• Title/Summary/Keyword: Biological Synthesis

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Synthesis and Biological Effects of Some 5-Heterocyclicmethyl-2'-deoxyurdines

  • Kwak, In-Young;Ryu, Eung K.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.306-309
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    • 1990
  • The synthesis of 5-hyterocyclimethyl-2'-deoxyuridines (4a-f) has been accomplished by displacement reaction of 5-(bromomethyl)-3', 5'-di-O-acetyl-2'-deoxyuridine with heterocyclic compounds, followed by removal of acetyl protecting group with methanolic ammonia. The compoudns synthesized were evaluated the inhibitory effects on L1210 cell probiferation and antiviral activities against Herpes simplex virus type 1 (HSV-1) None of the compounds exhibited sufficient biological activities.

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Molecular Modeling, Synthesis, and Screening of New Bacterial Quorum-sensing Antagonists

  • Kim, Cheol-Jin;Kim, Jae-Eun;Park, Hyung-Yeon;Mclean, Robert J.C.;Kim, Chan-Kyung;Jeon, Jong-Ho;Yi, Song-Se;Kim, Young-Gyu;Lee, Yoon-Sik;Yoon, Je-Yong
    • Journal of Microbiology and Biotechnology
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    • v.17 no.10
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    • pp.1598-1606
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    • 2007
  • A new series comprising 7 analogs of N-(sulfanyl ethanoyl)-L-HSL derivatives, 2 analogs of N-(fluoroalkanoyl)-$_L$-HSL derivatives, N-(fluorosulfonyl)-L-HSL, and 2,2-dimethyl butanoyl HSL were synthesized using a solid-phase organic synthesis method. Each of the 11 synthesized compounds was analyzed using NMR and mass spectroscopies, and molecular modeling studies of the 11 ligands were performed using SYBYL packages. Thereafter, a bacterial test was designed to identify their quorum-sensing inhibition activity and antifouling efficacy. Most of the synthesized compounds were found to be effective as quorum-sensing antagonists, where antagonist screening revealed that 10 among the 11 synthesized ligands were able to antagonize the quorum sensing of A. tumefaciens.

Synthesis and biological activity of spirobenzopyranone derivative as analogs of thelepin, isolated from the marine annelid Thelepus setosus (항균성물질 thelepin의 spirobenzopyranone 유도체의 합성과 생물활성)

  • Ko, Byoung-Seob;Oritani, Takayuki
    • Applied Biological Chemistry
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    • v.35 no.6
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    • pp.470-474
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    • 1992
  • For the further development of thelepin analog as antibiotic agents, we undertook the synthesis of spirobenzopyranone derivative ${\underline{5}}$ as thelepin analog by oxidative phenol coupling. The spirobenzopyranone analog ${\underline{5}}$ showed high activity against Bacillus subtilis (IFO 3108) in $5\;{\mu}g/disc$.

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