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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

Syntheses of Melanotan II and YSL Amide by Ajiphase ® Methodology

The promising antitumor peptides Melanotan II and YSL amide were synthesized for the first time in gram quantities in overall yields of 72 and 50%, respectively, by Ajiphase® methodology. This method was shown to be promising for peptide manufacturing. The proposed methods are as convenient as polymer-phase syntheses with the reagent consumption and associated analytical simplicity of classical solution syntheses.

Datum: 01.08.2019

Influence of Filipendula ulmaria (L.) Maxim. Extract on Lewis Lung Carcinoma Development and Cytostatic Therapy Effectiveness in Mice

Meadowsweet extract was prepared by heating the aerial part of Filipendula ulmaria (L.) Maxim. in EtOH (70%). Experiments in C57BL/6 mice with Lewis lung carcinoma (LLC) showed that the extract at doses of 50 and 100 mg/kg exhibited dose-dependent antimetastatic action. Combined treatment of animals with LLC using cyclophosphamide and meadowsweet extract at doses of 50 and 100 mg/kg increased the antitumor effect of the cytostatic drug.

Datum: 01.08.2019

Evaluation of the Cytotoxic Effect of Hydroxypyridinone Derivatives on HCT116 and SW480 Colon Cancer Cell Lines

According to the literature, iron chelators have been used to inhibit tumor cell proliferation. Hydroxypyridinones, due to easy derivatization and high affinity for iron, have been suggested as an attractive target for the development of iron scavenging ligands. N-arylhydroxypyridinone derivatives as iron chelators have been previously designed and synthesized, and the present study is performed in order to evaluate the antitumor efficacy of these compounds,. Four derivatives of hydroxypyridinone were tested against HCT116 and SW480 colon cancer cell lines for 48 h using MTT assay. One compound (3-hydroxy-2-methyl-1-phenylpyridin-4(1H)-one, PMPO) showed the maximum cytotoxic activity on both HCT116 and SW480 cancer cells with IC50 = 243 and 180 μmol, respectively, for 48 h treatment. The obtained results demonstrated that various concentrations of test compounds exhibited significant reduction of the cell viability (P < 0.05) in a concentration dependent manner. Our findings indicate that the proposed hydroxypyridinone derivatives can be considered as a new option for the treatment of colon cancer.

Datum: 01.08.2019

Application of Near-IR Spectroscopy to Analysis of Kemantane Drug Substance

Near-IR spectroscopy is a promising analytical method in pharmacy. It was shown that it can be used as a rapid method for confirming the identity and analyzing the purity of kemantane (5-hydroxyadamantan-2-one) drug substance.

Datum: 01.08.2019

Synthesis and Antioxidant and Anti-Influenza Activity of Aminomethanesulfonic Acids

Aminomethanesulfonic acid (I) and its N-methyl- (II), N-(2-hydroxy)ethyl- (III), N-(tert-butyl)- (IV), N-benzyl- (V), and 4-(N-phenylaminomethyl)phenyl- (VI) derivatives (V and VI not previously reported) were synthesized and characterized by elemental analysis and IR and mass spectroscopy. The in vitro antioxidant activities of aminomethanesulfonic acids I-VI were found to be comparatively weak. Compounds IV and V suppressed statistically significantly reproduction of influenza virus strains A/Hong Kong/1/68 (H3N2) and A/PR/8/34 (H1N1) in chorioallantoic membrane tissue culture.

Datum: 01.08.2019

In Vitro Effect of Flow Velocity on Aerodynamic Parameters of a Cromospir Metered Dose Inhaler

The effect of changing flow velocity on the aerodynamic particle size distribution of Cromospir metered dose inhaler (MDI) was studied using an Andersen cascade impactor (ACI) in the standard configuration designed for sampling at flow velocity 28.3 L/min and in a modified configuration at 60 L/min. The aerodynamic particle size distribution and the respirable fraction of the aerosol changed if the flow velocity of air passing through the impactor changed. Studies of the aerodynamic properties of aerosols with patient inhalation modeled at various air flow rates are recommended during quality assessment method development for aerosols and for in vitro comparisons of MDI efficiencies.

