YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Synthesis of Angiotensin Converting Enzyme Inhibitors

안지오텐신 변환효소(變換酵素) 억제(抑制) 작용(作用) 물질(物質)의 합성(合成)

  • Lee, Hee-Joo (Department of Pharmacy, Duksung Woman's College) ;
  • Kim, Young-Sook (Department of Pharmacy, Duksung Woman's College) ;
  • Chang, Young (Department of Pharmacy, Duksung Woman's College) ;
  • Lee, Jong-Ran (Natural Products Research Institute, Seoul National Universtiy) ;
  • YunChoi, Hye-Sook (Natural Products Research Institute, Seoul National Universtiy)
  • 이희주 (덕성여자대학교 약학과) ;
  • 김영숙 (덕성여자대학교 약학과) ;
  • 장영 (덕성여자대학교 약학과) ;
  • 이종란 (서울대학교 생약연구소) ;
  • 윤혜숙 (서울대학교 생약연구소)
  • Published : 1984.12.30
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Abstract

Phenylurea, phenylthiourea, benzylcarbamate and toluenesulfonate of L-alanyl-L-proline(comp. $3{\sim}6$) were synthesized and their effects against angiotensin-converting enzyme (ACE) were tested. Comp. 3 showed only mild inhibitory activities against ACE while comp. $4{\sim}6$ were inert indicating that those functional groups were not suitable for interactions with ACE. Ortho-hydroxy- or ortho-carboxy-benzamide of proline (comp. 7) and phenylalanine (comp. 8 and 9) were also tested. Of the benzamides, ortho-hydroxy function was unsuitable to exert inhibitory activities against ACE. Ortho-carboxy group of 9 seemed to have mild interactions with active site of ACE possibly because of the shorter distance between the amide and ortho-carboxyl group of the compound than the corresponding two active sites of the enzyme.

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