Structure-Activity Relationships of Imperialine Derivatives and their Anticholinergic Activity

null Atta-ur-Rahman; M. Iqbal Choudhary; Afgan Farooq; Shazia Anjum; Jesse Baumgold; Bilge Sener

doi:10.1055/s-2006-957397

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Planta Med 1998; 64(2): 172-174
DOI: 10.1055/s-2006-957397

Letters

Letter
© Georg Thieme Verlag Stuttgart · New York

Structure-Activity Relationships of Imperialine Derivatives and their Anticholinergic Activity

Atta-ur-Rahman , M. Iqbal Choudhary, Afgan Farooq, Shazia Anjum, Jesse Baumgold, Bilge Sener

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Publikationsdatum:
04. Januar 2007 (online)

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Abstract

In order to check the structure-activity relationship and prepare more potent derivatives of imperialine with anticholinergic activity, imperialinol, 3β-acetoxyimperialine, 3β-propionoxyimperialine, and 3β-butyroxyimperialine were prepared. Compounds 4 and 5 displayed better anticholinergic activity against muscarinic receptors of the heart and brain than imperialine. The decrease in activity in 2 showed the importance of the 6-keto functionality in imparting the anticholinergic activity.