SAR studies of capsazepinoid bronchodilators 3: The thiourea part (coupling region) and the 2-(4-chlorophenyl) ethyl moiety (C-region)

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. 2529 - 2540

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Citation Number: 12

Abstract

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 (C-region), it was revealed that capsazepinoids with a thiourea or an amide link between the B-ring and the C-region in ...