Document Detail


Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases.
MedLine Citation:
PMID:  22594259     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
A series of novel N-benzyl substituted amides of 1H-indole-5-carboxylic acid were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The target compounds (6b-6e) displayed moderate potency to inhibit BuChE. One of the compounds tested, i.e., 1-benzylpiperidine amide of 1H-indole-5-carboxylic acid (6a) was a weak, non-selective inhibitor for both enzymes. The highest inhibitory activity towards BuChE (30.06% [10 microM]) was determined for compound (6c) which is 1-(3-chloro)benzylpiperidine amide of 1H-indole-5-carboxylic acid.
Authors:
Anna Jakubowska; Katarzyna Kulig; Natalia Guzior; Barbara Malawska
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Acta poloniae pharmaceutica     Volume:  69     ISSN:  0001-6837     ISO Abbreviation:  Acta Pol Pharm     Publication Date:    2012 May-Jun
Date Detail:
Created Date:  2012-05-18     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985167R     Medline TA:  Acta Pol Pharm     Country:  Poland    
Other Details:
Languages:  eng     Pagination:  449-55     Citation Subset:  IM    
Affiliation:
Department of Physicochemical Drug Analysis, Chair of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9 St., 30-688 Kraków, Poland.
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