Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase
โ 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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โฆ 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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## Abstract Benzeneโ1,2โ, 1,3โ, and 1,4โdiโ__N__โsubstituted carbamates (1โ15) are synthesized as the conformationally constrained inhibitors of acetylcholinesterase and mimic __gauche__, __eclipsed__, and __anti__โconformations of acetylcholine, respectively. All carbamates 1โ15 are characterized
## Abstract For Abstract see ChemInform Abstract in Full Text.