The catalytic subunit of adenosine cyclic 3',5'-monophosphate dependent protein kinase from bovine skeletal muscle was rapidly inactivated by o-phthalaldehyde at 25 degrees C (pH 7.3). The reaction followed pseudo-first-order kinetics, and the second-order rate constant was 1.1 X 10(2) M-1 s-1. Absorbance and fluorescence spectroscopic data were consistent with the formation of an isoindole der...

o-Phthalaldehyde has been recently shown to be a useful reagent for chemical modification of cyclic nucleotide dependent protein kinases, hexokinase, and fructose-1,6-bisphosphatase. It reacts covalently with closely spaced (approximately 3 A) sulfhydryl and epsilon-amino functions of cysteine and lysine residues, respectively, of these enzymes to yield fluorescent isoindole derivatives. We hav...

A series of 17 long-chain arylpiperazines containing bulky, complex imide systems (5,8-dimethyl-3b,9-epoxy-(3a,4,5,6,7,8,9,9a)-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetra-hydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT1A, 5-HT2A and dopamine D2 receptors. Most of the new compounds showed mod...

gepirone, ipsapirone, tandospirone and others) are 1arylpiperazine derivatives with a high affinity to the 5HT1A receptor (1-3). Therefore, they are widely used in the treatment of psychotic and neurotic disorders. This paper is a continuation of our research in the field of 4aryl/heteroaryl piperazinylalkyl derivatives (4, 5) of 1(1H-pyrrole-1-ylmethyl)-10-oxa-azatricyclo[5.2.1.0] dec-8-ene-3,...

This study evaluates culture filtrate, rich in cellobiose dehydrogenase and laccases, of Termitomyces sp. OE 147, in decolouration and degradation of Reactive blue (RB) 21. About 35% decolouration was achieved at low volumes of the culture supernatant without addition of external redox mediators. An optimized dye to culture fluid ratio (75 ppm: 0.1 ml) at a pH of 4-5 resulted in removal of colo...

In the title compound, C(16)H(13)NO(2), the 2,3-dimethyl-phenyl group and the 1H-isoindole-1,3(2H)-dione group are essentially planar, with r.m.s. deviations of 0.006 and 0.013 Å, respectively, and are oriented at an angle of 78.19 (3)° with respect to each other. In the crystal, weak C-H⋯O inter-actions link the mol-ecules, forming a zigzag chain parallel to the b axis. Futhermore, C-H⋯π inter...

New trans- and cis-o-stilbene-methylene-sydnones 3a,b were synthesized by transforming the trans- and cis-o-aminomethylstilbene derivative, obtained by reduction of corresponding o-cyano derivatives, into glycine ester derivatives (43 and 31% yield) followed by hydrolysis (90 and 96% yield), nitrosation and ring closure with acetic acid anhydride (30 and 40% yield). The products were submitted ...

Three-component reaction of dialkyl acetylenedicarboxylates, isocyanides and 1,3- diimino isoindoline affords highly functionalized 2,6-dihydropyrimido[2,1-a]isoindole derivatives in good yields under catalyst free and mild reaction conditions.

In the title compound, C(12)H(7)NO(5), the dihedral angle between the isoindole-1,3-dione plane and the least-squares plane of the furan ring is 89.2 (2)°. In the crystal structure, mol-ecules are linked through inter-molecular C-H⋯O hydrogen bonds, forming centrosymmetric dimers.

A series of 17 long-chain arylpiperazines containing bulky, complex imide systems (5,8-dimethyl-3b,9-epoxy-(3a,4,5,6,7,8,9,9a)-octahydro-1Hbenzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetrahydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT , 5-HT and dopamine D receptors. Most of the new compounds showed moderate ...