Synthesis of N,N',N"-Trisubstituted Thiourea Derivatives and their Antagonistic Effect on the Vanilloid Receptor

  • Park, Hyeung-Geun (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Park, Mi-Kyung (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Choi, Ji-Yeon (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Choi, Sea-Hoon (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Lee, Ji-Hye (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Suh, Young-Ger (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Cho, Ha-Won (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Oh, Uh-Taek (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University) ;
  • Lee, Jee-Woo (Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University)
  • Published : 2003.04.01

Abstract

Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1- [3-(4'-hydroxy-3'-methoxy-phenyl)-propyl] -1,3-diphenethyl-thiourea (81, IC$\sub$50/= 0,32 $\mu\textrm{m}$), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC$\sub$50/= 0,65 $\mu\textrm{m}$) against the vanilloid receptor in a Ca$\^$2+/ -influx assay.

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