• 제목/요약/키워드: Biological Synthesis

검색결과 1,240건 처리시간 0.027초

Design, Combinatorial Library Synthesis and Biological Evaluation of Nonpeptide Scaffold for Beta Turns

  • Im, I-Sak;Thomas R.Webb;Dona Chianelli;Kim, Yong-Chul
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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    • pp.91-91
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    • 2003
  • The beta-turn has been implicated as an important conformation for biological recognition of peptides or proteins. We adapted the concept of general Ca atom positioning from the cluster analysis and recombination of each ideal beta-turn conformation pattern by Garland and Dean (1. Computer-Aided Molecular Design, 1999, 13, 469) as one strategy of designing non-peptide beta-turn scaffolds. (omitted)

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밀리타린 유도체의 합성 및 생리활성 평가 (Synthesis and Biological Evaluation of Militarin Derivatives)

  • 차해연;윤덕효;김태웅;성기호;박해일
    • 약학회지
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    • 제56권6호
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    • pp.372-376
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    • 2012
  • Militarin was isolated from Cordyceps militaris, a caterpillar-grown traditional medicinal mushroom and reported to possess anticancer activities against several tumor cells. A number of militarin derivatives bearing different numbers of ethylene glycol unit were synthesized and evaluated for their biological activities related with anticancer and antiinflammatory effects. Among militarin derivatives tested, the compounds 2 and 5 exhibited anticancer and antiinflammatory activities.

Pulmonary Fibrosis caused by Asbestos Fibers in the Respiratory Airway

  • Jung, Ji-Woo;Kim, Eung-Sam
    • 대한의생명과학회지
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    • 제27권3호
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    • pp.111-120
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    • 2021
  • Asbestos products had been widely used until 2007 in Korea since the 1930s. A total ban on their production and applications has been imposed because of the toxic effect of asbestos fibers on the human health. The inhaled asbestos fibers increase reactive oxygen species and inflammatory reactions in the respiratory airway including the alveolar sac, resulting in DNA damages and secretion of several inflammatory cytokines or chemokines. These paracrine communications promote the proliferation of fibroblasts and the synthesis of collagen fibers, thereby depositing them into the extracellular matrix at the interstitial space of alveoli. The fibrotic tissue hindered the gas exchange in the alveolus. This reviews describes not only the cytotoxic effects of asbestos fibers with different physical or chemical characteristics but also the interaction of cells that make up the respiratory airway to understand the molecular or cellular mechanisms of asbestos fiber-induced toxicity. In addition, we propose a pulmonary toxicity research technique based on the mini-lung that can mimic human respiratory system as an alternative to overcome the limitations of the conventional risk assessment of asbestos fibers.

Synthesis and optimization of immunomodulating hydrogel for biomedical application

  • Muthuramalingam, Karthika;Park, Sanggyu;Cho, Moonjae
    • Journal of Applied Biological Chemistry
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    • 제61권4호
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    • pp.351-355
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    • 2018
  • Treatment towards wound healing, a complex and dynamic process, has been given a great deal of efforts in the last few decades. Focus has been imposed on developing wound dressings that meet the requirements for proper wound healing. In this study, hydrogel made from blends of poly (vinyl alcohol) and ${\beta}$-1,6-branched-${\beta}$-1,3-glucan (beta-glucan) were synthesized by modified solvent casting method for wound dressing application. Optimization of hydrogel composition and analysis of wound dressing parameters such as stability and fluid uptake capacity (in the presence of water, saline and different pH solutions) has been studied. The result indicated that the PVA/beta-glucan hydrogel hold its structural integrity even at alkaline pH (pH~9) and upholds fluids four times of its original weight. Thus, the developed hydrogel is expected to be a promising candidate as wound dressing.

