Conformational effects on the activity of drugs. 7. Synthesis and pharmacological properties of 2-(p-nitrophenyl)-substituted morpholines.
A series of 1-(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-isopropyl-substituted compounds. In agreement with the previously obtained results, the weak alpha-adrenergic-stimulating activity and the potentiating effect on the responses to norepinephrine found in the open-chain compounds persist in their corresponding semirigid cyclic analogues. The results are discussed in the light of common knowledge of the structure-activity relationships of alpha-adrenergic drugs.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000818:Animals; D004347:Drug Interactions; D066298:In Vitro Techniques; D008297:Male; D008968:Molecular Conformation; D009025:Morpholines / Q000138:chemical synthesis / Q000494:pharmacology*; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects
D000317:Adrenergic alpha-Antagonists; D009025:Morpholines; D009638:Norepinephrine