STUDY LOW MOLECULAR WEIGHT BIOLOGICALLY ACTIVE COMPOUNDS, VEGETABLE AS LOOKING AGENTS FOR PREVENTION AND TREATMENT SEBORRHEA

The search for biologically active compounds that regulate liver function in fibrosis is an urgent medical and biological problem. A working hypothesis was tested, according to which low molecular weight biologically active compounds from Pleurotus ostreatus and Sacharamirses cerevisiae are capable of exerting immunomodulatory and antitoxic effects after intoxication of the body with ions of heavy metals, in particular copper sulfate. Elimination of the toxic effect caused by copper sulfate can also ensure the normalization of liver function in various pathologies, in particular with liver fibrosis. When determining toxicity, a study was carried out on Wistar rats, and when studying the effect of low molecular weight biologically active compounds on liver function, clinical trials were carried out on volunteers. The activity of alanine aminotransferase, aspartate aminotransferase, actonitase and glutathione peroxidase, as well as the content of bilirubin and lipid hydroperoxides were determined. It was shown that preliminary administration of biologically active compounds to rats at a dose of 0.05 mL/100 g of body weight provided the formation in some animals (up to 80%) of resistance to the toxic effect of copper sulfate (dose 2.5 mg/100 g of body weight). Such stability is associated with a shift in the balance of “prooxidants-antioxidants” towards antioxidants. The data obtained in the clinic on volunteers with liver fibrosis and hepatitis also testify in favour of the membranotropic action of biologically active compounds. Biologically active compounds provided a decrease or complete restoration of the activity of transferases (ALT and AST) in the blood serum of these patients, with the exception of one patient out of 20 examined. Our experiment has shown the relationship between the elimination of toxicity to the action of copper sulfate and the normalization of liver function in patients. The results obtained indicate that it will be promising to use a complex of low molecular weight components from P. ostreatus and S. cerevisiae as an antidote and hepatoprotective agent.

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Chemical ionization mass spectra of high molecular weight, biologically active compounds produced following supercritical fluid chromatography

Journal of Mass Spectrometry ◽

10.1002/bms.1200150409 ◽

1988 ◽

Vol 15 (4) ◽

pp. 239-242 ◽

Cited By ~ 19

Author(s):

H. T. Kalinoski ◽

B. W. Wright ◽

R. D. Smith

Keyword(s):

Molecular Weight ◽

High Molecular Weight ◽

Supercritical Fluid ◽

Supercritical Fluid Chromatography ◽

Mass Spectra ◽

Chemical Ionization ◽

Biologically Active Compounds ◽

Biologically Active ◽

Ionization Mass ◽

Active Compounds

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Low-molecular-weight heparin in the prevention and treatment of thromboembolic disorders

Disease Management and Clinical Outcomes ◽

10.1016/s1088-3371(98)00015-1 ◽

1998 ◽

Vol 1 (5) ◽

pp. 166-174 ◽

Cited By ~ 1

Author(s):

Evelyn R Hermes De Santis ◽

Betsy S Laumeister ◽

Vidhu Bansal ◽

Vandana Kataria ◽

Preeti Loomba ◽

...

Keyword(s):

Molecular Weight ◽

Low Molecular Weight Heparin ◽

Low Molecular Weight ◽

Prevention And Treatment

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EFFICIENCY AND PERSPECTIVES OF HIGH-THROUGHPUT SCREENING IN GRID – CSLABGRID EXPERIENCE IN EFFECTIVE SEARCHING FOR NEW BIOLOGICALLY ACTIVE COMPOUNDS

Visnik Nacional noi academii nauk Ukrai ni ◽

10.15407/visn2016.08.068 ◽

2016 ◽

pp. 68-72

Author(s):

P.A. Karpov ◽

◽

Ya.B. Blume ◽

Keyword(s):

High Throughput ◽

High Throughput Screening ◽

Biologically Active Compounds ◽

Biologically Active ◽

Active Compounds

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Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

10.26434/chemrxiv.6198929 ◽

2018 ◽

Author(s):

Honggui Lv ◽

Li-Jun Xiao ◽

Dongbing Zhao ◽

Qi-Lin Zhou

Keyword(s):

Butyric Acid ◽

Biologically Active Compounds ◽

Biologically Active ◽

Active Compounds ◽

Highly Efficient ◽

Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

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SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

SERIES CHEMISTRY AND TECHNOLOGY ◽

10.32014/2020.2518-1491.84 ◽

2020 ◽

Vol 5 (443) ◽

pp. 85-91

Author(s):

Ibrayev M.K., ◽

◽

Takibayeva A.T., ◽

Fazylov S.D., ◽

Rakhimberlinova Zh.B., ◽

...

Keyword(s):

13C Nmr Spectroscopy ◽

Biologically Active Compounds ◽

Biologically Active ◽

Active Compounds ◽

Synthesis Conditions ◽

Alkaloid Cytisine ◽

Azole Ring ◽

Cyclic Compounds ◽

New Compounds ◽

Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

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Lactoferrin in Bone Tissue Regeneration

Current Medicinal Chemistry ◽

10.2174/0929867326666190503121546 ◽

2020 ◽

Vol 27 (6) ◽

pp. 838-853 ◽

Cited By ~ 6

Author(s):

Madalina Icriverzi ◽

Valentina Dinca ◽

Magdalena Moisei ◽

Robert W. Evans ◽

Mihaela Trif ◽

...

