Isoquinuclidine-based expectorants. Synthesis and biological activities of N-alkoxybenzylisoquinuclidines

…, E Takizawa, Y Ohkura, C Fukai, T Tomiyama

Index: Yokota; Takizawa; Ohkura; Fukai; Tomiyama European Journal of Medicinal Chemistry, 1997 , vol. 32, # 5 p. 377 - 384

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Citation Number: 7

Abstract

N-Di-, trialkoxybenzylisoquinuclidines and related compounds were synthesized and evaluated for expectorant activities. Structure-activity relationship investigations in this series showed that both the trialkoxyphenyl ring and the basic nitrogen atom at the benzylic position were necessary for activity. N-Trialkoxybenzylisoquinuclidines 7a, 7c, 7d, 7f and 7g significantly increased bronchial secretion, and ethoxy derivative 7c showed the highest ...