Chong Hyun Ryu

Publications (3)6.7 Total impact

• Article: Chain branching approach in structure modification of TRPV1 receptor antagonist MK056 and its analogs.

  Mijung Jang, Chong Hyun Ryu, Young-Ho Park, Hee-Doo Kim
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  ABSTRACT: A series of chain branched 1,3-dibenzylthiourea derivatives were designed, synthesized, and evaluated for their antagonist activity against TRPV1. The synthesized chain branched 1,3-dibenzylthioureas 9a-g were tested for their antagonist activities against TRPV1 by (45)Ca(2+)-influx assay using neonatal rat cultured spinal sensory neurons. Fluorinated ethyl-branched analog 9g showed the most potent antagonist activity with an IC(50) value of 0.41 μM, but all of the chain branched analogs were less potent than the parent compounds MK-056 and SC-0030, indicating that chain branching on the benzylic position of B-ring is detrimental to potency. Optimized receptor binding seems to be interfered by chain branching, and resulted in decrease in potency.
  Archives of Pharmacal Research 02/2012; 35(2):321-6. · 1.59 Impact Factor
• Source

  Available from: sookmyung.ac.kr

  Article: Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists.

  Chong Hyun Ryu, Mi Jung Jang, Jeong Wha Jung, Ju-Hyun Park, Hye Young Choi, Young-Ger Suh, Uhtaek Oh, Hyeung-Geun Park, Jeewoo Lee, Hyun-Joo Koh, Joo-Hyun Mo, Yung Hyup Joo, Young-Ho Park, Hee-Doo Kim
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  ABSTRACT: A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. (R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC(50) value of 0.05 microM which is 10-fold more potent than capsazepine.
  Bioorganic & Medicinal Chemistry Letters 05/2004; 14(7):1751-5. · 2.55 Impact Factor
• Source

  Available from: sookmyung.ac.kr

  Article: Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.

  JungWha Yoon, HyeYoung Choi, Hyun Joo Lee, Chong Hyun Ryu, Hyeung-geun Park, Young-ger Suh, Uhtaek Oh, Yeon Su Jeong, Jin Kyu Choi, Young-Ho Park, Hee-Doo Kim
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  ABSTRACT: A series of acyclic phenethylthiocarbamate derivatives have been synthesized, and their antagonist effect against vanilloid receptor tested. Chain branching led to a significant change in antagonist activity of the parent molecule. Ethyl-branched 1e showed a 6.3 microM of IC(50) value in 45Ca(2+)-influx assay.
  Bioorganic & Medicinal Chemistry Letters 06/2003; 13(9):1549-52. · 2.55 Impact Factor