• Title/Summary/Keyword: Analogs

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Synthesis of Tetrahydroquinoline linked-TZD Analogs as Novel Activators of PPARν

  • Lee, Soo-Mi;Lee, Sun-Mi;Raok Jeon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.118-118
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    • 2003
  • The use of PPARν (peroxisome proliferator activated receptor ν) activators in the treatment of type 2 diabetes is well established due to their ability to lower blood glucose and insulin levels and omprove insulin sensitivity. Thiazolidinedione analog is one of the potential antidiabetic drug that binds and activates PPARν selectively. In an effort to develop novel and effective antidiabetic thiazolidindione analogs, synthesis of tetrahydroquinoline and para-substituted benzene-linked thiazolidinedione analogs were carried out via coupling reaction of the hydrophobic segments with hydroxybenzylthiazolidinedione.

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Clinical application of gonadotropin-releasing hormone analogs in children and adolescents

  • Kim, Ho-Seong
    • Clinical and Experimental Pediatrics
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    • v.53 no.3
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    • pp.294-299
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    • 2010
  • Although the increasing incidence of central precocious puberty (CPP) in Korea has recently raised public concerns about health and growth problems, there are many areas of uncertainty regarding the pathogenesis, diagnosis, and management of CPP. In this paper, we review the definition of precocity, the assessment of CPP, and the hormonal abnormalities that support the diagnosis. In addition, we review the practical guidelines regarding the clinical use of gonadotropin-releasing hormone analogs in children with CPP. Indications for treatment, determination of dosage, monitoring during treatment, and discontinuation of therapy are discussed.

Synthesis of Quinolone Analogs of Isoflavonoids (퀴놀론 계열 이소플라보노이드의 합성)

  • 전라옥;이지혜;정상헌
    • YAKHAK HOEJI
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    • v.47 no.5
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    • pp.283-287
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    • 2003
  • Isoflavonoids are abundant in natural products and reported with many synthetic variations. However, relatively few quinolone analogs of isoflavonoids have been described. As part of our endeavor to pursue biologically active novel isoflavonoids, we report an efficient synthetic route for quinolone analogs of isoflavonoids. The key intermediate, 2'-aminochalcone 2 was obtained from substituted aniline and cyclized to afford quinolones 6, 8a, and 8b.

Polyoxygenated Flavone Analogs as Inhibitors of PGE2 Production

  • Kim, Jeong-Soo;Tran, Thanh-Dao;Chi, Yeon-Sook;Kim, Hyun-Pyo;Kim, Sang-Hee;Park, Hae-Il
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.245.1-245.1
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    • 2003
  • As part of our research to discover novel synthetic flavonoids which can be applied to chronic inflammation diseases, many structurally modified flavone analogs have been synthesized to obtain information concerning the relationships between structures and the anti-inflammatory activities. We previously reported that 7-methoxyflavone analogs generally exhibited strong inhibitory activities against cyclooxygenase-2 catalyzed prostaglandin production. (omitted)

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Synthesis of TZD Analogs as PPAR${\gamma}$ Specific Ligands

  • Lee, Soo-Mi;Lee, Sun-Mi;Jeon , Raok
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.186.2-186.2
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    • 2003
  • PPARs (peroxisome proliferator activated receptors) are member of nuclear hormone receptors superfamily. Activations of PPARs upon binding with ligands modulate glucose metabolite, differentiation of adipocyte, inflammation response, and so on. Thiazolidinedione analog is one of the potential antidiabetic drug that binds and activates PPAR selectively and enhances insulin sensitivity. In an effort to develop novel and effective antidiabetic thiazolidindione analogs, we have synthesized tetrahydroquinoline and para-substituted benzene-linked thiazolidinedione analogs by coupling reaction of the hydrophobic segments with hydroxybenzylthiazolidinedione.

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A Study on the Syntheses of Simple Analogs of Tetracycline and Flavonoid (Tetracycline과 Flavonoid의 간단한 유도체 합성에 관한 연구)

  • Kim, Hakwon
    • Journal of the Korean Chemical Society
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    • v.40 no.8
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    • pp.549-556
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    • 1996
  • This work describes studies aimed at the synthesis of simple analogs of antibiotic tetracycline(TC) and flavonoid. The synthesis of proposed analogs of tetracycline and flavonide has been accomplished from readily available compounds 9 and 15. The 1,3-cyclohexanedione derivative 9 was transformed to the benzoate derivative 12 followed by base-mediated intramolecular benzoylation to give the bicyclic TC-analog 13. The bicyclic TC-analog 25 and the flavonoid-analogs 26 and 27 have been prepared from the quinol derivative 15.

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2-Hydroxyquinoline and Its Structural Analogs Show Antidiabetic Effects against α-Amylase and α-Glucosidase

  • Lee, Hwa-Won;Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • v.58 no.1
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    • pp.1-3
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    • 2015
  • This study investigated the inhibitory activities of 2-hydroxyquinoline and its analogs against ${\alpha}$-glucosidase and ${\alpha}$-amylase. Based on the $IC_{50}$ values of 2-hydroxyquinoline analogs tested against ${\alpha}$-glucosidase and ${\alpha}$-amylase, 2-hydroxyquinoline had potent inhibitory activity (64.4 and $130.5{\mu}g/mL$, respectively), while 2-methyl-8-hydroxyquinoline showed weakly inhibitory activity (90.7 and $215.4{\mu}g/mL$, respectively). 2-Methylquinoline demonstrated no activity against ${\alpha}$-glucosidase and ${\alpha}$-amylase. In conclusion, 2-hydroxyquinoline analogs, with the existence of a methyl group and hydroxyl on quinoline, can be useful as a new diabetes treatment.

Design, Characterization, and Antimicrobial Activity of a Novel Antimicrobial Peptide Derived from Bovine Lactophoricin

  • Kim, Ji-Sun;Jeong, Ji-Ho;Kim, Yongae
    • Journal of Microbiology and Biotechnology
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    • v.27 no.4
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    • pp.759-767
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    • 2017
  • Lactophoricin (LPcin), which is a part of proteose peptone isolated from bovine milk, is a cationic amphipathic ${\alpha}-helical$ antimicrobial peptide. Its truncated variants and mutated analogs were designed and their antimicrobial activities were evaluated by using various assays, like broth dilution methods and disk diffusion methods as well as hemolysis assay. Three analogs, LPcin-C8 (LPcin-YK1), LPcin-T2&6W (LPcin-YK2), and LPcin-T2&6W-C8 (LPcin-YK3), which showed better antibiotic activities than LPcin, were selected. Their secondary structures were also characterized by using CD spectropolarimetry. These three analogs of LPcin could be used as an alternative source of powerful antibacterial agents.

Synthesis of Chrysin Analogs with a Heteroaryl Group and Evaluation for their Anti-inflammatory Activities (헤테로 고리를 갖는 크리신 유도체의 합성 및 항염증 작용에 대한 평가)

  • Che, Hai-Yan;Truong, Ngoc Tuyen;Kim, Hyun-Pyo;Park, Hae-Il
    • YAKHAK HOEJI
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    • v.55 no.6
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    • pp.462-465
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    • 2011
  • Chrysin analogs with 2-heteroaryl groups were synthesized and evaluated for their inhibitory activities against $PGE_2$ and NO production from LPS-induced RAW 264.7 cells. Chrysin analogs were synthesized from 2-hydroxy-4,6-dimethoxy-acetophenone and heteroaryl aldehydes in 3 steps. The tested chrysin analogs showed decreased inhibitory activity against $PGE_2$ and NO production than those of chrysin.