| Autor: |
Haney WG, Brown RG, Isaacson EI, Delgado JN |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of pharmaceutical sciences [J Pharm Sci] 1977 Nov; Vol. 66 (11), pp. 1602-6. |
| DOI: |
10.1002/jps.2600661125 |
| Abstrakt: |
A series of isomeric (Z)-and (E)-oxime O-beta-dimethylaminoethyl ether methylhalide derivatives was synthesized, and their (Z)-and (E)-assignments were made on the basis of chemical and spectral data. The respective (Z)-and (E)-isomers were evaluated as anticholinergic agents on the rat ileum. The antimuscarinic potencies of the respective (Z)-and (E)-isomers were compared to determine the effect upon potency of this type of geometric isomerism. Three general structure-activity relationships and discernible among the synthesized compounds: (a) among oxime O-ethers derived from aromatic aldehydes, the higher potency consistently resides in the isomer where the aryl substituent is (E) to the ammonium ether substituent; (B) among oxime O-ethers derived from diaryl ketones, the (Z)-and (E)-isomers are approximately equipotent; and (c) oxime O-ethers derived from diaryl ketones are the most potent of the synthesized compounds. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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