50534-33-3Relevant academic research and scientific papers
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.
SUBSTITUTED OXIMES AND HYDRAZONES AS NEUROKININ ANTAGONISTS
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Page 10, (2010/02/08)
Compound represented by structural formula (I) or a pharmaceutical acceptable salt thereof, wherein a is 0-3; b, d and e are 0-2; R is H, alkyl, F or -OR; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, -C(O)-, -O-, -NR-, -S(O)e-, -N(R)C(O)-, -C(O)N(R)-, -OC(O)NR-, -OC(=S)NR-, -N(R)C(=S)O-, -S(O)2N(R)-, -N(R)S(O)2-, -N(R)C(O)O-, -OC(O)- or -N(R)C(O)NR-; or d is 0 and X is a bond or -NR-; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, napthyl or heteroaryl; R is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R is R or -OR, R, R, R and R are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
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.
Coordination control of intramolecular electron transfer in boronate-bridged zinc porphyrin - Diimide molecules
Shiratori,Ohno,Nozaki,Yamazaki,Nishimura,Osuka
, p. 8747 - 8757 (2007/10/03)
Three sets of dyads, in which a zinc-porphyrin (ZP) electron donor is connected to an aromatic diimide electron accepter, either pyromellitimide (PI) or naphthalene-1,8:4,5-tetracarboxylic acid diimide (NI), via a boronate-ester bridge, a piperidine bridge, and a 1,3-dioxolane bridge, respectively, were prepared for the purpose of control of intramolecular electron transfer (ET) by acid-base reactions at the connecting bridge. Boronate - ester bridge is a Lewis acidic site and confers a chance to regulate intramolecular ET reaction upon base coordination. This has been demonstrated by suppression of photoinduced ET from ZP to PI or NI in highly electron-pair donating solvents or upon addition of a fluoride anion. To extend this strategy to control of ET-path selectivity, we prepared triad 18, which consists of a ZP donor bearing NI and PI accepters at similar distances through a boronate - ester bridge and an acetal bridge, respectively. Photoexcitation of 18 in a free form led to intramolecular ET from 1ZP* preferentially to NI, but the ET path was completely switched toward PI in F--coordinated form without a serious drop in the rate, constituting a novel ET-switching molecular system.
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.
Phthalimidopiperidines and anti-convulsant compositions thereof
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, (2008/06/13)
Phthalimidopiperidines of the formula STR1 are described where R1 is hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, phenyl(lower)alkyl, pyridyl(lower)alkyl, furyl(lower)alkyl or thienyl(lower)alkyl and R2 and R3 are hydrogen or various substituents. The compounds are useful pharmaceutically, particularly as anti-convulsants, and also in some cases as anti-arrhythmic agents and anti-inflammatory agents, and in some cases useful as intermediates for the preparation of 4-aminoquinoline derivatives having anti-malarial activity.
