• 제목/요약/키워드: pharmaceutical activity

검색결과 4,232건 처리시간 0.031초

Monoamine Oxidase Inhibitors from the Whole Plant of Cayratia japonica

  • Han, Xiang-Hua;Hong, Seong-Su;Park, Seon-Soon;Huh, Jae-Doo;Lee, Kyong-Soon;Lee, Myung-Koo;Hwang, Bang-Yeon;Ro, Jai-Seup
    • 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.256.1-256.1
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    • 2003
  • As a part of our ongoing research to discover novel monamine oxidase (MAO) inhibitors of plant origin, we found that a MeOH extract from the whole plant of Cayratia japonica (Vitaceae) strongly inhibited the MAO activity in mouse brain. The EtOAc-soluble fraction was. therefore, subjected to the bioactivity-guided fractionations to isolate the active compounds. (omitted)

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Bioactive Fabaceous Saponins and Structure-Activity Relationship

  • Kinjo, Junei;Nohara, Toshihiro
    • 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.143-146
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    • 2002
  • Saponins are glycosidic compounds present in many edible and inedible plants. Structurally, they are composed of a lipid-soluble aglycone consisting of either a sterol or, more commonly, a triterpenoid and water-soluble sugar residues differing in type and amount of sugars [1]. Because of their amphiphilic nature, they are highly surface-active. Their biological activity is closely related to the chemical structures that determine the polarity, hydrophobicith and acidity of compounds [1]. (omitted)

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Synthesis and Antibacterial Activity of New Cephalosporins with Lactonyloxyimino Moiety

  • Suh, Kwee-Hyun;Park, Joo-Woong
    • Archives of Pharmacal Research
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    • 제17권2호
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    • pp.87-92
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    • 1994
  • A series of $7-{2-(aminothiazol-4-yl)-2-Z-({\gamma}-lacton-3-yl)oxyiminoactamido}$ cephalosporins with various substituents at the 30position in cephem nucleus in cephem nucleus were synthesized and evaluated microbiologically. The tested compounds showed potent activities but were somewhat less active than cefotaxime or cefixime against a wide variety of Gram-positive and Gram-negative bacteria.

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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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    • 제22권1호
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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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Pharmacophore Modelling, Quantitative Structure Activity Relationship (QSAR) and Docking Studies of Pyrimidine Analogs as Potential Calcium Channel Blockers

  • Choudhari, Prafulla B.;Bhatia, Manish S.;Jadhav, Swapnil D.
    • 대한화학회지
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    • 제57권1호
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    • pp.99-103
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    • 2013
  • The present communication deals with the Pharmacophore modeling, 3D QSAR and docking analysis on series of Pyrimidine derivatives as potential calcium channel blockers. The computational studies showed hydrogen bond donor, hydrogen bond acceptor, and hydrophobic group are important features for calcium channel blocking activity. These studies showed that Pyrimidine scaffold can be utilized for designing of novel calcium channels blockers for CVS disorders.

Synthesis and Antitubercular Activity of 6-Chloro (Unsubstituted)- 2-Methoxy-9-Substituted Acridine Derivatives

  • Aly, Enayat I.;Abadi, Ashraf H.
    • Archives of Pharmacal Research
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    • 제27권7호
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    • pp.713-719
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    • 2004
  • Several analogues of the general formulae 2-methoxy-9-substituted acridine and 6-chloro-2-methoxy-9-substituted acridine were synthesized and evaluated in vitro at 6.25 $\mu\textrm{g}$/mL against M. tuberculosis $H_{37}Rv$. Compounds 15 and 17 showed potential antitubercular activity with 100% inhibition to the virulent mycobacterium.

Structure-Activity Relationship of 2-Substituted Hydroquinones as Tyrosinase Inhibitors for Topical Delivery

  • Lee, Yeon-Jung;Yoon, Sung-Il;Kim, Dae-Duk;Kim, Jung-Sun
    • Journal of Pharmaceutical Investigation
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    • 제36권2호
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    • pp.103-107
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    • 2006
  • In order to develop hydroquinone analogues for topical delivery, a structure-activity relationship study has been performed. A series of 2-substituted hydroquinones were tested for their ability to inhibit mushroom tyrosinase, alter melanin release and exert cytotoxicity in B6-F10 melanocytes. The electronic property of the 2-substituents did not affect the tyrosinase inhibition nor melanocyte toxicity. However, lipophilicity did affect to some degree the tyrosinase inhibition. The discrepancy in the structure-activity relationship may be due to the poor aqueous solubility of select analogues. Compounds with steric bulk at the 2-position seems to be less soluble, not enabling the analogue to interact effectively with the tyrosinase enzyme. Among the analogues tested, 2-isopropyl hydroquinone seems to be the most promising candidate for topical delivery, being the least toxic analogue with moderate melanin release inhibition.

Synthesis and Antinociceptive Activity of (5-Chloro-2(3H)-Benzoxazolon-3-yl) Propanamide Derivatives

  • Onkol, Tijen;Sahin, M.Fethi;Yidirim, Engin;Erol, Kevser;Ito, Shigero
    • Archives of Pharmacal Research
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    • 제27권11호
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    • pp.1086-1092
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    • 2004
  • In this study, (5-chloro-2(3H)-benzoxazolon-3-yl)propanamide derivatives were synthesized. The chemical structures of the compounds were elucidated by their IR and $^1H-NMR$ spectral data and microanalysis. The compounds were tested for anti nociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods. The varying levels of anti nociceptive activity of the compounds were compared with those of dipyrone and aspirin. Among these compounds, compound 5e, 5g, and 5h have been found to be significantly more active than the others and the standards in all the tests.