• Title/Summary/Keyword: amino acid derivatives

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Synthesis and Surface Active Properties of Long Chain N-Acyl Collagen Derivatives (고급 지방산 N-아실 콜라겐 유도체의 합성 및 계면활성)

  • Kim, T.Y.;Nam, K.D.;Nam, S.I.;Ahn, J.H.;Lee, J.H.
    • Journal of the Korean Applied Science and Technology
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    • v.10 no.2
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    • pp.81-90
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    • 1993
  • The Surfactants composed of acylated aterocollagen which is produced by the acylation of the side chain amino radicals of aterocollagen with an aliphatic acid having 12 to 18 carbon atoms will be discussed in this study. This condensation is done at moderate reaction temperature (<$25^{\circ}C$) in aqueous alkaline solution. The products of this reaction were identified by UV/VIS spectroscopy and infrared spectroscopy. For these compounds, surface active properties and physical properties including isoelectric point, Krafft point, surface tension, critical micelle concentration(cmc), foaming power, viscosity behaviour, water holding capacity, skin irritation and emulsifying power were measured respectively. The experimental results received that the products have a good emulsifying power, excellent water holding capacity while having low skin irritation. Thus, these derivatives will be expected to be used as an emulsifying agent for O/W type cosmetic emulsion.

Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives

  • Nevade, Sidram A.;Lokapure, Sachin G.;Kalyane, Navanath V.
    • Journal of the Korean Chemical Society
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    • v.57 no.6
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    • pp.755-760
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    • 2013
  • The present study is synthesis of derivatives of N'-(4-amino-5-sulfanyl-4H-1,2,4-triazole-3-yl)-2-(1H-benzimidazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted by disc diffusion method. Compound $2MB_1$, $2MB_3$, $2MB_5$ inhibit the appreciable microbial growth while rest of the compound possess the moderate activities. Anti-inflammatory activity tested by reduces local edema induced in the rat paw by injection of phlogestic agent. Compound $2MB_1$, $2MB_8$, $2MB_5$, $2MB_3$ and $2MB_6$ exhibit satisfying anti-inflammatory activity while analgesic activity conducted by acetic acid induced writhing effect in mice while compound $2MB_1$, $2MB_4$ and $2MB_7$ having the good analgesic activity. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and mass spectral data.

Chelators for 68Ga radiopharmaceuticals

  • Seelam, Sudhakara Reddy;Lee, Yun-Sang;Jeong, Jae Min
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.2 no.1
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    • pp.22-36
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    • 2016
  • $^{68}Ga$ is a promising radionuclide for positron emission tomography (PET). It is a generator-produced ($^{68}Ge/^{68}Ga$-generator) radionuclide with a half-life of 68 min. The employment of $^{68}Ga$ for basic research and clinical applications is growing exponentially. Bifunctional chelators (BFCs) that can be efficiently radiolabeled with $^{68}Ga$ to yield complexes with good in vivo stability are needed. Given the practical advantages of $^{68}Ga$ in PET applications, gallium complexes are gaining increasing attention in biomedical imaging. However, new $^{68}Ga$-labeled radiopharmaceuticals that can replace $^{18}F$-labeled agents like [$^{18}F$]fluorodeoxyglucose (FDG) are needed. The majority of $^{68}Ga$-labeled derivatives currently in use consist of peptide agents, but the development of other agents, such as amino acid or nitroimidazole derivatives and glycosylated human serum albumin, is being actively pursued in many laboratories. Thus, the availability of new $^{68}Ga$-labeled radiopharmaceuticals with high impact is expected in the near future. Here, we present an overview of the different new classes of chelators for application in molecular imaging using $^{68}Ga$ PET.

Nitrogen Compounds of Korea Ginseng and their Physiological Significance

  • Park, Hoon;Cho, Byung-Goo;Lee, Mee-Kyoung
    • Proceedings of the Ginseng society Conference
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    • 1990.06a
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    • pp.175-189
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    • 1990
  • Nitrogen compounds of Panax ginseng and their biological activities in plant and animal were reviewed. Major nitrogen compounds found in P. ginseng are free amino acids. Water solilble proteins, indouble proteins and peptides. Minor nitrogen compounds are dencichine. Glycolyroteins, amines, alkaloides, methoxy or alkyl pyrazine derivatives, free nucleosides and nucleic acid bases. 4-methyl-i-thiazoltethanol and pyroglutamic acid the contents of total nitrogen and protein in root Increased until 13 years old which was the highest age tinder investigation. Soluble protein content increased with the root weight and was higher in xylem pith than cortex-epidermis indicating the close relation with root growth. Arginine, which covered 58% of total free amino acids, may serve as storage nitrogen. Arginine seems to be changed into proline in rhizome. threonine in stem and again threonine and arginine in leaf. The greater the root weight the higher the polyamine stimulated Polyamine stimlllated the growth of root callus. Physiological roles of other minor nitrogen compounds are unknown although content is relatively high ((1.if) 6.w). Biochemical and pharmacological activities of some nitrogen compounds for animal were more investigated than physiological role there plant itself. Radiation and U.V protective function (heat stable protein). insulin-like activity in lipogenesis and livolysis (adenosine and pyroglutamic acid), depression of blood sugar content (glycopevtide). htmostatic and nellrotoxic activity (dencichine) and, sedative and hypnotic activity (4-methyl-i-thiazoleethanol) are reported. Heat stable protein increased with root age. The traditional quality criteria appear to be well in accordance with biological activities of nitrogen compounds. Chemical studies of nitrogen compounds seem relatively rare, probably due to difficulty of isolation, subsequently the investigations of biological activities are little.

