. alpha.-Adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1, 4-benzodioxans as selective presynaptic. alpha. 2-adrenoreceptor antagonists

MR Stillings, CB Chapleo, RCM Butler…

Index: Stillings, Michael R.; Chapleo, Christopher B.; Butler, Richard C. M.; Davis, J. Alfred; England, C. David; et al. Journal of Medicinal Chemistry, 1985 , vol. 28, # 8 p. 1054 - 1062

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Citation Number: 64

Abstract

The synthesis and pharmacological activity of a series of 2-substituted derivatives of the selective a,-adrenoreceptor antagonist idazoxan (RX 781094) is described. Substitution in this position by alkyl, alkenyl, cycloalkenyl, and alkoxy groups in many cases gives compounds whose potencies and selectivities are significantly greater than those of the parent compound.