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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

Controlled-Release Matrixes for Drugs Based on Polyamide-Polyhydroxybutyrate Compositions

The transport properties of films based on poly(3-hydroxybutyrate) (PHB) and polyamide were studied. The factor responsible for the rate of controlled release of antiseptic from film compositions was the link between diffusion and PHB destruction. A model of this process and measurements of the coefficients of diffusion of an antiseptic are presented. The fundamental possibility of using these compositions as matrix systems for prolonged (more than one month) controlled delivery of a model pharmaceutical (the antiseptic furacillin) with constant and controllable release rates is discussed. The study matrixes could be used as wound coverings (dressings).

Datum: 19.04.2018

Effects of 3-Hydroxypyridine and Succinic Acid Derivatives on Monoamine Oxidase Activity In Vitro

The effects of original Russian 3-hydroxypyridine and succinic acid derivatives (emoxypine, Reamberin, and Mexidol) on monoamine oxidase (MAO-A and MAO-B) activity in rat liver were studied in vitro. The study drugs used in vitro at concentrations in the pharmacokinetic range (10 9 to 10 6 M), were found to have MAO-modulating actions, the directions depending on their chemical structural properties. The isolated 3-hydroxypyridine derivative emoxypine decreased MAO-A activity by 34 – 44% and MAO-B activity by 9 – 10% (p < 0.05 in both cases). The succinic acid derivative Reamberin increased MAO-A activity by 2-3% and MAO-B activity by 14% (p < 0.05 in both cases). Mexidol, which is a derivative of both 3-hydroxypyridine and succinic acid, decreased MAO-A activity by 13% and MAO-B activity by 4% (p < 0.05 in both cases). The 2-ethyl-3-methyl-3-hydroxypyridinium cation and the succinate anion were antagonists in terms of their MAO-modulating actions. Combining these antagonist ions into the structure of Mexidol led to complete loss of the MAO-stimulating effect of the succinate part and a significant reduction in the MAO-inhibiting action of the 3-hydroxypyridine component.

Datum: 19.04.2018

Development of an Industrial Reference Sample for the Specific Activity of Erythropoietin

On the basis of WHO recommendations and the principles developed for the standardization of erythropoietins we selected one epoetin alfa pharmaceutical substances included in the State Register of Medicines as a candidate reference sample. The results of the manufacturer’s monitoring of this pharmaceutical substance complied with the requirements of the normative documentation and additional verification of identity by capillary zone electrophoresis demonstrated the presence of eight isoforms, which corresponded to the requirements of the European Pharmacopeia. Conditions for the preparation of an industrial reference sample in lyophilized form were developed. The industrial reference sample was attested in interlaboratory tests and the value of the attested property - specific activity - was 2400 IU/ampule, with confidence limits of 94.5% to 105.8%. Studies of the stability of the industrial reference sample developed here gave a shelf life of five years at a storage temperature of -20°C, with potential to extend this on the basis of stability monitoring results.

Datum: 16.04.2018

Solvent-Free Synthesis and Antibacterial Evaluation of Novel Coumarin Sulfonamides

A series of new coumarin-6-sulfonamides have been synthesized as potential antibacterial agents. The reaction of coumarin with chlorosulfonic acid was found to yield the corresponding coumarin sulfonyl chloride (1). In the next step, coumarin sulfonyl chloride, was reacted with various amines in the presence of K2CO3 under solvent-free conditions to produce coumarine sulfonamides (2a – 2s) in good to excellent yields. The chemical structures of the products were elucidated by IR, 1H NMR, and 13C NMR spectroscopy and elemental analysis. All the synthesized compounds have been screened for their in vitro anti-bacterial activities against Escherichia coli and Staphylococcus aureus bacteria.

Datum: 16.04.2018

Synthesis and Anticonvulsive Activity of 3- and 4-Benzoylpyridine Oxime Derivatives

We present here the synthesis of 3- and 4-benzoylpyridine oxime derivatives with potential anticonvulsant action. The most active compound in the maximum electric shock test was 4-benzoylpyridine O-2-morpholinoethyloxime oxalate (1a), i.p. doses of 60 – 150 mg/kg of which increased the survival of mice to 100%. The best effect in the corasol antagonism test was obtained with 4-benzoylpyridine O-(isonicotinoyl)oxime (2c), i.p. doses of 12.5 mg/kg of which increased the survival of mice to 67% and the latent period of onset of generalized tonic-clonic convulsions to 52 sec. Compound 1a had low toxicity (the i.p. LD50 in mice was 316 mg/kg) and a therapeutic index of 21.

