CONFORMATIONAL EFFECTS ON THE ACTIVITY OF DRUGS .7. SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF 2-(PARA-NITROPHENYL)-SUBSTITUTED MORPHOLINES

A series of l-(p-nitrophenyl)-2-aminoethanol derivatives and their morpholine analogues have been synthesized and pharmacologically investigated in order to confirm some pharmacological observations made with the N-iso-propyl-substituted compounds. In agreement with the previously obtained results, the weak α-adrenergic-stimulating activity and the potentiating effect on the responses to norepinephrine found in the open-chain compoundspersist in their corresponding semirigid cyclic analogues. The results are discussed in the light of common knowledge of the structure-activity relationships of α-adrenergic drugs. © 1979, American Chemical Society. All rights reserved.