SAR studies of capsazepinoid bronchodilators. Part 1: The importance of the catechol moiety and aspects of the B-ring structure
M Berglund, S Skogvall, O Sterner - Bioorganic & medicinal chemistry, 2008 - Elsevier
M Berglund, S Skogvall, O Sterner
Bioorganic & medicinal chemistry, 2008•ElsevierCapsazepine 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 …
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 …
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.
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