STUDIES ON BENZOHETEROCYCLIC DERIVATIVES (IX) STRUCTURE-ACTIVITY RELATIONSHIPS OF 5 OR 7 SUBSTITUTED 2-(3'-ALKOXYPROPYLAMINOMETHYL) 2.3-DIHYDROBENZOFU RAN ANALOGUES ON ANALGESIC, SPINAL REFLEX DEPRESSING AND ADRENERGIC α-BLOCKING EFFECTS

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It has been reported that benzodioxan derivatives, e.q. 2-alkoxymethyl 1.4-benzodioxan (1) and 2-(3'-methoxypropylaminomethyl) 1.4-benzodioxan (Quiloflex) (2, 3) have adrenergic α-blocking, sedative and spinal reflex depressing properties.<BR> Through our intensive pharmacological screening of benzofuran derivatives which possess quite similar chemical structure with 1.4-benzodioxan ring, we found that most of these compounds revealed the similar pharmacological properties to the benzodioxan derivatives (4). It is very interesting that 2-(3'-alkoxypropylaminomethyl) 2.3-dihydrobenzofuran analogues which showed relatively potent skeletal muscle relaxant, sedative, analgesic and adrenergic α-blocking actions, were very similar to chemical structure of Quiloflex.<BR> The purpose of our present work was to investigate the structure-activity relationships of 5 or 7 substituted 2-(3'-alkoxypropylaminomethyl) 2.3-dihydrobenzofuran analogues, particulary of the substituents and their position on the ring concerning analgesic, spinal reflex depressing and adrenergic α-blocking effects.
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