• Title/Summary/Keyword: inhibitory compounds

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Synthesis and COX-2 Inhibitory Activity of Benzothiazine-3-carboxamide Derivatives (Benzothiazine-3-carboxamide 유도체의 합성과 COX-2 저해효과)

  • 신혜순;최희전;권순경
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.375-380
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    • 2002
  • In this study, newly designed COX-2 inhibitors, synthetic derivatives of benzothiazine-3-carboxamide, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. 7-Bromo-1,2-benzoisothiazine derivatives were obtained from 4-bromotoluene over the chlorosulfonation, amination and oxidation. And benzothiazine ring was synthesized through Gabriel-Colmann rearrangement reaction. To evaluate inhibitory effect of COX-2, synthetic derivatives of benzothiazine-3-carboxamide were tested with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Some of the synthesized lead compounds have potentially shown the structure-activity relationship for selectivity of COX-2 inhibition activity.

Synthesis and Biological Activity of Annulated Pyrazoles as Selective COX-2 Inhibitors. I.

  • Kim, Hyun-Hee;Park, Jae-Gyu;Moon, Tae-Chul;Chang, Hyun-Wook;Jahng, Yurng-Dong
    • Archives of Pharmacal Research
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    • v.22 no.4
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    • pp.372-379
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    • 1999
  • A series of disubstituted 4,5-polymethylenepyrazoles were synthesized and evaluated their inhibitory activities against COX-2. Some compounds showed strong (0.3 nM) inhibitory activity on COX-2 and were found somewhat selective (up to 16) on COX-2 over COX-1.

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Inhibitory Constituents against HIV-1 Protease from Agastache rugosa

  • Min, Byung-Sun;Masao-Hattori;Lee, Hyeong-Kyu;Kim, Young-Ho
    • Archives of Pharmacal Research
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    • v.22 no.1
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    • pp.75-77
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    • 1999
  • Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with $IC_{50}$ values of 360 and $87{\mu}M$, respectively.

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Phenolic Compounds from Barks of Pinus densiflora siebold et Zuccarini and Their NO Production Inhibitory Activities.

  • Kwon, Young-Min;Yeom, Seung-Hwan;Kim, Min-Ki;Lee, Jae-Hee;Lee, Min-Won
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.374.1-374.1
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    • 2002
  • The barks o.f Pinus densiflara representative Pinus species graws in Korea, have been used for oriental traditional medicine as the remedies for rheumatitis. hemorrhage and cancer. Water soluble fraction of 80% acetone extracts from the barks af Pinus densiflera (PDB) showed nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$. LPS stimulated RAW 264.7 cell. (omitted)

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Antiallergic Activities of Daidzein, a Metabolite of Puerarin and Daidzin Produced by Human Intestinal Microflora

  • Park, Eun-Kyung;Choo, Min-Kyung;Kim, Dong-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.225.1-225.1
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    • 2003
  • To evaluate the antiallergic activities of puerarin and daidzin from the rhizome of Pueraria lobata, in vitro and in vivo inhibitory activities of these compounds and their metabolite daidzein were measured. Daidzein exhibited potent inhibitory activity on the B-hexosaminidase release induced by DNP-HSA and potently inhibited the PCA reaction in mice. (omitted)

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Virus-cell fusion inhibitory compounds from Ailanthus altissima Swingle

  • Lee, Hyang-Hee;Chang, Young-Su;Moon, Young-Hee;Woo, Eun-Rhan
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.264.1-264.1
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    • 2003
  • In order to search for the anti-HIV agents from natural products, Eighty MeOH extracts of medicinal plants were applied to a syncytia formation inhibition assay which is based on the interaction between the HIV-1 envelope glycoprotein gp120/gp41 and the cellular membrane protein CD4 of T lymphocytes. Among them, Ailanthus altissima showed a potent virus-cell fusion inhibitory activity. (omitted)

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Tyrosinase Inhibitory Activity of the EtOH Extracts and Their Fractions of Crude Drugs

  • Li, Xun;Park, Sung-Uk;Kim, Youn-Chul
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.267.2-267.2
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    • 2003
  • Melanin biosynthesis inhibitors are useful not only for the materials used in cosmetics as skin-whitening agents but also for the remedy of hyperpigmentation. In order to find the new skin-whitening compounds from the natural products. screening of tyrosinase inhibitory activity in vitro has been carried out. The EtOH extracts of two hundred crude drugs were performed at the concentration of 500 $\mu\textrm{g}$/$m\ell$. (omitted)

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Antioxidative Activities of Phenolic Compounds Isolated from Inonotus obliquus (차가버섯으로부터 분리한 페놀성 화합물의 항산화효과)

  • Kim, Hyoung-Ja;Jin, Chang-Bae;Lee, Yong-Sup
    • Korean Journal of Pharmacognosy
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    • v.38 no.2 s.149
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    • pp.164-169
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    • 2007
  • ln our continued search for biologically active compounds from traditional medicine, we found that ethyl acetate fraction from Inonotus obliquus showed potent antioxidant activities on three different cell-free bioassay systems. Bioassay-directed chromatographic fractionation of the ethyl acetate fraction from Inonotus obliquus afforded four phenolic compounds, 4-(3,4-dihydroxyphenyl)-(E)-3-buten-2-one (1) , 3,4-dihydroxybenzaldehyde (2), protocatechuic acid (3) and caffeic acid (4) along with three sterols such as lanosterol (5), ergosterol peroxide (6) and 9,11-dehydroergosterol peroxide (7). Among isolates, phenolic compounds (1-4) were assessed for antioxidant activities. Almost phenolic compounds showed potent DPPH and superoxide anion radicals scavenging and lipid peroxidation inhibitory activities indicating that these phenolic compounds contribute to the antioxidative activities of I. obliquus. Compounds 2-3 and 7 were isolated for the first time from this plant.