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SAR studies of capsazepinoid bronchodilators. Part 1: The importance of the catechol moiety and aspects of the B-ring structure.

Author:
  • Maria Dalence
  • Magnus Berglund
  • Staffan Skogvall
  • Olov Sterner
Publishing year: 2008
Language: English
Pages: 2499-2512
Publication/Series: Bioorganic & Medicinal Chemistry
Volume: 16
Issue: 5
Document type: Journal article
Publisher: Elsevier

Abstract english

Capsazepine as well as its derivatives and analogues are general inhibitors of constriction of human small airways. From a systematic variation of the capsazepine structure, divided into four regions, SARs were established. This part concerns the catechol moiety of the A-ring as well as the 2,3,4,5-tetrahydro-1H-2-azepine moiety (the B-ring) of capsazepine. It is revealed that a conformational constrain (as a fused ring) is important and that compounds with a six-membered B-ring (as a 1,2,3,4-tetrahydroisoquinoline) in general are more potent than the corresponding isoindoline, 2,3,4,5-tetrahydro-1H-2-benzazepine and 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.

Keywords

  • Organic Chemistry

Other

Published
  • ISSN: 0968-0896
Olov Sterner
E-mail: olov.sterner [at] science.lu.se

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