• Title/Summary/Keyword: Analogues

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Synthesis and Antiviral Evaluation of 1'-Branched-5'-Norcarbocyclic Adenosine Phosphonic Acid Analogues

  • Oh, Chang-Hyun;Yoo, Kyung-Ho;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.31 no.9
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    • pp.2473-2478
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    • 2010
  • Novel 1'-methyl-5'-norcarbocyclic adenosine phosphonic acid analogues were synthesized using an acyclic stereoselective route from commercially available 3,3-diethoxy-propan-1-ol 4. The synthesized nucleoside phosphonate 19 and phosphonic acid 21 were subjected to antiviral screening against various viruses.

FUZZY EQUIVALENCE RELATIONS AND FUZZY FUNCTIONS

  • Lee, Keon-Chang
    • International Journal of Fuzzy Logic and Intelligent Systems
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    • v.9 no.1
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    • pp.20-29
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    • 2009
  • In this paper, by using the definition of fuzzy equivalence relations introduced by Dib and Youssef, we obtain fuzzy analogues of many results concerning ordinary equivalence relations. Moreover, we investigate fuzzy analogues of many results concerning relationships between ordinary equivalence relations and ordinary functions. In particular, we obtain the fuzzy-canonical decomposition of a fuzzy function.

Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects (Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색)

  • 신혜순;이희주
    • Biomolecules & Therapeutics
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    • v.3 no.3
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    • pp.217-222
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    • 1995
  • Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

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Synthesis of Novel Carboacyclic Nucleosides with Vinyl Bromide Moiety as Open-chain Analogues of Neplanocin A

  • Choi, Myung-Hee;Kim, Hee-Doo
    • Archives of Pharmacal Research
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    • v.26 no.12
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    • pp.990-996
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    • 2003
  • A novel carboacyclic nucleoside analogue, 9-[2-bromo-4-hydroxy-3-hydroxymethyl-2-butenyl] adenine, and its derivatives were designed and synthesized as open-chain analogues of neplanocin A. The syntheses were accomplished via the coupling of adenine or pyrimidine bases to the key intermediate allylic bromide 7. The bromide 7 was prepared from epichlorohydrin in a seven step process in a 54% overall yield. The synthesized compounds were evaluated for their antiviral activity against the polio virus, HSV and HIV.

Synthesis of 3'(β)-C-methyl Carbodine Analogues as Potential Anti-HCV Agents

  • Li, Hua;Baik, Young-Chan;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1147-1151
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    • 2009
  • The synthetic route of novel 3′-C-methyl carbodine analogue is described. The construction of tertiary alcohol at 3′- position of carbodine analogues was successfully made via sequential [3,3]-sigmatropic rearrangement, ring-closing metathesis (RCM) and stereoselective dihydroxylation reactions starting from ethyl glycolate.

Understanding the RNA-Specificity of HCV RdRp: Implications for Anti-HCV Drug Discovery

  • Kim, Jin-young;Chong, You-hoon
    • Bulletin of the Korean Chemical Society
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    • v.27 no.1
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    • pp.59-64
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    • 2006
  • Unlike other viral polymerases, HCV RNA-dependent RNA polymerase (RdRp) has not been successfully inhibited by nucleoside analogues presumably due to its strong substrate specificity for RNA. Thus, in order to understand the RNA-specificity of HCV RdRp, the structural characteristics of the active site was investigated. The hereto unknown 2-OH binding pocket at the active site of RdRp provides invaluable implication for the development of novel anti-HCV nucleoside analogues.

Studies of Tertiary Structures of Mastoparan B and Alanine Analogues by NMR Spectroscopy

  • Kyeunghee Yu;Kang, Shin-Won;Park, Nam-Gyu;Kim, Yangmee
    • Proceedings of the Korean Biophysical Society Conference
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    • 1999.06a
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    • pp.33-33
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    • 1999
  • Mastoparan B (MP-B), an antimicrobial cationic tetradecapeptide amide isolated from the venom of the hornet Vespa basalis, is an amphiphilic ${\alpha}$-helical peptide. In order to study the relationship between the structure and biological activity, we used the three analogues by replacing amino acids with alanine (4LysAla: 4MP-B, 12-LYsAla: 12MP-B, 9TrpAla: 9Mp-B).(omitted)

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Malyngolide Analogues. Synthesis of (${\pm}$)-Dehydromalyngolide and (${\pm}$)-Isomalyngolide

  • Sunggak Kim;Youn Chul Kim;Chang Yong Hong
    • Bulletin of the Korean Chemical Society
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    • v.5 no.3
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    • pp.97-100
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    • 1984
  • Two novel malyngolide analogues, (${\pm}$)-dehydromalyngolide and (${\pm}$)-isomalyngolide, of (-)-malyngolide antibiotic have been synthesized by application of our previously developed synthetic sequence for the synthesis of (${\pm}$)-malyngolide. Dehydromalyngolide was synthesized from the known lactone (4) in a 55 % overall yield in six steps, while isomalyngolide was synthesized from the readily available keto ester (11) in a 56 % overall yield in four steps.