116314-17-1Relevant articles and documents
PHARMACOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THE PREPARATION THEREOF AND COMPOSITIONS CONTAINING THE SAME
-
, (2008/06/13)
Pharmacologically active catechol derivatives of formula I I wherein R1 and R2 independently comprise hydrogen, alkyl, acyl, optionally substituted aroyl, lower alkylsulfonyl or alkylcabamoyl or taken together form a lower alkylidene or cycloalkylidene, X comprises an electronegative substituent such as halogen, nitro, cyano, lower alkylsulfonyl, sulfonamido, aldehyde, caboxyl or trifluoromethyl and R3 comprises hydrogen, halogen, hydroxy alkyl, amino, nitro, cyano, trifluoromethyl, lower alkylsulfonyl, sulfonamide, aldehyde, alkyl carbonyl, aralkylidene carbonyl or carboxyl or a group selected from wherein R4 comprises hydrogen, alkyl, cyano, carboxyl or acyl and R5 comprises hydrogen, cyano, carboxyl, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, optionally substituted aroyl or heteroaroyl, hydroxyalkyl or carboxyalkyl or R4 and R5 together form a five to seven membered substituted cycloalkanone ring; -(CO)n(CH2)m-COR wherein n is 0-1 and m is 0-7 and R comprises hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; wherein R8 and R9 independently comprise hydrogen or one of the following optionally substituted groups; alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, or together form an optionally substituted piperidyl group; -NH-CO-R10 wherein R10 comprises a substituted alkyl group
Synthesis of Some Novel Potent and Selective Catechol O-Methyltransferase Inhibitors
Baeckstroem, Reijo,Honkanen, Erkki,Pippuri, Aino,Kairisalo, Pekka,Pystynen, Jarmo,et al.
, p. 841 - 846 (2007/10/02)
A series of disubstituted catechol derivatives was synthesized and tested as potential COMT inhibitors.The most active compounds were more than 1000 times more potent (IC 50 = 3-6 nM) in vitro than the known COMT inhibitor, 3',4'-dihydroxy-2-methylpropiop
