141287-63-0Relevant academic research and scientific papers
Synthesis and preliminary structure-activity relationships of 1-[(3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate (P10358), a novel acetylcholinesterase inhibitor
Martin, Lawrence L.,Davis, Larry,Klein, Joseph T.,Nemoto, Peter,Olsen, Gordon E.,Bores, Gina M.,Camacho, Fernando,Petko, Wayne W.,Rush, Douglas K.,Selk, David,Smith, Craig P.,Vargas, Hugo M.,Winslow, James T.,Effland, Richard C.,Fink, David M.
, p. 157 - 162 (2007/10/03)
A series of carbamate analogs of besipirdine (HP 749) was synthesized as potential agents with enhanced cholinomimetic properties for the treatment of Alzheimer's disease. Compound 5a (P10358, 1-[(3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate) emerged as a potent, reversible acetylcholinesterase inhibitor that significantly enhanced performance on oral or parenteral administration in learning and memory paradigms.
1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates
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, (2008/06/13)
There are disclosed various compounds of the formula below, STR1 where n is 0 or 1; X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy; Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy; R1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl; R2 is hydrogen, loweralkyl, formyl or cyano; R3 is hydrogen or loweralkyl; R4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR3 R4 taken together constitutes STR2 R5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
