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.
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- ArchPharm Chemistry in Life Sciences.
Pharmaceutical Chemistry: Current Research Articles - Abstracts
Series of new compounds containing 2-pyrrolidinomethyl and 2-piperazinomethyl groups and 2-morpholino and 2-morpholinoethylamine substituents were synthesized. The antiglycation activities of 2-(morpholin-4-yl)-1-(propen-2-en-1-yl)-1H-benzimidazole and 2-(morpholin-4-yl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole were comparable to that of aminoguanidine. Some compounds exhibited moderate antiserotonin, anti-angiotensin, antioxidant, and dipeptidyl peptidase-4 (DPP-4) inhibitory effects.
The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.
N-Substituted 4-aryl-2-hydroxy-4-oxobut-2-enoic acid hydrazides and their complexes with Ni(II), Mn(II), Co(II), Cu(II), and Zn(II) were prepared. Their antimicrobial activity and behavioral response effects in mice were studied. Compounds with low acute toxicities and activities comparable to or exceeding those of the reference drugs were discovered.
The effect of solvent polarity on bioactive extraction contents of three famous medicinal plants (Securigera securidaca, Portulaca oleracea and Achillea eriophora) with reported analgesic and anti-inflammatory activities was evaluated by GC-MS analysis. Pain and inflammation-lowering properties of all extracts were evaluated and compared to ibuprofen as well-known nonsteroidal anti-inflammatory drug (NSAID). The results indicated that, more extracted sterols, fatty acids, polyols (or alcohols), phenols, and flavonoids from S. securidaca and P. oleracea as well as antraquinone and terpenes from A. eriophora may be responsible for higher analgesic and anti-inflammatory activities of these herbal extracts. Carbon tetrachloride and chloroform (or dichloromethane) more effectively extract phytochemicals than do aqueous ethanol solutions, which can be related to higher solubility of these compounds in the former non-aqueous organic solvents.
3-Acyloxy-5-aryl-7-bromo-1,2-dihydro-3H-1,4-benzodiazepin-2-ones (3 – 18) were synthesized and shown to possess (ED50 = 0.05 – 5 mg/kg) hypnotic, sedative, anticonvulsant, and anxiolytic properties. The hypnotic activity of the tested compounds varied in the dose range 0.22 – 1.50 mg/kg i.p. in mice. The pharmacological properties of 3 – 14 were comparable to those of cinazepam (Levana® IC) and its metabolite 3-hydroxyphenazepam. The CBDR affinity was shown to increase with acyl length in the series C2-C5 whereas it decreased significantly in the series C6-C8. The tested compounds were characterized by low toxicity with LD50 > 650 mg/kg i.p. in mice.
Benzimidazole ring system is well known for its potential for various biological activities. Recent research works have indicated the excellent antiviral potential of various derivatives of this heterocycle. Depending upon the nature of substitution and side chain functionalities, benzimidazole derivatives exhibit anti-HCV, anti-HBV, anti-HIV, anti-HSV, anti-Coxsackie virus, anti-rotavirus, anti-mosquito larvae, anti-PRSV, anti-adenovirus, anti-tobacco mosaic, and anti-Sunn-hemp rosette viruses, etc. In this article, the recent literature available on antiviral benzimidazole derivatives is summarized. The article could be useful in designing new antiviral agents based on this ring system.
An HPLC method was developed for quantitative determination and pharmacokinetic analysis of ivabradine and its N-demethylated metabolite using the new internal standard domperidone. The method is highly sensitive and selective and can be used in bioassays. The sample preparation procedure was optimized and did not significantly influence the standard error of the quantitative chromatographic method.
Method development for determining prekallikrein activator in medicinal preparations of human immunoglobulins and albumin found that the adequacy of chromogenic determination of prekallikrein activator depends on the activity of the used prekallikrein reagent, the quantitative component ratio in the reaction mixture and its incubation time, and the concentration of employed chromogenic reagent. Acceptance criteria for commercial prekallikrein reagents are justified. The main method parameters and validation test results confirming the linearity in the range 0 – 35 IU/mL, accuracy, and intralaboratory precision are presented and correspond to those for biological analytical methods. The elaborated method can be used for quality assessment of prekallikrein activator content in medicinal preparations of human immunoglobulins and albumin.
Zoledronic acid is the drug substance of the highly efficient antiresorptive medicine Zometa. An improved synthesis of zoledronic acid via bis-phosphonation of 2-(1H-imidazol-1-yl)acetic acid is reported.
Natural deep eutectic solvents (NADES) are promising green solvents for extracting biologically active compounds from plant raw material. This is the first study in which NADES were used to extract phlorotannins from brown algae Fucus vesiculosus L. and Ascophyllum nodosum (L.) Le Jolis. The extraction efficiency of polyphenols was evaluated using 10 NADES based on choline chloride, lactic acid, betaine, and glucose in various mole ratios. The effect of H2O in aqueous solutions of NADES on extraction of phlorotannins was studied. Algae were extracted by maceration for 120 min at 50°C with a 1:5 raw-material:extractant ratio. Phlorotannins were quantified by spectrophotometry using the Folin–Ciocalteu method. The maximum extraction of phlorotannins (60 – 72%) was achieved using aqueous NADES solutions (50 – 70%) based on choline chloride with added lactic or malic acid and also on malic acid and betaine. The NADES had efficiencies comparable to Me2CO and EtOH.