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Acrylic Polymer Composition Suitable for Ion Delivery and Selective Detection of Proton, and Hydroxyl and Cu(II) Ions (이온 이동에 적합한 아크릴고분자 박막의 조성과 수소이온, 수산화이온, 구리이온의 선택적 검출)

  • Lee, Dahye;Woo, Heejung;Do, Jung Yun
    • Polymer(Korea)
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    • v.38 no.6
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    • pp.801-808
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    • 2014
  • Ion diffusion and chemical binding to acrylic polymer were investigated in a solid film. The composition of acrylic monomers containing amino group and carboxylic acid was adjusted for rapid ion migration in the film. p-Methylred (PMR) and phenolphthalein derivatives were optically sensitive to the concentration of proton and hydroxyl anion, respectively and verified the ion migration through the film layers. A rapid proton migration was observed in the film of a high amino content. On the other hand, $OH^-$ migration occurred rapidly in a high content of carboxylic acid group. The proton migration occurred through the internal layer as well as surface layer of a film and was reversible during 50 repetition examination. Copper(II) ion migration was examined with a Rhodamine-containing polymer film. The light absorption and emission spectra of a Rhodamine-Cu complex showed the key contribution of carboxylic acid group to the Cu(II) migration in a film.

Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity (Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성)

  • Baek Du-Jong;Ahn Jong-Woong;Lee Chongock
    • YAKHAK HOEJI
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    • v.49 no.1
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    • pp.68-73
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    • 2005
  • Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

Mechanism Studies of Substituted Triazol-1-yl-pyrimidine Derivatives Inhibition on Mycobacterium tuberculosis Acetohydroxyacid Synthase

  • Chien, Pham Ngoc;Jung, In-Pil;Reddy, Katta Venugopal;Yoon, Moon-Young
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4074-4078
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    • 2012
  • The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

Thermotropic Liquid Crystalline Behavior of Aliphatic Acid Esters of N,O-Hydroxypropyl Chitosans (N,O-히드록시프로필 키토산 지방산 에스터들의 열방성 액정 거동)

  • Kim, Hyo Gap;Jung, Seung Yong;Ma, Yung Dae
    • Polymer(Korea)
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    • v.37 no.3
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    • pp.276-287
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    • 2013
  • Two kinds of N,O-hydroxypropyl chitosans (HPCTOs) with degree of substitution (DS) and molar substitution (MS) ranging from 2.15 to 2.39 and 2.9 to 4.1, respectively, and five kinds of aliphatic acid esters of HPCTOs (HPCTOAms, m=0,2,4,7,9, the number of methylene units in aliphatic substituent) based on the HPCTOs were synthesized, and the thermotropic liquid crystalline properties of the derivatives were investigated. All the derivatives formed enantiotropic cholesteric phases whose optical pitches (${\lambda}_m$'s) increased with increasing temperature. However, the glass and clearing temperatures, the magnitude of ${\lambda}_m$ of the mesophase at the same temperature, and the temperature dependence of ${\lambda}_m$ of the investigated derivatives highly depended on MS and m. The thermotropic mesophase properties of HPCTOAms were significantly different from those reported for the aliphatic acid esters of hydroxypropyl celluloses. The results indicate that the secondary amino group in the C-2 position plays an important role in the thermal stabilization and temperature dependence of ${\lambda}_m$ of the cholesteric mesophase.

Analysis of Components in the Different Parts of Ailanthus altissima (가죽나무(Ailanthus altissima)의 부위별 성분 분석)

  • Lee, Yang-Suk
    • Food Science and Preservation
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    • v.15 no.2
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    • pp.261-268
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    • 2008
  • This study was carried out to analyze the components of the roots, stems, and leaves of Ailanthus altissima to obtain basic data on the nutritional and functional materials developed a functional food with A. altissima. Among the general components, crude ash (9.20%) in the roots, crude protein (11.36%) in leaves, and carbohydrates (81.74%) in stems were higher than other parts. The content of soluble protein was the highest 9,839.52 mg% in leaves. Reducing sugar and free sugar in roots were 1,813.94 mg% 1,140.20 mg% and 1,670.98 mg% 1,190.42 mg% in leaves, respectively. The contents of free amino acid (2,018.58 mg%) in roots were higher than leaves (1,070.88 mg%) and stems (427.55 mg%). Especially arginine (1,446.63 mg%) and aspartic acid (252.82 mg%) in roots were the highest. Total content of amino acid derivatives were 780.70 mg% in leaves and 430.95 mg% in roots. Especially, taurine was 61.68 mg% in roots. In the results of mineral analysis, the contents of Ca, K and Mg which account for 83% to 98% of mineral contents, were high in all parts. The polyphenol compounds in leaves and water extract of leaves were 821.58 mg% and 8,040.35 mg%. And contents of flavonoids were 2,501.67 mg% in leaves and 13,592.20 mg% in ethanol extract of leaves, respectively.

Interaction of flavins and some alcohols on the molecular level

  • Yu, Byung-Sul;Chung, Hyun-Ho;Lee, Sang-Jong;Kim, Yang-Bae;Kim, Chong-Kook
    • Archives of Pharmacal Research
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    • v.4 no.1
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    • pp.43-51
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    • 1981
  • The effect of some alcohols on the riboflavin derivatives in non-polar solvent was studied by various spectroscopic method in order to support the view point that alcohol may directly interect with the isoalloxazine moiety of FAD, the coenzyme of D-amino-acid oxidase. The most possible association complex between alcohol and riboflavin is the 1:1 complex through the 2-C carbonyl function of the isollaxazine ring nd the hydroxyl proton of alcohol. It is appeared that methanol has a larger association constant than any other alcohols, and the association constant decreases with the carbon number increases and being bulkier in the alkyl group of alcohols.

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