92132-77-9Relevant articles and documents
DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR
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Page/Page column 87, (2008/12/05)
The present invention provides a Compound of formula (I), wherein: R1 is a group selected from -CH2OH,-NH(CO)H; and R2 is a hydrogen atom; or R1 together with R2 form the group -NH-C(O)-CH=CH-, wherei
Synthesis of 3-substituted benzamides and 5-substituted isoquinolin-1(2H)-ones and preliminary evaluation as inhibitors of poly(ADP-ribose)polymerase (PARP)
Watson, Corrine Y.,Whish, William J. D.,Threadgill, Michael D.
, p. 721 - 734 (2007/10/03)
Inhibitors of poly(ADP-ribose)polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. 3-Substituted benzamides and 5-substituted isoquinolin-1-ones have been synthesised and evaluated for inhibition of PARP. Reduction of 3-(bromoacetyl)benzamide, followed by treatment with base, gave RS-3-oxiranylbenzamide. Reduction of 3-(hydroxyacetyl)benzonitrile with bakers' yeast gave the R-diol which was converted to R-3-(1,2-dihydroxyethyl)benzamide. Similar reduction of 3-(acetoxyacetyl)benzonitrile led towards the S-diol which was converted to its cyclic acetonide. E-2-(2,6-Dicyanophenyl)-N,N-dimethylethenamine was formed by condensation of 2,6-dicyanotoluene with dimethylformamide dimethyl acetal (DMFDMA); cyclisation under acidic conditions afforded 5-cyanoisoquinolin-1-one. Heck coupling of 5-iodoisoquinolin-1-one with propenoic acid formed E-3-(1-oxoisoquinolin-5-yl)propenoic acid. 3-Oxiranylbenzamide, 5-bromoisoquinolin-1-one and 5-iodoisoquinolin-1-one were among the most potent inhibitors of PARP activity in a preliminary screen in vitro. Copyright (C) 1998 Elsevier Science Ltd.
2-GUANYL-4-(SUBSTITUTED PHENYL) THIAZOLE DERIVATIVES
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, (2008/06/13)
Compounds of the formula: STR1 wherein R 1 is hydrogen, cyano or cyano(lower)alkyl;R 2 is hydrogen, cyano, carboxy, carbamoyl, guanyl, (lower)alkoxyimino, hydrazinocarbonyl, (lower) alkylaminoimino, STR2 with the proviso that one but never both of R