Aqueous extracts of nettle leaves (100 mg/kg) and greater burdock roots (25 mg/kg) decreased the blood levels of glucose, triglycerides, total cholesterol, and low- and very-low-density lipoproteins; increased the cholesterol and protein contents of high-density lipoproteins; and prevented low-density lipoprotein oxidation and high-density lipoprotein and hemoglobin glycosylation in experimental diabetes mellitus induced in rats by streptozotocin and a high-fat (30%) diet. The hypolipidemic action of the plant extracts did not decrease if the animals were fed a high-fat diet. Rosiglitazone exhibited more significant hypoglycemic and hypolipidemic effects with a low-fat diet. Flavonoids and carotenoids were responsible for the antidiabetic action of the nettle and burdock extracts.
New fluorenecarboxylic acid derivatives (structural analogs of amizil) were synthesized. A compound with low toxicity (LD50 = 45 ± 9.9 mg/kg) and antidepressant and antianxiety effects was identified. The central and peripheral muscarinic anticholinergic properties of 2-dimethylaminoethyl 9-hydroxyfluorene-9-carboxylate were studied using an arecoline tremor model. Apharmacological analysis showed that the new amizil structural analog exhibited pronounced central muscarinic anticholinergic activity and did not possess peripheral muscarinic anticholinergic effects. The advantages of the tested compound over amizil, amitriptyline that is widely used in the clinic, and the benzodiazepine tranquilizer diazepam were discussed. The results indicated that 2-diethylaminoethyl 9-hydroxyfluorene-9-carboxylate was promising for further development for the treatment of depressive and anxiety disorders.
The property profile of N-decyltropine (IEM-1556) has significant advantages over that of its prototype, the selective nicotinic receptor antagonist tert-butyldecylammonium (IEM-1678), because its anticonvulsant, antiparkinsonian, antidepressant, and analgesic activities are significantly greater and its therapeutic index is 2.8 times higher than that of IEM-1678. The higher pharmacological activity and lower toxicity of IEM-1556 are explained by the fact that IEM-1556 not only blocks nicotinic receptors but also stimulates subdiaphragmatic vagal afferents.
High-throughput screening identified a new class of antibacterial compounds based on N-pyridyl-substituted p- and m-carboxypiperidine amides. Constructs with the two reporter genes RFP and Katushka2S allowed the detection of compounds that inhibit protein translation against DNA biosynthesis. Some agents of this class demonstrated antibacterial activity by inhibiting translation. The most promising compound had an MIC of 12 μg/mL. Thus, this class could become a valuable platform for developing new compounds with higher antibacterial activity and selectivity.
A quantitative HPLC method was developed for analyzing mefebut in pharmacokinetic studies. The method was highly sensitive and selective and could be used for determinations in bioassays. The optimized sample-preparation method did not significantly influence the standard error of the quantitative determination.
Novel thiocoumarins and quinolin-2-ones were synthesized and screened for anticonvulsant activity. The structure–activity relationship of a series of synthesized compounds and previously prepared coumarin derivatives was analyzed. The methyl ester of N-(3-nitro-2-oxo-1,2-dihydroquinolin-4-yl)-4-aminobutyric acid (3a) at a dose of 12.5 mg/kg (i.p.) had the greatest anticonvulsant activity in mouse tests.
Flavonoid glycosides that are present in acylated form have good prospect to be developed into therapeutic agents due to their improved biological properties, stability and physico-chemical properties compared to their maternal compounds. The present study aimed to compare the free radical scavenging and cytotoxic activities of a series of acylated and non-acylated kaempferol glycosides isolated from Stenochlaena palustris. The in silico binding interactions of the most cytotoxic glycoside with epidermal growth factor receptor was also evaluated. Results indicated that the free radical scavenging capability and cytotoxicity of kaempferol 3-O-β-D-glucopyranoside were enhanced through acylation with selected hydroxycinnamoyl groups, whereas mono-acylation did not improve both activities. Molecular docking study revealed that di-acylation was essential for the compound to bind to five major active sites of the receptor. Kaempferol 3-O-β-D-glucopyranosides that are di-acylated may be further explored for their chemopreventive and anticancer properties due to their significant antioxidant and cytotoxic properties.
There is an error in the order of the author names.
The correct order should be: Muhammad Azhar Abbas,1 Afeefa Aslam,2 Mudassir Iqbal,3,* Sajid Bashir,3 Tahir Mehmood,4 and Joerg Kressler5
A quantitative procedure was developed for determining total flavonoids in horse chestnut buds (Aesculus hippocastanum L.) using differential spectrophotometry at 422 nm and recalculation as rhamnocitrin or 7-O-methylkaempferol (3,5,4′-trihydroxy-7-methoxyflavone), the dominant flavonoid in this raw material. The error of a single determination of total flavonoids in horse chestnut buds with 95% confidence probability was ± 2.23%. The contents of total flavonoids in horse chestnut buds varied from (1.24 ± 0.01) to (2.31 ± 0.03)%.
Activation energies for desorption of vinpocetine from silicon (Si) and silicon-dioxide (SiO2) surfaces were analyzed and compared. The molecular mechanism of vinpocetine desorption was found to differ depending on the adsorbent and ionization state, which in turn depended on the pH. Nonpolar interactions between the adsorbent and vinpocetine played a decisive role during desorption from a hydrophobic Si surface without substituents. Quantum-chemical estimates of the activation energy led to the conclusion that vinpocetine in aqueous solution at pH 6.8 and 7 was bound more strongly to SiO2 than to Si. The activation energies for vinpocetine desorption from Si and SiO2 surfaces at pH 2 were statistically indistinguishable and statistically significantly less than the activation energies at pH 6.8 and 7.
Category: Current Chemistry Research
Last update: 11.04.2018.
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