Datum: 01.08.2019

Comparative Evaluation of Antiparkinsonian, Anti-Inflammatory, and Analgesic Effects of Hemantane and Two 2-Aminoadamantane Derivatives Differing From it by a Bridgehead Hydroxyl

2-Adamantylaminopropanol hydrochloride (ADK-971) and 5-hydroxyadamantan-2-ylaminopropanol hydrochloride (ADK-1013) were less active than hemantane in parkinsonian syndrome murine models. ADK-971 and AKD-1013, like hemantane at a dose of 20 mg/kg, exhibited comparable antiexudative effects in the mouse acetic peritonitis model. However, ADK-971 and ADK-1013 (20 mg/kg), in contrast to hemantane at the same dose, did not possess analgesic effects against visceral and thermal somatic pain in mice.

Datum: 01.08.2019

Metal-Based Molecular Compounds: Structure, Analytical Properties, dsDNA Binding Studies and In Vitro Antiproliferative Activity on Selected Cancer Cell Lines

In this work, to contribute to research in the area of new chemotherapeutic agents, we attempted at obtaining new metal-based compounds as alternatives to the existing metal-based anticancer drugs. In this context, Cu(II), Zn(II) and Pt(II) metal-based complexes of pharmaceutically active compound, effective antineoplastic methotrexate (MTX), were synthesized, and their structures were elucidated by analytical (melting point, elemental analysis, conductivity, and solubility), spectroscopic (UV-Vis, IR, 1H NMR, LC-MS and ICP-OES) and thermal (TGA, DTA) methods. UV-Vis spectroscopy examined interactions of MTX pharmaceutically active substances and their metal-based compounds with the fish sperm double-stranded DNA (FS-dsDNA). Regarding the data obtained from spectroscopic measurements, it is understood that all compounds interact with FS-dsDNA. The antiproliferative activity of the active agent MTX and the newly synthesized metal-based compounds was investigated on C6 and He-La cells in comparison to the active anticancer agents present in the market using real-time cell analyzer with four different concentrations. Also, interactions of all compounds obtained with the double-stranded FS-dsDNA were studied using pencil graphite electrode (PGE) by monitoring changes in the signal of the guanine base. The associated surface morphology was examined by differential pulse voltammetry (DPV) and scanning electron microscopy (SEM) techniques.

Datum: 01.08.2019

Modeling the Desorption Stage in Lyophilization Technology of bis ( N -Monosuccinyl-L-Glutamyl-L-Lysine) Hexamethylenediamide (GK-2)

Modeling lyophilization is the most convenient approach to optimizing the drying stage because it allows the optimal temperature regime for secondary drying to be selected using a small number of experiments and the duration of the process to be calculated as a function of the conditions. A simple mixed mathematical model of the process was used because of the ability to extrapolate the data and the small number of required experiments. The dependences of the drying rate on thermal variables at a constant total pressure and of the possibility of a dynamic temperature rise on residual moisture content were calculated. The optimal secondary drying regime was determined by comparing the performance of various regimes, verifying the reproducibility of the model, and comparing theoretical and experimental values of residual moisture. The most suitable drying regime for bis(N-monosuccinyl-L-glutamyl-L-lysine) hexamethylenediamide (GK-2) lyophilizates for injection was selected.

Datum: 01.08.2019

Correction Factors in Formulas for Calculating Impurity Contents: Essence and Determination Methods and Their Limitations

Formulas for calculating relative response factors (RRFs) and correction factors (Fs) of impurities and those necessary for understanding the essence of RRFs and Fs are presented. The main methods for determining Fs and their limitations (conditions necessary for correct determination of RRFs and Fs) are considered. These limitations do not appear in the European and US pharmacopoeias although they must be considered to determine the correct Fs. Examples and recommendations are given for reliable determination and correct use of the Fs.