Datum: 16.04.2018

Effects of Pharmaceutical Preparations on the Rate of Degradation of Poly(Lactide-Co-Glycolide) Scaffolds

The effects of acetylsalicylic acid, ibuprofen, 6-methyluracil, and chondroitin sulfate impregnated in poly-(lactide-co-glycolide) scaffolds of different chemical compositions and molecular weights using supercritical carbon dioxide on the processes of scaffold degradation in phosphate-buffered saline pH 7.4 were studied and the rate constants of these processes were determined. Incorporation of acetylsalicylic acid and ibuprofen into poly(lactide-co-glycolide) scaffolds was found to produce significant increases in the rate of hydrolysis of the polymer base, while the presence of methyluracil and chondroitin sulfate had virtually no effect.

Datum: 16.04.2018

Sustained-Release Tablets of Hydrochlorothiazide, a Slightly Water-Soluble Molecule Using Glyceryl Behenate

Hydrochlorothiazide (Hctz) is an antihypertensive drug acting as diuretic. In order to prolong the drug activity, various formulations of Hctz were developed. This work was aimed at developing a sustained-release formulation using glyceryl behenate (Compritol 888 ATO, C888) as a waxy retardant matrix and Hctz as the model of slightly water-soluble drug. Two different ratios of Hctz/C888 (1:1 and 1:2) were tried to determine if increasing the C888 fraction will retard the release of Hctz. Melt granulation and direct compression have been tested on the two ratios in order to identify which one is most effective to modify the release of Hctz. The results showed that the 1:2 ratio (Hctz 25 mg versus C888 50 mg) successfully retarded the dissolution of Hctz. On the other hand, hot fusion method was found to be more effective than compression of physical mixtures in retarding the drug dissolution from the matrix. Thus, formulations based on the appropriate matrix of Compritol 888 ATO can be used to produce prolonged-release tablets for slightly water-soluble drugs like Hctz.

Datum: 16.04.2018

Multidrug Resistance Reversal Activity of Some New Dihydropyridines Studied by IN SITU Single-Pass Intestinal Perfusion (SPIP) Method in Rat

P-glycoprotein (P-gp) mediated efflux affects the pharmacokinetics of several drugs. By analogy to verapamil, 1,4-dihydropyridines (DHPs) have been widely studied as P-gp inhibitors. Previously, we have reported on two new DHPs: IA1(A) and IIA5(B) as inhibitors of human MRP1, an efflux protein closely related to P-gp. The aim of the present study was to investigate the inhibitory effects of these two compounds on intestinal P-gp using the method of in situ single-pass intestinal perfusion (SPIP) in rat. According to this, the intestinal absorption of zidovudine (a P-gp substrate) was studied in anaesthetized rat jejunum in the absence and presence of DHPs IA1(A) and IIA5(B) (2 mg/kg). Verapamil (0.8 mg/kg), a well-known P-gp inhibitor, was employed as a standard. Zidovudine solution (200 ig/mL) in phosphate buffer (pH 7.4) was perfused through the jejunal segment, the perfusate concentrations were quantified by HPLC, and the permeability coefficient (Peff) and fraction absorbed (Fabs) were calculated. Phenol red was used as a non-absorbable marker to correct water flux through the segment. In rats pretreated with compounds IA1 and IIA5, Peff and Fabs of zidovudine were found to be 0.1669 ± 0.12 cm/sec, 0.2035 ± 0.18 and 0.2798 ± 0.12 cm/sec, 0.3015 ± 0.14, respectively, and were comparable to those of the standard (Peff = 0.462713 ± 0.3 cm/sec, Fabs = 0.511835 ± 0.14). The differences between IA1, IIA5 and the standard were evaluated using ANOVA and found to be statistically significant (P < 0.05). Compounds IA1 and IIA5 have a modulating effect on intestinal P-gp. Compound IIA5 was relatively more potent P-gp inhibitor and, quite interestingly, the results were in agreement with our earlier in silico and in vitro studies.

Datum: 16.04.2018

Synthesis and Antiaggregant Activity of 2-[3-Methyl-1-Ethylxanthinyl-8-Thio]Acetic Acid Salts Containing a Thietane Ring

Reaction of 7-(thietanyl-3)-, 7-(1-oxothietanyl-3)-, and 7-(1,1-dioxothietanyl-3)-8-bromo-3-methyl-1-ethylxanthines with thioglycolic acid produced 2-[3-methyl-1-ethylxanthinyl-8-thio]acetic acids containing a thietane ring with yields of 76 – 93%. Interaction of these acids with bases (sodium hydroxide, morpholine, hexamethyleneimine) produced 2-[3-methyl-1-ethylxanthinyl-8-thio]acetic acid salts containing a thietane ring, with yields of 44 – 96%. The structures of these compounds were confirmed by IR and NMR spectroscopy data. The compounds synthesized here had potentially high antiaggregatory activity.

