• Title/Summary/Keyword: Medicinal chemistry

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

  • Rhee, Chung K.;Kim, Jong-Hoon;Suh, Byung-Chul;Xiang, Myung-Xik;Youn, Yong-Sik;Bang, Won-Young;Kim, Eui-Kyung;Shin, Jae-Kyu;Lee, Youn-Ha
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.202-207
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    • 1999
  • New series of catechol ether type derivatives 5, 6 have been synthesized and applied to biological tests. Even though it is ap preliminary data, some of our target molecules show the promising result against PDE IV inhibition. SAR and biological studies with studies with synthetic compounds will be discussed in detail.

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Design, Synthesis, And In Vitro Evaluation of Apio Analogs of Neplanocin A and Aristeromycin

  • Lee, Jeong-Ah;Yoo, Byul-Nae;Moon, Hyung-Ryong;Lee, Kang-Man;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.241.1-241.1
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    • 2003
  • Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand, neplanocin A and aristeromycin are the representative of the carbocyclic nucleosides and have been recognized as potent inhibitors of S-adenosylhomocysteine hydrolase. Based on these findings. it was of great interest to design apio analogues of neplanocin A and aristeromycin. (omitted)

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Antimicrobial activity of Mongolian medicinal plants

  • Gonchig, Enkhmaa;Erdenebat, Sarnaizul;Togtoo, Ouyntsetseg;Bataa, Sukhkhuu;Gendaram, Odontuya;Kim, Young-Sup;Ryu, Shi-Yong
    • Natural Product Sciences
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    • v.14 no.1
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    • pp.32-36
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    • 2008
  • The antimicrobial activity of seventy five ethanol extracts obtained from 67 different kinds of plant species of the Mongolian flora were evaluated by means of the disc diffusion method against five species of microorganisms, Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, Micrococcus luteus and Pseudomonas aeruginosa. Among the plant extracts examined, 34 kinds of extracts demonstrated significant antibacterial activity against one or more species of microorganisms, respectively. Especially, the root extract of Paeonia anomala, the whole herb extract of Myricaria alopecuroides, the whole herb extract of comarum zalesovianum, the whole herb extract of Agrimonia pilosa and some other plant extracts demonstrated a particularly potent antimicrobial activity. The ethylacetate fractions obtained from the whole herb extract of Myricaria alopecuroides and from those of Sedum aizoon, Paeonia anomala, Sedum hybridum and Dasiphora fruticosa exhibited a particularly potent antibacterial activity especially against Staphylococcus aureus and Micrococcus luteus.

Isoflavanones from the Stem of Cassia siamea and Their Anti-tobacco Mosaic Virus Activities

  • Hu, Qiu-Fen;Niu, De-Yun;Zhou, Bin;Ye, Yan-Qing;Du, Gang;Meng, Chun-Yang;Gao, Xue-Mei
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.3013-3016
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    • 2013
  • Two new isoflavanones, (3R) 7,2',4'-trihydroxy-3'-methoxy-5-methoxycarbonyl-isoflavanone (1) and (3R) 7,2'-dihydroxy-3',4'-dimethoxy-5-methoxycarbonyl-isoflavanone (2), together with six known isoflavanones (3-8), were isolated from the stems of Cassia siamea. The structure of 1-8 was elucidated by spectroscopic methods including extensive 1D- and 2D-NMR techniques. Compounds 1, 2, 5-8 were evaluated for their anti-tobacco mosaic virus (Anti-TMV) activity. The results showed that compounds 1 and 6 showed potential anti-TMV activity with inhibition rates of 24.6% and 26.9%, respectively. Compounds 2, 5, 7, 8 also showed anti-TMV activity with inhibition rates in the range of 11.8-18.6%.

Phenolic Compounds Obtained from Stems of Couepia ulei with the Potential to Induce Quinone Reductase

  • Jang, Dae-Sik;Park, Eun-Jung;Kang, Young-Hwa;Vigo, Jose-Schunke;James-G.Graham;Fernando-Cabieses;Harry-H.S.Fong;John-M.Pezzuto;A.Douglas-Kinghorn
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.169-172
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    • 2004
  • Activity-guided fractionation of the EtOAc-soluble extract of the stems of Couepia ulei, using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells led to the isolation of two active compounds, a new natural product, erythro-2,3-bis(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-o1 (1), and a known compound, evofolin-B (2), along with five inactive compounds all of known structure, viz., betulinic acid, oleanolic acid, pomolic acid, ($\pm$)-syringaresinol, and ursolic acid. These isolates were identified by analysis of physical and spectral data. Compounds 1 and 2 exhibited QR inducing activity, with observed CD (concentration required to double induction) values of 16.7 and 16.4 $\mu\textrm{M}$, respectively.

Synthesis and Antibacterial Activity of 1β-Methyl-2-[5-(α,β-disubstituted ethyl)pyrrolidin-3-ylthio]carbapenem Derivatives. Part II

  • Kim, Jin-Woong;Park, Hyeong Beom;Chung, Bong Young;Lee, Jong Baek;Cho, Jung-Hyuck;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.27 no.8
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    • pp.1164-1170
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    • 2006
  • The synthesis of a new series of 1$\beta$-methylcarbapenems having 5-($\alpha,\beta$-disubstituted ethyl)pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. A particular compound (VIh) having $\alpha$-hydroxy-$\beta$-piperazinylethyl substituted moiety showed the most potent activity.

Screening of the Tyrosinase Inhibitors from Marine Algae and Medicinal Plants (해조류 및 생약의 Tyrosinase 억제활성 검색)

  • Lee, Bong-Ho;Kang, Key-Jung;Lee, Eun-Seog;Lee, Nam-Ho;Choi, Byoung-Wook
    • Korean Journal of Pharmacognosy
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    • v.29 no.3
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    • pp.237-242
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    • 1998
  • We have tested tyrosinase inhibitory activity on the methanol extracts of 23 species marine algae and 23 species traditional medicinal plant. Among them, four medicinal plants, Ephedra sinica, Atractylodes japonica, Pinnelia ternata, and Citrus aurantium, showed strong inhibition potency over 90% at concentration of 0.33 mg/mL. Also, two marine algae, Enteromorpha compressa and Sargassum singgildianum showed mild inhibition potency over 50% at concentration of 0.33 mg/mL.

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