Step-Wise, Tandem One-Pot Syntheses and Antifungal Evaluation of 2-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-arylbenzamides in Water – a Green Protocol
Springer » Pharmaceutical Chemistry Journal
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2d ago
One-pot, eco-friendly, three-component syntheses of 2-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-aryllbenzamides have been developed by combining phthalic anhydride with anilines and anthranilamide in water without any catalyst. The reactions are simple to set up, have excellent yields, and employ water as solvent, making their synthesis an environmentally friendly procedure. All synthesized compounds were tested against fungal strains, and compounds 4c, 4d, 4g, and 4i showed prominent activity ..read more
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The Role of the HL-10 Peptide in Regulating the Expression of Apoptosis-Related Genes in the HeLa Cancer Cell Line
Springer » Pharmaceutical Chemistry Journal
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6d ago
Anticancer peptides are among the most important bioactive peptides found in animal sources. The modulation of the molecular process of apoptosis via the genes involved in the signaling pathway is now being studied for cancer treatment. In this study, the anticancer properties of peptide HL-10 extracted from scorpion venom by regulating the apoptosis signaling pathway were investigated. In the present study, the anticancer activity of the HL-10 peptide against the HeLa cancer cell line was assessed using the cytotoxicity assay. The real-time PCR method was used to analyse the expression levels ..read more
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Stereospecificity of the Cytoprotective and Antidepressant-Like Activities of GTS-301, a Dimeric Dipeptide Mimetic of Neurotrophin-3
Springer » Pharmaceutical Chemistry Journal
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6d ago
A dimeric dipeptide mimetic based on the β-turn of the 4th loop of neurotrophin-3, bis-(N-monosuccinyl-L-asparaginyl-L-asparagine)hexamethylenediamide (GTS-301LL), was recently designed and synthesized by us. GTS-301, like the full-length neurotrophin, activated TrkC and TrkB receptors and exhibited neuroprotective activity on HT22 cells under oxidative stress conditions in the concentration range 10–5 – 10–12 M and antidepressant-like activity in the forced swimming test in mice (10 – 40 mg/kg, intraperitoneally). The stereospecificity of the pharmacological effects of GTS-301LL was revealed ..read more
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In Vitro Antioxidant Activity of Asteriscus Graveolens (Forsk.) and Its Protective Effect on Doxorubicin-Induced Hepatotoxicity and Testicular Oxidative Damage in Rats
Springer » Pharmaceutical Chemistry Journal
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6d ago
Asteriscus graveolens (Asteraceae) is a medicinal herb, used in Algeria to treat diabetes, hypertension, pain, fever, inflammation and gastrointestinal diseases. Doxorubicin (DOX) is an antibiotic antineoplastic drug used to treat many types of cancers; unfortunately, its antitumor activity links toxic effects to several organs including the heart, liver and testis. The appropriate mechanism of its organotoxicity is linked to free reactive oxygen species (ROS) generation and oxidative stress induction. In this study, the antioxidant and protective role of A. graveolens and vitamin E (Vit E) ag ..read more
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Chemical Composition and Antioxidant Activity of Petroleum Ether Extract from Kaempferia galanga L.
Springer » Pharmaceutical Chemistry Journal
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6d ago
Kaempferia galanga L. (KGL) from Hainan, China was extracted by ultrasonic-assisted extraction with 90% ethanol solution, and then extracted with petroleum ether after the ethanol extract was recovered to be alcohol free. The antioxidant activity of the petroleum ether fraction of KGL was first tested using the ABTS method. GC-MS was used to analyze the chemical constituents of the petroleum ether fraction. The scavenging effect on ABTS free radicals of the petroleum ether fraction was weak, indicating that the antioxidant activity of the petroleum ether fraction was moderate. A total of 25 ch ..read more
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Correction to: Genotoxic Effects of New Azoloazine Derivatives with Antitumor Activity in MCF-7 Tumor Cell Culture
Springer » Pharmaceutical Chemistry Journal
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6d ago
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Study of the Pressing Process of N-Butyl-N-Methyl-1-Phenylpyrrolo-[1,2-a]Pyrazine-3-Carboxamide (GML-3) Tablets Using Mathematical Modeling Techniques
Springer » Pharmaceutical Chemistry Journal
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1w ago
N-Butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) is an original molecule developed at the Research Zakusov Institute of Pharmacology. GML-3 has both anxiolytic and antidepressant activity, which makes the development of tablets based on it a promising task. Optimization of the pressing process is currently an urgent task of the pharmaceutical industry because this technological stage has a significant impact on the disintegration of tablets and the release of the active pharmaceutical ingredient. The Heckel and Kuenz–Leuenberger models were used to study the pressing proce ..read more
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Synthesis, Characterization and Biological Evaluation of Novel Benzimidazole Derivatives against Candida albicans
Springer » Pharmaceutical Chemistry Journal
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1w ago
In heterocyclic chemistry, benzimidazole is recognized as a “privileged structure” due to its association with a wide range of biological activities. In this present research work, we included the synthesis, characterization and biological evaluation of substituted derivatives. The designated derivatives were synthesized by the condensation method. ortho-Phenylenediamine was used as the starting material. The designated benzimidazole derivatives were synthesized using different acids and aldehydes. Further, the in-vitro antifungal-activity-synthesized compounds were evaluated against Candida a ..read more
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In-Vitro Effect of Ammodaucus Leucotrichus Flower and Fruit Essential Oils on Nitric Oxide Production and Arginase Activity in Human Peripheral Blood Mononuclear Cells (PBMC) from Patients with Behçet Disease
Springer » Pharmaceutical Chemistry Journal
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1w ago
Ammodaucus leucotrichus is an Algerian aromatic medicinal plant, widely known as “Oum-draiga or Kamoune-l’ibel”. In folk medicine, the flower and fruit of this plant are widely used for the treatment of cough, fever, diarrhea, colic, and cold. In this study, we describe for the first time the modulatory effects of flower and fruit essential oils (EOs) of A. leucotrichus subsp. leucotrichus on NOS and Arginase activities and their regulation during Behçet disease, an auto-inflammatory vasculitis of unknown etiology. The EOs were obtained by Clevenger-hydrodistillation and their chemical composi ..read more
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Prospects of Creating Collagen Substances Based on a Study of the Physical and Chemical Characteristics of Proteins of Hydrobiont Dermal Emulsions
Springer » Pharmaceutical Chemistry Journal
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1w ago
Proteins of the collagen family were identified in the dermal emulsion of a freshwater fish, the African clary catfish (Clarias gariepinus). Acumulative assessment of their physicochemical properties gave reason to consider the emulsion obtained using the developed method as a source of functional biopolymers, particularly collagen proteins. The fractional composition, charge state, molecular mass, and the ability for hydrolysis by Clostridium histolytica collagenase were experimentally determined. Evaluation of the amino-acid composition allowed the analogy and features of collagen proteins o ..read more
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