Datum: 16.04.2018

A Study on Essential Oil Chemical Compositions, Antioxidant, and Antimicrobial Activities of Native and Endemic Satureja Species Growing in Iran

In this study, chemical compositions of the essential oil and antioxidant activities of four Satureja species, namely S. hortensis (SH), S. bachtiarica (SB), S. laxiflora (SL), and S. intermedia (SI) were evaluated. GC and GC/MS were employed to analyze the essential oil samples extracted via hydrodistillation. DPPH and FRAP assays were used to evaluate the radical scavenging and antioxidant properties as well as antimicrobial activities. The GC and GC/MS analysis revealed and identified a total of 25 compounds. The most abundant chemical constituents were ρ-cymene (13.07 – 17.50%) in all four species, γ-terpinene in SL, SH, and SI (11.35 – 37.60%), thymol in SL, SB, and SI (24.54 – 38.75%), and carvacrol in SB and SH (32.07 – 42.51%). The FRAP assay showed that none of the methanol and dichloromethane extracts possessed significant antioxidant activity as compared to quercetin. In addition, the radical scavenging activity of SB and SI methanol extracts were higher than that of SL and SH (DPPH assay). However, all extracts did not show potent radical scavenging activities. It should be noted that this study was the first to evaluate the possible antioxidant or radical scavenging properties of SI and SL. The antimicrobial assay demonstrated a potent activity of all samples against Escherichia coli, Staphylococcus aureus, Candida albicans, Aspergillus fumigatus, and Epidermophyton floccosum (minimum inhibitory concentrations, MIC = 0.06 – 8 μg/mL). Due to rich content of thymol and carvacrol isomers in Satureja species, they can be suggested for use in various pharmacological applications.

Datum: 16.04.2018

Antitumor Potential of Substances from the Fungus Ganoderma lucidum

We present here a review of published data mostly from the last 10 years on the antitumor activity of substances from the fungus Ganoderma lucidum. Its main biologically active components are described, particularly triterpenes, polysaccharides, glycoproteins, and proteoglycans. The mechanisms of the antitumor actions of these compounds in vitro and in vivo are discussed, these including blockade of the cell cycle, induction of apoptosis, decreases in the metastatic potential, suppression of angiogenesis, and immunomodulatory activity. The potential of using substances from G. lucidum for the treatment of oncological patients is assessed.

Datum: 16.04.2018

Current Requirements for Assessment of Elemental Impurities (Heavy Metals) in Medicines

One element of ensuring the quality and safety of medicines consists of normalizing and controlling elemental impurities (heavy metals). The sources and causes of the presence of elemental impurities (heavy metals) in medicines are discussed. Changes in approaches to assessment of elemental impurities in medicines in the State Pharmacopeia and leading non-Russian pharmacopeias are discussed. A risk-oriented approach to assessing elemental impurities used in international practice is presented.

Datum: 16.04.2018

Design, Synthesis, and Pharmacological Activity of a New Matrix Metalloproteinase-9 Inhibitor

The new MMP-9 inhibitor 1-{4-[(4-chlorobenzoyl)amino]phenyl}sulfonyl-L-proline, with a theoretical inhibition constant of IC50 = 4 × 105 M, was constructed on the basis of structural requirements for selective inhibitors of gelatinases. This constructed compound and its close structural analogs were synthesized and these substances were found to have low toxicity, (LD50 > 300 mg/kg). The new inhibitor given p.o. at a dose of 20 mg/kg/day on the background of acute myocardial infarction significantly decreased the content of immunoreactive MMP-9 in plasma in rats, to the level obtained with doxycycline.

Datum: 14.04.2018

Acetoxybenzoylglycylglycines as Potential Cerebroprotective Compounds

3,4,5-Trimethoxy- and 2-, 3-, and 4-acetoxybenzoylglycylglycines and their water-soluble potassium and lithium salts were synthesized. The cerebroprotective properties of the water-soluble potassium and lithium salts of acetoxybenzoylglycylglycines were studied experimentally. The most marked cerebroprotective proteins in cerebral ischemia were found with the lithium salt of 2-acetoxybenzoylglycylglycine.

