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Isoquinuclidine-based expectorants. Synthesis and biological activities of N-alkoxybenzylisoquinuclidines by M Yokota; E Takizawa; Y Ohkura; C Fukai; T Tomiyama is a Chemistry article available to read on EtoBox.

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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 activity in these compounds. The n-propyloxy derivatives 7d and 7f also accelerated bronchoalveolar surfactant secretion with about two to four times more activity than ambroxol (7d and 7f: ED,, = 27.5 and 15.5 mg/kg po, respectively); however, compounds 7a, 7c and 7g were less active than ambroxol. Compounds 7d and 7f were selected for further examination. These compounds displayed antioxidant activity in vitro (7d and 7f; I(+ = 48.0 and 66.0 pM, respectively). Compound 7d also showed inhibition on bradykinin-or antigen-induced airway inflammation m guinea pigs. These findings suggest that compounds 7d and 7f are potent expectorants with antiinflammatory activity.

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Author

M Yokota; E Takizawa; Y Ohkura; C Fukai; T Tomiyama

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)

Published

1997

Language

EN

Field

Chemistry (Physical Sciences)