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Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase

โœ Scribed by David M. Fink; M.G. Palermo; Gina M. Bores; Francis P. Huger; Barbara E. Kurys; Michael C. Merriman; Gordon E. Olsen; Wayne Petko; Gerard J. O'Malley


Book ID
103983333
Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
346 KB
Volume
6
Category
Article
ISSN
0960-894X

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โœฆ Synopsis


A series of irrfino 1,2,3,4-tetrahydrocyclopent [b]indole caltmn~tes was prepared and evaluated as dual acetyichollm, stem~ (ACHE) and monoan-fine oxida~ (MAO) inhibitors. Halogen substitution ortho to the cartmn-me functionality in the eight position resulted in a significant increase in binding affinity for both AChE and MAO-A.

Alzhekner's Disease (AD) is a neurodegenerative disorder that is the rmjor cause of dementia amongst the elderly.

This disease affects about 2% of the population over the age of 65, and up to 50% of the population over the age of 85. l As general heakh care improves and the proportion of elderly people in the population increases, the number of AD patients is anticipated to increase dramatically. 2


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Benzene-1,2-, 1,3-, and 1,4-di-N-substit
โœ Ming-Cheng Lin; Mei-Ting Hwang; Han-Ging Chang; Chung-Sheng Lin; Gialih Lin ๐Ÿ“‚ Article ๐Ÿ“… 2007 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 214 KB

## Abstract Benzeneโ€1,2โ€, 1,3โ€, and 1,4โ€diโ€__N__โ€substituted carbamates (1โ€“15) are synthesized as the conformationally constrained inhibitors of acetylcholinesterase and mimic __gauche__, __eclipsed__, and __anti__โ€conformations of acetylcholine, respectively. All carbamates 1โ€“15 are characterized