Datum: 14.04.2018

Encapsulation and Controlled Release of Vitamin B 2 Using Peracetyl-β-Cyclodextrin Polymer-Based Electrospun Nanofiber Scaffold

Hydrophobic β-cyclodextrin polymer nanofibers were obtained by the electrospinning of peracetyl-β-cyclodextrin polymer (AcβCDP) from acetone : DMF (3 : 2 v/v) solution. The morphology of AcβCDP nanofibers was studied by scanning electron microscopy. The proposed novel hydrophobic β-CD polymer was synthesized through reaction of water-soluble β-CD polymer crosslinked with epichlorohydrin (β-CD-ECH polymer) and acetic anhydride in the presence of pyridine. The peracylation of β-CD-ECH polymer is verified by FT-IR and solubility data. The final part of this study is focused on incorporating vitamin B2 (VB2) into the AcβCDP nanofiber. In vitro release of VB2 from AcβCDP/VB2 nanofiber in model physiological media was investigated; the results exhibited initial burst and then slow drug release. The release of VB2 from AcβCDP/VB2 nanofiber is slower than from AcβCDP/VB2.

Datum: 14.04.2018

Correction to: Hemostasis Parameters and Toxic Effects of 3-Substituted and Condensed Chromen-2-Ones (Coumarins)

Due to an error in preparing the XML file of this paper, all numerical data in Table 1 were omitted. The corrected table appears below:

Datum: 01.03.2018

Novel Free-Radical Scavengers Based on Ferrofluid/Polyaniline Nanocomposites

We investigated the antioxidant activity of novel ferrofluid/polyaniline nanocomposites with various mass ratios synthesized via in situ chemical oxidative polymerization of aniline without stirring in the presence of stabilized Fe3O4 nanoparticles and citric acid as a surfactant. The structural, morphological, thermal, magnetic, and electrical properties of the nanocomposites were characterized by IR and UV spectroscopy, XRD, SEM, TEM, TGA, VSM, and four-point-probe methods. The antioxidant potency was determined by modified 2,2-diphenyl-1-picrylhydrazyl (DPPH) method using an in vitro system. The DPPH free-radical scavenging tests of nanocomposites showed that their antioxidant properties depended on the amount of polyaniline in the composition. Results of the comparison of DPPH scavenging capacity of nanofiber polyaniline and granular ferrofluid/polyaniline nanocomposite show that the antioxidant activity is related to the morphology of polyaniline.

Datum: 01.03.2018

Benzimidazole Ring System as a Privileged Template for Anticancer Agents

Cancer still remains a continued threat for human race in the 21st century. It is the major cause of human casualties globally and is thus, a hot topic of research in medicinal laboratories. Scientists are striving to find selective anticancer agents having low toxicity for normal human cells. Heterocyclic ring systems play key role as templates/pharmacophores for various drugs, and benzimidazole ring is especially important for its anticancer derivatives. In this review article, we have focused on the structural features of anticancer derivatives based on benzimidazole ring system. It highlights various benzimidazole-based anticancer compounds which have been developed in recent years.

Datum: 01.03.2018

Compatibility of Ramipril and Lercanidipine Drug Substances in a Single Solid Dosage Form

The chemical properties of ramipril and lercanidipine drug substances were studied to select the conditions necessary for technology development of solid dosage forms. Mixtures containing two or three ingredients were formulated to study the chemical compatibility of the substances and their compatibility with the excipients and were placed into storage. Analyses of these mixtures showed that the substances could be compatible in a single dosage form. Samples of intermediates (mixtures, granulates, tableting masses, tablet cores) and finished products (film-coated tablets) were manufactured, placed into storage, and analyzed to find the optimum processing factors. It was proven that the tableting process and the coexistence of ramipril and lercanidipine in any kinds of intermediates had significant effects on the ingrowth of impurities. The need to use bilayer tablet technology was justified.

Datum: 01.03.2018

Synthesis and Antidepressant Properties of 3-Methyl-7-(1,1-Dioxothietan-3-YL)-8-Cyclohexylamino-1-Ethyl-1 H -Purine-2,6(3 H ,7 H )-Dione

3-Methyl-7-(1,1-dioxothietan-3-yl)-8-cyclohexylamino-1-ethyl-1H-purine-2,6(3H,7H)-dione was synthesized via the reaction of 8-bromo-3-methyl-7-(1,1-dioxothietan-3-yl)-1-ethyl-1H-purine-2,6(3H,7H)-dione and cyclohexylamine and exhibited antidepressant activity that was most pronounced at a dose of 1.6 mg/kg.

Datum: 01.03.2018


Category: Current Chemistry Research

Last update: 11.04.2018.

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