Structure-activity relationships of imperialine derivatives and their anticholinergic activity.
In order to check the structure-activity relationship and prepare more potent derivatives of imperialine with anticholinergic activity, imperialinol (2), 3 beta-acetoxyimperialine (3), 3 beta-propionoxyimperialine (4), and 3 beta-butyroxyimperialine (5) were prepared. Compounds 4 and 5 displayed better anticholinergic activity against muscarinic receptors of the heart and brain than imperialine (1). The decrease in activity in 2 showed the importance of the 6-keto functionality in imparting the anticholinergic activity.
Atta-ur-Rahman
Choudhary
M I
MI
Farooq
A
A
Anjum
S
S
Baumgold
J
J
Sener
B
B
D000470:Alkaloids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D002595:Cevanes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D018680:Cholinergic Antagonists / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects / Q000502:physiology*; D006325:Heart Atria; D006624:Hippocampus / Q000187:drug effects / Q000502:physiology*; D066298:In Vitro Techniques; D015394:Molecular Structure; D010946:Plants, Medicinal; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
D000470:Alkaloids; D002595:Cevanes; D018680:Cholinergic Antagonists; D011976:Receptors, Muscarinic; C047331:peiminine