Abstract
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 paper concerns the chlorination of the A-ring as well as the replacement of the catechol with bioisosteric groups. It is revealed that chlorination of the A-ring has a profound effect on activity. Moreover, di-chlorination of the 6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline structure results in a 10-fold increase in potency compared to capsazepine.
Original language | English |
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Pages (from-to) | 2513-2528 |
Journal | Bioorganic & Medicinal Chemistry |
Volume | 16 |
Issue number | 5 |
DOIs | |
Publication status | Published - 2008 |
Bibliographical note
The information about affiliations in this record was updated in December 2015.The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)
Subject classification (UKÄ)
- Organic Chemistry