Structure-activity relationships of imperialine derivatives and their anticholinergic activity


Atta-ur-Rahman A., Choudhary M., Farooq A., Anjum S., Baumgold J., Sener B.

PLANTA MEDICA, vol.64, no.2, pp.172-174, 1998 (Journal Indexed in SCI) identifier

  • Publication Type: Article / Letter
  • Volume: 64 Issue: 2
  • Publication Date: 1998
  • Title of Journal : PLANTA MEDICA
  • Page Numbers: pp.172-174

Abstract

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.