ChemInform Abstract: Syntheses and Biological Evaluation of (.+-.)-3a-Phenyl Congeners of Physostigmine and Phenserine.

✍ Scribed by Xue-Feng Pei; Nigel H. Greig; Arnold Brossi

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 34 KB
• Volume: 30
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199923255

✦ Synopsis

Syntheses and Biological Evaluation of (±)-3a-Phenyl Congeners of Physostigmine and Phenserine.

-The title compounds (XIV), synthesized for the first time by a modification of the Julian total synthesis of physostigmine, are evaluated for their anticholinesterase action against human acetyl-and butyrylcholinesterase. The complete loss of cholinesterase activity demonstrates that sterically bulky substitution at the 3a position of the parent compounds is poorly tolerated. -(PEI, XUE-FENG; GREIG, NIGEL H.;