• Title/Summary/Keyword: new drugs

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Synthesis and Biological Valutaion of New 5-Fluorobenzimidazole Antifungal Agents (새로운 5-Fluorobenzimidazole 항진균제의 합성과 생물학적 평가)

  • Ryu, Soung-Ryual
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.1
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    • pp.118-125
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    • 2011
  • New type of 5-fluorobenzimidazole derivatives was synthesized through the reaction of 4-fluoro-5-(2,6-dimethylmorpholinyl)-2-aminoaniline with 5-nitro-2-furoic acid and 5-methoxy-3-chlorobenzothiophene-2-carboxylic acid in presence of PPA and treatment of $OH^-$. the resulting substituted 5-fluorobenzimidazole derivatives(6), (7) was characterized by high solubility in common polar organic solvents. We considered 5-fluorobenzimidazole derivatives were useful especially for antifungal drugs. These results are discussed from the viewpoints of the chemical and physical structures of the 5-fluorobenzimidazole derivatives.

An Algorithm for Predicting Binding Sites in Protein-Nucleic Acid Complexes

  • Han, Nam-Shik;Han, Kyung-Sook
    • Proceedings of the Korean Society for Bioinformatics Conference
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    • 2003.10a
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    • pp.17-25
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    • 2003
  • Determining the binding sites in protein-nucleic acid complexes is essential to the complete understanding of protein-nucleic acid interactions and to the development of new drugs. We have developed a set of algorithms for analyzing protein-nucleic acid interactions and for predicting potential binding sites in protein-nucleic acid complexes. The algorithms were used to analyze the hydrogen-bonding interactions in protein-RNA and protein-DNA complexes. The analysis was done both at the atomic and residue level, and discovered several interesting interaction patterns and differences between the two types of nucleic acids. The interaction patterns were used for predicting potential binding sites in new protein-RNA complexes.

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BIOPHARMACEUTIC PROPERTIES OF DRUGS: NEW TOOLS TO FACILITATE DRUG DISCOVERY AND DEVELOPMENT

  • Amidon, Gordon L.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.3-5
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    • 1997
  • Properties of a good drug include safety, efficacy, half-life and bioavailability. With the current approach to drug discovery based on receptor-based and cell-based screening methods, compounds are frequently moved into development with poor bioavailability. With low bioavailability, drug administration is typically limited to parenteral routes, thus limiting the potential wide-spread utility of these therapeutic agents. The first and most important factor limiting a drug's bioavailability is the intestinal membrane permeability which in turn determines the maximum fi:action of the dose administered that can be absorbed. We have recently utilized new intubation methods for performing permeability measurements in humans and establishing a fundamental human data base for correlating intestinal jejunal membrane permeabilities with permeabilities determined in other systems, e.g., animals, tissue culture, as well as physical chemical properties.

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Antimicrobial Activity of Basil, Oregano, and Thyme Essential Oils

  • Sakkas, Hercules;Papadopoulou, Chrissanthy
    • Journal of Microbiology and Biotechnology
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    • v.27 no.3
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    • pp.429-438
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    • 2017
  • For centuries, plants have been used for a wide variety of purposes, from treating infectious diseases to food preservation and perfume production. Presently, the increasing resistance of microorganisms to currently used antimicrobials in combination with the appearance of emerging diseases requires the urgent development of new, more effective drugs. Plants, due to the large biological and structural diversity of their components, constitute a unique and renewable source for the discovery of new antibacterial, antifungal, and antiparasitic compounds. In the present paper, the history, composition, and antimicrobial activities of the basil, oregano, and thyme essential oils are reviewed.

A New Class of Sol-Gel Transition Hydrogels for Macromolecular Delivery

  • Lee, Yu-Han;Park, Sung-Young;Chung, Hyun-Jung;Park, Tae-Gwan
    • Proceedings of the Polymer Society of Korea Conference
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    • 2006.10a
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    • pp.52-53
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    • 2006
  • A new series of PEO-PPO-PEO and PPO-PEO-PPO copolymers having several hydroxyl groups on the PPO chain segment were synthesized, further modified with various poly(lactic acid) PLA oligomeric chains to confer physical stability after thermo-gelation in the body fluid. Gel stability was endowed by either increasing hydrophobic interaction between PLA chains or inducing stereocomplex formation between enatiomeric isomers of PLA chains. Macromolecular drugs were incorporated within the gels and their release patterns were investigated using Pluronic F127 as a control.

