Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 5, Pages 2529-2540Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.11.056
Keywords
capsazepine; coupling region; thiourea; C-region; 2-(phenyl)ethyl; SAR; bronchodilator; small human airways; asthma; COPD
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Certain derivatives and analogues of capsazepine are potent in vitro inhibitors of bronchoconstriction in human small airways. During an investigation of the dependency of the potency on the structural features of the capsazepinoids in the thiourea moiety (coupling region) and the 2-(4-chlorophenyl)ethyl moiety (Gregion), it was revealed that capsazepinoids with a thiourea or an amide link between the B-ring and the Gregion in general have a good bronchorelaxing activity, while urea is a less attractive choice. Further, it was shown that 1,2,3,4-tetrahydroisoquinolines with a 2-(phenyl)ethyl derivative as the C-region are considerably more potent than those with an octyl group, while 2,3,4,5-tetrahydro-1H-2-benzazepines were found to be more insensitive to the nature of the Gregion. (C) 2007 Elsevier Ltd. All rights reserved.
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