Keyword(s):

Bone Tissue ◽

Tissue Regeneration ◽

Bone Cells ◽

Bone Diseases ◽

Biologically Active Compounds ◽

Biologically Active ◽

Bone Tissue Regeneration ◽

Bone Homeostasis ◽

Active Compounds

: Among the multiple properties exhibited by lactoferrin (Lf), its involvement in bone regeneration processes is of great interest at the present time. A series of in vitro and in vivo studies have revealed the ability of Lf to promote survival, proliferation and differentiation of osteoblast cells and to inhibit bone resorption mediated by osteoclasts. Although the mechanism underlying the action of Lf in bone cells is still not fully elucidated, it has been shown that its mode of action leading to the survival of osteoblasts is complemented by its mitogenic effect. Activation of several signalling pathways and gene expression, in an LRPdependent or independent manner, has been identified. Unlike the effects on osteoblasts, the action on osteoclasts is different, with Lf leading to a total arrest of osteoclastogenesis. : Due to the positive effect of Lf on osteoblasts, the potential use of Lf alone or in combination with different biologically active compounds in bone tissue regeneration and the treatment of bone diseases is of great interest. Since the bioavailability of Lf in vivo is poor, a nanotechnology- based strategy to improve the biological properties of Lf was developed. The investigated formulations include incorporation of Lf into collagen membranes, gelatin hydrogel, liposomes, loading onto nanofibers, porous microspheres, or coating onto silica/titan based implants. Lf has also been coupled with other biologically active compounds such as biomimetic hydroxyapatite, in order to improve the efficacy of biomaterials used in the regulation of bone homeostasis. : This review aims to provide an up-to-date review of research on the involvement of Lf in bone growth and healing and on its use as a potential therapeutic factor in bone tissue regeneration.

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Diverse thiophenes as scaffolds in anti-cancer drug development: A concise review

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666201202113333 ◽

2020 ◽

Vol 20 ◽

Author(s):

Neha V. Bhilare ◽

Pratibha B. Auti ◽

Vinayak S. Marulkar ◽

Vilas J. Pise

Keyword(s):

Drug Development ◽

Anticancer Agents ◽

Heterocyclic Ring ◽

Biologically Active Compounds ◽

Biologically Active ◽

Cancer Drug ◽

Active Compounds ◽

Natural Origin ◽

Concise Review ◽

Anti Cancer

: Thiophenes are one among the abundantly found heterocyclic ring systems in many biologically active compounds. Moreover various substituted thiophenes exert numerous pharmacological actions on account of their isosteric resemblance with compounds of natural origin thus rendering them with diverse actions like antibacterial, antifungal, antiviral, anti-inflammatory, analgesic, antiallergic, hypotensives etc.. In this review we specifically explore the chemotherapeutic potential of variety of structures consisting of thiophene scaffolds as prospective anticancer agents.

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New Potential Biologically Active Compounds: Synthesis and Characterization of Urea and Thiourea Derivativpes Bearing 1,2,4-oxadiazole Ring

Current Organic Synthesis ◽

10.2174/1570179417666200417112106 ◽

2020 ◽

Vol 17 (7) ◽

pp. 525-534 ◽

Cited By ~ 1

Author(s):

Nevin Arıkan Ölmez ◽

Faryal Waseer

Keyword(s):

Microwave Irradiation ◽

Room Temperature ◽

Antimicrobial Activities ◽

Phenyl Isocyanate ◽

Single Step ◽

Biologically Active Compounds ◽

Biologically Active ◽

Active Compounds ◽

Thiourea Derivatives ◽

Acyl Chlorides

Background: Urea, thiourea, and 1,2,4-oxadiazole compounds are of great interest due to their different activities such as anti-inflammatory, antiviral, analgesic, fungicidal, herbicidal, diuretic, antihelminthic and antitumor along with antimicrobial activities. Objective: In this work, we provide a new series of potential biologically active compounds containing both 1,2,4-oxadiazole and urea/thiouprea moiety. Materials and Methods: Firstly, 5-chloromethyl-3-aryl-1,2,4-oxadiazoles (3a-j) were synthesized from the reaction of different substituted amidoximes (2a-j) and chloroacetyl chloride in the presence of pyridine by conventional and microwave-assisted methods. In the conventional method, 1,2,4-oxadiazoles were obtained in two steps. O-acylamidoximes obtained in the first step at room temperature were heated in toluene for an average of one hour to obtain 1,2,4-oxadiazoles. The yields varied from 70 to 96 %. 1,2,4-oxadiazoles were obtained under microwave irradiation in a single step in a 90-98 % yield at 160 °C in five minutes. 5-aminomethyl-3-aryl-1,2,4- oxadiazoles (5a-j) were obtained by Gabriel amine synthesis in two steps from corresponding 5-chloromethyl-3- aryl-1,2,4-oxadiazoles. Finally, twenty new urea (6a-j) and thiourea (7a-j) compounds bearing oxadiazole ring were synthesized by reacting 5-aminomethyl-3-aryl-1,2,4-oxadiazoles with phenyl isocyanate and isothiocyanate in tetrahydrofuran (THF) at room temperature with average yields (40-70%). Results and Discussions: An efficient and rapid method for the synthesis of 1,2,4-oxadiazoles from the reaction of amidoximes and acyl halides without using any coupling reagent under microwave irradiation has been developed, and twenty new urea/thiourea compounds bearing 1,2,4-oxadiazole ring have been synthesized and characterized. Conclusion: We have synthesized a new series of urea/thiourea derivatives bearing 1,2,4-oxadiazole ring. Also facile synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from amidoximes and acyl chlorides under microwave irradiation was reported. The compounds were characterized using FTIR, 1H NMR, 13C NMR, and elemental analysis techniques.

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