Synthesis ot Brefeldin A Lactam Analogue

  • Paek, Seung-Mann;Seo, Seung-Yong;Jung, Jae-Kyung;Han, Young-Taek;Seo, Young-Ger
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.245.2-245.2
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    • 2003
  • (+)-Brefeldin A (1) has been, since its isolation1 and structural elucidation2 many years ago, one of the most attractive targets for synthetic chemists due to its wide range of biological activities and well-functionalized macrolide structure. Its biological mode of action has been disclosed by a number of important discoveries. Especially the ability of brefeldin A to induce DNA fragmentation associated with apoptosis in cancer cells has stimulated a great deal of recent interest in its preclinical development as an anticancer agent. (omitted)

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Synthesis and Biological Studies of A Novel Series of Catechol Ether Type Derivatives as Potential Phosphodiesterase(PDE) IV Inhibitors

  • Lee, Jae-Mok;Lee, Koun-Ho;Kim, Jong-Hoon;Song, Seog-Beom;Chun, Hyung-Ok;Yeon, Kyu-Jeong;Kwon, Soon-Ji
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.348.1-348.1
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    • 2002
  • We synthesized various catechol ether type derivatives substituted by the hydrazine moiety and evaluated for their ability to inhibit PDE Ⅳ (Phosphodiesterase Ⅳ). These new compounds were synthesized from 4-methoxy-3-hydroxy benzaldehyde through 5 or 7 steps. Some of them have similar or more potent inhibitory activity against PDE Ⅳ than known PDE Ⅳ inhibitor. Ariflo (SB 207499). Structure activity relationship (SAR) and biological studies of described compounds will be discussed in detail. (omitted)

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Synthesis and Evaluation of Biological activities of New Imine Derivatives of Apicidin

  • Jin, Cheng-Hua;Kim, Hyung-Kyo;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.253.2-253.2
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    • 2002
  • Apicidin. a natural product HDAC inhibitor. is recently isolated from Fusarium sp. at Merk Research Laboratories, induces therapeutic applications as a broad spectrum antiprotozoal agent to muti-drug resistant malaria and a potential antitumor agent. The biological activity of apicidin appears to be apicocomplexan HDAC at low nanomolar concentrations. (omitted)

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Synthesis of dimeric fluorescent TSPO ligand for detection of glioma

  • Tien Tan Bui;Hee-Kwon Kim
    • 대한방사성의약품학회지
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    • 제7권1호
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    • pp.56-65
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    • 2021
  • TSPO, an 18-kDa translocator protein, is a peripheral-type benzodiazepine receptor that has been associated to a variety of biological activities such as apoptosis, steroidogenesis, and cell proliferation. Because TSPO overexpression has been found in various forms of cancer, it has recently become one of the most appealing biological targets for cancer therapies and detection. In order to create new optical imaging agents for improved diagnostics, we synthesized a novel dimeric fluorescent TSPO ligand based on PRB28 structure and SCy5.5. Following the preparation of the novel TSPO ligand, in vivo and ex vivo imaging tests were performed to examine the tumor uptake characteristics of the fluorescent TSPO ligand in a glioma animal model, and it was found that novel TSPO ligand was accumulated in glioma. These results suggested that novel dimeric fluorescent TSPO ligand will be applied to detect glioma.

A Novel Synthesis of Heterocyclic Compounds Containing Coumarin Moiety of Potential Antimicrobial Activity

  • El-Fattah, M. E. Abd
    • Archives of Pharmacal Research
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    • 제21권6호
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    • pp.723-728
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    • 1998
  • The chemical behaviours of 4-methyl-2-oxo-2H-benzopyran-7-yl oxoacetyl hydrazine (2) towards some different reagents such as anhydride compounds, aromatic aldehydes, carb on disulphide, and nitrous acid yielded the corresponding pathalazine derivatives (3, 4, 5), hydrazone derivative (6), 1,3,4-oxadiazole derivative (7, 8, 9) and acid azide (10) respectively. Treatmen of 10 with absolute alcohols, amines and ethyl amino acid ester gave the corresponding carbamate derivative (11), substituted urea derivative (12) and ethyl substituted alkyl acetate (13) respectively. The biological activity of some synthesized compounds was evaluated.

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Synthesis of Praziquantel Derivatives and Their In Vitro Activity Against Adult Clonorchis sinensis

  • Kim, Choong-Sup;Min, Duk-Young
    • Archives of Pharmacal Research
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    • 제21권6호
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    • pp.744-748
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    • 1998
  • Several praziquantel derivatives have been prepared by the acylation of compound 5, and examined on their biological activity in vitro agninst adult clonorchis sinensis collected from rabbits infected with metacercariae which was isolated from Pseudorasbora parva, a second intermediate host, captured in Nakdong river in Korea.

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