50534-33-3Relevant articles and documents
Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases
Jakubowska, Anna,Kulig, Katarzyna,Natalia, Guzior,Malawska, Barbara
experimental part, p. 449 - 455 (2012/08/27)
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 μM]) was determined for compound (6c) which is 1-(3-chloro)benzylpiperidine amide of 1H-indole-5-carboxylic acid.
Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors
Dener, Jeffrey M,Wang, Vivian R,Rice, Kenneth D,Gangloff, Anthony R,Kuo, Elaine Y.-L,Newcomb, William S,Putnam, Daun,Wong, Martin
, p. 2325 - 2330 (2007/10/03)
Truncation of potent and selective dibasic inhibitors afforded monocharged inhibitors of human mast-cell tryptase. Using two classes of analogues as lead structures, several monocharged derivatives were identified with Ki values ranging from 0.
Inhibitors of microsomal triglyceride transfer protein and method
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, (2008/06/13)
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure STR1 wherein R1 to R7, Q, X and Y are as defined herein.