183428-91-3Relevant academic research and scientific papers
AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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Paragraph 0368-0369, (2015/03/16)
The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions cont
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABAA receptor agonists
Petersen, Jette G.,S?rensen, Troels,Damgaard, Maria,Nielsen, Birgitte,Jensen, Anders A.,Balle, Thomas,Bergmann, Rikke,Fr?lund, Bente
, p. 404 - 416 (2014/08/05)
A series of 6-aminonicotinic acid analogues have been synthesized and pharmacologically characterized at native and selected recombinant GABA A receptors. 6-Aminonicotinic acid (3) as well as 2- and 4-alkylated analogues (9-11, 14-16) display low to mid-micromolar GABAAR binding affinities to native GABAA receptors (Ki 1.1-24 μM). The tetrahydropyridine analogue of 3 (22) shows low-nanomolar affinity (K i 0.044 μM) and equipotency as an agonist to GABA itself as well as the standard GABAA agonist isoguvacine. Cavities surrounding the core of the GABA binding pocket were predicted by molecular interaction field calculations and docking studies in a α1β 2γ2 GABAA receptor homology model, and were confirmed by affinities of substituted analogues of 3. The tight steric requirements observed for the remarkably few GABAAR agonists reported to date is challenged by our findings. New openings for agonist design are proposed which potentially could facilitate the exploration of different pharmacological profiles within the GABAAR area.
AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF
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Page/Page column 83, (2013/04/10)
The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions cont
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8,-tetrahydro-imidazo[1,2,-a]pyridines as antiprotozoal agents
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Page/Page column 20, (2008/06/13)
A method for treating a microbial infection, including an infection from a protozoan pathogen, such as Trypanosoma brucei rhodesiense and Plasmodium falciparum, in a subject in need thereof by administering to the subject an effective amount of a dication
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1, 2-a]pyridines as antiprotozoal agents
Ismail, Mohamed A.,Brun, Reto,Wenzler, Tanja,Tanious, Farial A.,Wilson, W. David,Boykin, David W.
, p. 3658 - 3664 (2007/10/03)
2-[5-(4-Amidinophenyl)-furan-2-yl]-5,6,7,8-tetrahydro-imidazo [1,2-a]pyridine-6-carboxamidine acetate salt (7) was synthesized from 2-[5-(4-cyanophenyl)-furan-2-yl]-imidazo[1,2-a]pyridine-6-carbonitrile (4a), through the bis-O-acetoxyamidoxime followed by
PYRIDINONE THROMBIN INHIBITORS
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: STR1 for example: STR2