Datum: 01.08.2019

Synthesis, Antiproliferative Activity, and Effect on Carcinoma A549 Cell Microtubules of New Tubuloclustin Analogs

Combretastatin analogs of the antitumor agent tubuloclustin {N-[7-(adamant-2-yloxy)-7-oxoheptanoyl]-Ndeacetylcolchicine} were prepared via esterification of combretastatin by monoesters of pimelic or adipic acid with adamantan-2-ol or (adamantan-1-yl)methanol. These conjugates were stable and cytotoxic to human lung carcinoma A549 cells (EC50 ≈ 50 – 70 nM) and caused depolymerization of microtubules and slight clustering of tubulin. Tubuloclustin analogs with shortened linkers were prepared via amidation by N-deacetylcolchicine of monoesters of adipic or succinic acids with adamantan-1-ol or (adamantan-1-yl)methanol. The conjugate N-[6-(adamantyl)-6-oxohexanoyl]-N-deacetylcolchicine was more active (EC50 ≈ 4 nM) than tubuloclustin and promoted strong tubulin clusterization. All compounds induced apoptosis of A549 cells. Tests in vivo of N-[6-(adamantyl)-6-oxoheaxnoyl]-N-deacetylcolchicine on carcinoma A549 experimental models were concluded to be promising.

Datum: 01.08.2019

Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: Emerging Lipid Based Drug Delivery Systems

In the past decade, research in the area of nanodrug delivery has reached a new height with the advent of lipid based nanodrug delivery systems. Lipids being biocompatible and possessing diverse physicochemical properties have tremendous potential to enhance oral bioavailability of water insoluble drugs. Incorporation of a drug in lipid carriers is a smart approach to overcome problems related with conventional oral therapy. In recent years, two lipid based nanoparticles, namely solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are widely explored. SLN are spherical nanoparticles with a drug-containing solid lipid core stabilized with surfactants and formulated mainly to improve bioavailability of the drug molecules. Despite several advantages of SLNs, their major drawbacks include limited drug loading, drug leakage, and crystallization during storage. These drawbacks were avoided or reduced by the development of a new generation of lipid nanoparticles, the NLC, wherein a solid lipid is blended with liquid lipid. Modulation of drug release was added advantage with NLC formulations. The present review focuses on production techniques, characterization, release characteristics, stability, toxicity and potential applications of SLNs and NLCs.

Datum: 01.08.2019

Calculations of Geometric Parameters and Physicochemical Properties of Complexes Formed of FE(II)-Reactive 1,2,4-Trioxolane Ring and Some Anti-Malaria Drugs Via Traceless Linker

There is a method to employ aberrant levels of mobile ferrous iron (Fe(II)) for selective drug delivery in vivo. This approach makes use of a 1,2,4-trioxolane moiety, which serves as an Fe(II)- sensitive “trigger,” making drug release contingent on Fe(II)-promoted trioxolane fragmentation. In this study we focused on the prototype drug conjugate of 1,2,4-trioxolane ring joined via a traceless linker to drug species, which is conjugated to the linker via a free amine or alcohol function to form a complex.We studied four complexes formed of different drugs with various linkers. The structure and physicochemical properties of complexes were studied using the Hartree – Fock method with 6-311++G** basis set. The influence of the oxalan ring and various drugs on the properties of complexes has been studied. Geometric parameter, energies, nuclear chemical shielding constants, direction of dipole moment vector, partition coefficients, electric polarizabilities, and other physicochemical properties of these compounds have been calculated.

Datum: 01.08.2019

Influence of Lychnis chalcedonica L. Flavonoids on Transplanted Tumor Development and Cytostatic Therapy Effectiveness in Mice

A complex of biologically active compounds was isolated from Lychnis chalcedonica L. cultivated at the Siberian Botanical Garden at Tomsk State University. HPLC analysis found that the isolated compounds were flavonoids with retention times 10.40, 12.45, 13.29, and 15.47 min. The major flavonoid constituent was vicenin with tr = 13.29 min and a peak area of 87.4%. The flavonoid complex of L. chalcedonica was studied using three transplanted tumor models, i.e., Lewis lung carcinoma (LLC), melanoma B-16 (B-16), and lung cancer RL-67 (RL-67). Tests on C57BL/6 mice showed that the L. chalcedonica flavonoid complex inhibited development of melanoma B-16. Co-administration of L. chalcedonica flavonoids and cyclophosphamide enhanced the antitumor effect of the cytostatic in animals with B-16, RL-67, and LLC.

