drugs for P-glycoprotein were built using linear regression, random forest, and support vector methods. QSAR modeling used a full-trial search of all possible combinations of the seven most significant molecular descriptors with clear physicochemical interpretations. The statistics of the obtained models were satisfactory according to an internal cross-validation and external validation tests using 44 new compounds. H-bond descriptors were components of almost all most significant QSAR models. This confirmed that H-bonds played an important role in penetration of the compounds through the blood–brain barrier. The developed statistical models could be used to assess P-glycoprotein transport of investigational new drugs.
Microcolumn HPLC-UV Analysis of Glycyrrhiza Uralensis and Licorice Preparations
Abstract
A microcolumn HPLC method with UV detection (MC-HPLC-UV) using ProntoSIL-120-5-C18 sorbent (1 × 60 mm, 1 μm) and gradient elution by LiClO4(4.1 M)/HClO4(0.1 M)–MeCN was developed for quantitative analysis of seven compounds (liquiritin-2″-O-glucoside, liquiritin, isoliquiritin-2″-O-apioside, isoliquiritin, licorice-saponin G2, yunganoside E2, glycyrrhizic acid) in Glycyrrhiza uralensis Fisch. roots. Validation of the procedure showed that the metrological parameters were satisfactory. The procedure was used for research on G. uralensis roots growing in Siberia and quantitative analysis of glycyrrhizic acid in 28 commercial licorice preparations.
Antiarrhythmic Activity of the Flavonoid Fraction of Plantago Major L. Extract
Abstract
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.
Dissolution of Ketoprofen from Poly(Ethylene Glycol) Solid Dispersions
Abstract
The effect of solid dispersions (SDs) on the solubility of the nonsteroidal anti-inflammatory drug ketoprofen was determined. Ketoprofen and its SDs with poly(ethylene glycol) PEG-400, -1000, -1500, -2000, and -3000 were studied. Dissolution of ketoprofen from the SDs increased by 1.2 – 1.8 times; the dissolution rate, by 1.7 – 2.4 times. The improved release of ketoprofen from the SDs was proposed to be due to several factors such as solubilization and amorphization of the compound and formation of intermolecular H-bonds. The results could be used to develop rapidly dissolving ketoprofen solid dosage forms.
Joint Mechanical Processing of a Drug Substance with Enterosorbent
Abstract
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.
In Vitro Evaluation of Drug Content in and Drug Release Kinetics from Stents with Different Types of Polymer Coating
Abstract
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.
Validation of a GC-MS Method for Quantitative Determination of Cyclohexanone by Oxidative Cleavage
Abstract
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.
Medicinal Plants
Angionorm Complex Herbal Preparation Constituents Identified by High Performance Liquid Chromatography-Mass Spectrometry
Abstract
Angionorm is an original Russian preparation based on the dried aqueous EtOH (25%) extract of a herbal mixture containing horse chestnuts (Aesculus hippocastanum L.), licorice roots (Glycyrrhiza glabra L.), hawthorn fruit (Crataegus), and dog-rose hips (Rosa canina). Areversed-phase HPLC-MS-MS procedure with gradient elution was developed to identify the main constituents in extracts of the mixture and each raw material type. Standards helped to identify 15 compounds of various classes (phenolic and hydroxycinnamic acids and their esters, flavonoids, flavonoid glycosides, triterpene saponins). Peaks of hyperoside, liquiritin, â-glycyrrhizic acid, and escin isomers were identified using MRM transitions, elution order, and literature data. Herbal sources of identified constituents were determined. Marker compounds characteristic of each raw-material type in the mixture extract were proposed.
Drug Synthesis Methods and Manufacturing Technology
Development of the Optimal Diphilic Emulsion Compositions for Phytoextract Suppositories
Abstract
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.
Structure of Chemical Compounds, Methods of Analysis and Process Control
HPLC-MS Method for Simultaneous Quantitative Determination of an Innovative Russian Gestagen and its Metabolites in Rat and Rabbit Blood Sera
Abstract
An HPLC-MS method for simultaneous quantitative determination of a novel gestagenic pharmaceutical and two of its metabolites in rat and rabbit blood sera was developed and validated. The method was selective and specific. The detection limit for all analytes was 5 ng/mL; lower limit of quantitation, 10 ng/mL. Calibration curves for all analytes had the form y = ax + b. The correlation coefficients were >0.99. Matrix effects, degree of extraction, and stability of analytes in standard solutions, analytical samples, and the biomatrix with multiple freeze—thaw cycles were studied.