SAR studies of capsazepinoid bronchodilators. Part 2: Chlorination and catechol replacement in the A-ring

M Berglund, MF Dalence-Guzmán, S Skogvall…

Index: Berglund, Magnus; Dalence-Guzman, Maria F.; Skogvall, Staffan; Sterner, Olov Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 5 p. 2513 - 2528

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Citation Number: 15

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 ...