Datum: 01.08.2019

Synthesis and In Vivo Evaluation of New Coumarin Conjugates as Potential Indirect-Action Anticoagulants

A synthetic method for a series of new coumarin conjugates was developed. Their structures and physicochemical properties were determined by modern spectral methods (IR, NMR, ESI-MS). The anticoagulant activity was studied in vivo by determining the prothrombin time (PT). Compounds 4a (PT = 10.88 ± 0.56 sec) and 4b (13.10 ± 3.56 sec) were the most active and comparable to the reference drug warfarin (7.97 ± 1.93 sec).

Datum: 01.08.2019

Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity

New 4-phenylpyrrolidone derivatives were designed from racetam structures that combine nootropic and anticonvulsant activity. The proposed compounds were synthesized using 4-phenylpyrrolidone and aromatic amines. The anticonvulsant activity of the new compounds was studied. The structure–activity relationship was analyzed. The most active compound was the 2,6-dimethylanilide of (2-oxo-4-phenylpyrrolidin-1-yl)acetic acid at doses of 2.5 – 5.0 mg/kg, which surpassed the reference drug levetiracetam at doses of 2.5 – 600 mg/kg in all tests and possessed distinct nootropic activity that was comparable to that of the reference nootropic drug piracetam at a dose of 400 mg/kg.

Datum: 01.08.2019

Using a Molecular Sensor Array with Colorimetric Detection to Identify Active Ingredients in Drug Formulations

A method for multiplex digital colorimetric qualitative analysis of nonsteroidal anti-inflammatory drugs (meloxicam, acetylsalicylic acid and its metabolites, paracetamol), β-adrenoblockers (carvedilol), secretolytics (bromhexine), fluoroquinolones (ofloxacin), metabolic stimulants (meldonium dihydrate), etc., was developed. The molecular chip operating efficiency was confirmed by verifying the authenticity of >40 medicinal substances. The proposed universal approach was new in principle and could be used for pharmaceutical quality control.

Datum: 01.07.2019

Antiviral Properties of the New Coordination Compound Silver Bis(Citrato)Germanate

The new coordination polymer silver bis(citrato)germanate was synthesized and exhibited pronounced antiviral activity against human influenza virus strains A/Hong Kong/1/68 (H3N2) and A/Puerto Rico/34 (H1N1). Its effective dose was five times lower than that of the reference drug oseltamivir, which made this compound promising for further studies in animal models.

Datum: 01.07.2019

Insulin Preparation for Blood Glucose-Level Regulation

A new approach for delivering insulin into the bloodstream through the gastrointestinal system after peroral administration of diluted insulin solutions to animals with experimental diabetes was studied. It was shown that such solutions provided a physiological pathway for delivering insulin into the bloodstream.

Datum: 01.07.2019

Development of a Technique for Codetermination of Tannin and Gallic Acid in Medicinal Plant Raw Material

Development and validation of a new technique for direct spectrophotometric quantitative determination of high- and low-molecular-mass tannins are reported. The proposed method enables simultaneous codetermination using Firordt calculations of tannins and gallic acid in medicinal plant raw material and herbal preparations without preliminary separation from complicated mixtures with other biologically active compounds found in the plant extracts. The developed method was validated (using nettle raw material as an example). The contents of gallic acid and tannins in the samples were (1.20 ± 0.04)% and (1.52 ± 0.03)%, respectively, which agreed with literature data.

Datum: 01.07.2019


Category: Current Chemistry Research

Last update: 11.04.2018.

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