Monoamine oxidase (MAO) is an enzyme that metabolizes a wide range of monoamines and is important in the control of the concentration of these neurotransmitters. Several reports have shown that stress can decrease MAO inhibitory activity. An endogenous MAO inhibitory component was first discovered in normal human urine by Glover et al. (22), and the compound responsible for the MAO activity was...

In continuation of our endeavor with respect to the development of potent and effective isatin-based anticancer agents, we adopted the molecular hybridization approach to design and synthesize four different sets of isatin-quinazoline (6a-f and 7a-e)/phthalazine (8a-f)/quinoxaline (9a-f) hybrids. The antiproliferative activity of the target hybrids was assessed towards HT-29 (colon), ZR-75 (bre...

A highly enantioselective aza-Henry reaction with isatin N-Boc ketimines using a Cu(II)-BOX complex as a catalyst is described. The reaction, which does not require protection of the N1 atom, provides the corresponding nitroamines bearing a quaternary stereocentre with high yields and enantiomeric excesses (up to 99.9%).

The Morita-Baylis-Hillman reaction of acrylamide, as an activated alkene, has seen little development due to its low reactivity. We have developed the reaction using isatin derivatives with acrylamide, DABCO as a promoter and phenol as an additive in acetonitrile. The corresponding aza version with acrylate and acrylonitrile has also been developed resulting in high product yields.

The concentration of transmitter in the synaptic cleft and its clearance time are one of the main determinants of synaptic strength. We estimated the time course of glycine at rat lumbar motoneurons synapses in spinal cord slices by recording synaptic currents in the presence of a low-affinity competitive antagonist at glycine receptors [2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazini...

Since indole is present at up to 500 microM in the stationary phase and is an interspecies biofilm signal (J. Lee, A. Jayaraman, and T. K. Wood, BMC Microbiol. 7:42, 2007), we investigated hydroxyindoles as biofilm signals and found them also to be nontoxic interspecies biofilm signals for enterohemorrhagic Escherichia coli O157:H7 (EHEC), E. coli K-12, and Pseudomonas aeruginosa. The genetic b...

Marine molluscs are rich in biologically active natural products that provide new potential sources of anti-inflammatory agents. Here we used bioassay guided fractionation of extracts from the muricid Dicathais orbita to identify brominated indoles with anti-inflammatory activity, based on the inhibition of nitric oxide (NO) and tumour necrosis factor α (TNFα) in lipopolysaccharide (LPS) stimul...

The composition and stability of the complexes of isatin-β-thiosemicarbazone with Co(II), Ni(II), Cu(II), Zn(II), Pd(II) and Hg(II) have been investigated using spectrophotometric method at 30 °C and constant ionic strength of 0.1 mol dm-3 (KNO3) in 70 % ethanol. Experimental results indicate the formation of MeL and MeL2 complexes for Ni(II) and Co(II), and MeL for Cu(II), Zn(II), Pd(II) and H...