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Nucleic Acid Aptamers: New Methods for Selection, Stabilization, and Application in Biomedical Science

  • Kong, Hoon Young;Byun, Jonghoe
    • Biomolecules & Therapeutics
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    • v.21 no.6
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    • pp.423-434
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    • 2013
  • The adoption of oligonucleotide aptamer is well on the rise, serving an ever increasing demand for versatility in biomedical field. Through the SELEX (Systematic Evolution of Ligands by EXponential enrichment), aptamer that can bind to specific target with high affinity and specificity can be obtained. Aptamers are single-stranded nucleic acid molecules that can fold into complex three-dimensional structures, forming binding pockets and clefts for the specific recognition and tight binding of any given molecular target. Recently, aptamers have attracted much attention because they not only have all of the advantages of antibodies, but also have unique merits such as thermal stability, ease of synthesis, reversibility, and little immunogenicity. The advent of novel technologies is revolutionizing aptamer applications. Aptamers can be easily modified by various chemical reactions to introduce functional groups and/or nucleotide extensions. They can also be conjugated to therapeutic molecules such as drugs, drug containing carriers, toxins, or photosensitizers. Here, we discuss new SELEX strategies and stabilization methods as well as applications in drug delivery and molecular imaging.

The Cytotoxic Action of New Ag-Porphyrin as a Potential Chemotherapeutic Agent

  • Nelli, Babayan;Artak, Tovmasyan;Ani, Gevorkyan;Gennadi, Gasparyan;Rouben, Aroutiounian
    • Korean Journal of Environmental Biology
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    • v.26 no.2
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    • pp.115-120
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    • 2008
  • Earlier we have described new water-soluble Ag- and Zn-derivatives of tetrachloride meso-tetra (4-N-oxiethylpyridyl) porphyrin (TOEtPyP) as potential anticancer drugs. In this work the effect of one of these metal porphyrins, TOEtPyP Ag, on the cell population kinetics was studied in vitro using morphological and biochemical techniques. The results suggested that TOEtPyP Ag action consisted in the simultaneous suppression of the cell growth and activation of the cell death. About 40% of the cells were shown to die via apoptotic pathway. So, the porphyrin studied may be attributed to inducers of both necrotic and apoptotic processes. The results obtained support our previous assertion that TOEtPyP Ag may be considered as a potential chemotherapeutic agent.

Electrochemical Determination of Ciprofloxacin Based on the Enhancement Effect of Sodium Dodecyl Benzene Sulfonate

  • Zhang, Shenghui;Wei, Shuang
    • Bulletin of the Korean Chemical Society
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    • v.28 no.4
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    • pp.543-546
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    • 2007
  • Herein, a new electrochemical method was described for the determination of ciprofloxacin based on the enhancement effect of an anionic surfactant: sodium dodecyl benzene sulfonate (SDBS). In pH 4.0 phosphate buffer and in the presence of 1.0 × 10-4 mol/L SDBS, ciprofloxacin yields a well-defined and sensitive oxidation peak at the carbon paste electrode (CPE). Compared with that in the absence of SDBS, the oxidation peak current of ciprofloxacin remarkably increases in the presence of SDBS. The experimental parameters, such as supporting electrolyte, concentration of SDBS, and accumulation time, were optimized for ciprofloxacin determination. The oxidation peak current is proportional to the concentration of ciprofloxacin over the range from 8.0 × 10-8 to 5.0 × 10-6 mol L-1. The detection limit is 2.0 × 10-8 mol L-1 after 2 min of accumulation. This new voltammetric method was successfully used to detect ciprofloxacin in drugs.

Using reverse docking to identify potential targets for ginsenosides

  • Park, Kichul;Cho, Art E.
    • Journal of Ginseng Research
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    • v.41 no.4
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    • pp.534-539
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    • 2017
  • Background: Ginsenosides are the main ingredients of ginseng, which, in traditional Eastern medicine, has been claimed to have therapeutic values for many diseases. In order to verify the effects of ginseng that have been empirically observed, we utilized the reverse docking method to screen for target proteins that are linked to specific diseases. Methods: We constructed a target protein database including 1,078 proteins associated with various kinds of diseases, based on the Potential Drug Target Database, with an added list of kinase proteins. We screened 26 kinds of ginsenosides of this target protein database using docking. Results: We found four potential target proteins for ginsenosides, based on docking scores. Implications of these "hit" targets are discussed. From this screening, we also found four targets linked to possible side effects and toxicities, based on docking scores. Conclusion: Our method and results can be helpful for finding new targets and developing new drugs from natural products.

A Study for New Hepatotropic Agents from Natural Resources -The Effect of Azalea Pollen on Aromatic Toxicants Induced Hepatotoxicity- (천연자원을 이용한 간기능 증진제 개발 연구-Aromatic toxicants 에 의해 유도된 간기능 장해에 미치는 진달래 화분립의 영향)

  • 윤수홍;박은주
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.21 no.4
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    • pp.341-347
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    • 1992
  • In search for new drugs and methods of pharmacotherapy of liver damage , the pollen extracts was administrated to the experimental animals and ivnestigated its biochemical effects in the serum and liver when aromatic hepatotoxicants-phenybutazone, aniline and benzo(a) pyrene-was administered. As the results are the pretretment of azalea pollen was prevented the leakage of asartate aminotransaminase (AST), alanine aminotransfease(ALT), alkaline phosphatase (ALP) activity and bilirubin level to serum and liver, except serum lactate dehydrogenase (LDH) activity.

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