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1.
Bioorg Med Chem ; 14(7): 2409-17, 2006 Apr 01.
Article in English | MEDLINE | ID: mdl-16321543

ABSTRACT

A microwave-assisted three-component, regioselective one-pot cyclocondensation method has been developed for the synthesis of a series of novel spiro[indole-thiazolidinones] (6a-l) using an environmentally benign procedure at atmospheric pressure in open vessel. This rapid method produces pure products in high yields within few minutes in comparison to a conventional two-step procedure. The crystal structure of one representative compound has been determined by X-ray diffraction. The synthesized compounds have been screened 'in vitro' for antifungal activity against Rhizoctonia solani, Fusarium oxysporum and Collectotrichum capsici. All compounds have shown good activity against these pathogens.


Subject(s)
Antifungal Agents/chemical synthesis , Benzimidazoles/chemistry , Indoles/chemical synthesis , Spiro Compounds/chemical synthesis , Triazoles/chemistry , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Benzimidazoles/radiation effects , Colletotrichum/classification , Colletotrichum/drug effects , Crystallization , Fusarium/classification , Fusarium/drug effects , Indoles/chemistry , Indoles/pharmacology , Indoles/radiation effects , Microwaves , Models, Molecular , Molecular Structure , Rhizoctonia/classification , Rhizoctonia/drug effects , Spiro Compounds/chemistry , Spiro Compounds/pharmacology , Stereoisomerism , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/radiation effects , Thiazolidines , Triazoles/radiation effects , X-Ray Diffraction
2.
Brain Res Dev Brain Res ; 140(2): 287-97, 2003 Feb 16.
Article in English | MEDLINE | ID: mdl-12586434

ABSTRACT

The excitotoxic cascade may represent an important pathway leading to brain damage and cerebral palsy. Brain lesions induced in newborn mice by ibotenate (acting on N-methyl-D-aspartate receptors) and by S-bromowillardiine (acting on alpha-3-amino-hydroxy-5-methyl-4-isoxazole propionic acid and kainate receptors) mimic some aspects of white matter cysts and transcortical necrosis observed in human perinatal brain damage. Fructose 1,6-biphosphate (FBP) is a high-energy glycolytic pathway intermediate which, in therapeutic doses, is non-toxic and neuroprotective in hypoxic-ischemic models of brain injury. Mechanisms of action include modulation of intracellular calcium through phospholipase C (PLC) activation. The goal of this study was to determine the neuroprotective effects of FBP in a mouse model of neonatal excitotoxic brain injury. Mice that received intraperitoneal FBP had a significant reduction in size of ibotenate-induced (80% reduction) or S-bromowillardiine-induced (40% reduction) cortical plate lesions when compared with control animals. Studies of fragmented DNA and cleaved caspase 3 confirmed the survival promoting effects of FBP. FBP had no detectable effect on excitotoxic white matter lesions. The effects of FBP were antagonized by co-administration of PLC, protein kinase C or mitogen-associated protein kinase inhibitors but not by protein kinase A inhibitor. A moderate, transient cooling of pups immediately after the insult extended the therapeutic window for FBP, as FBP administered 24 h after ibotenate was still significantly neuroprotective in these pups. This data extends the neuroprotective profile of FBP in neonatal brain injury and identifies gray matter lesions involving N-methyl-D-aspartate receptors as a major target for this promising drug.


Subject(s)
Alanine/analogs & derivatives , Alanine/pharmacology , Animals, Newborn/physiology , Brain/drug effects , Brain/physiology , Fructosediphosphates/pharmacology , Ibotenic Acid/pharmacology , Neurons/drug effects , Neurons/physiology , Neuroprotective Agents/pharmacology , Neurotoxins/pharmacology , Animals , Brain/cytology , Cell Survival/drug effects , Enzyme Inhibitors/pharmacology , Female , Hydrogen-Ion Concentration , Lactic Acid/metabolism , Male , Mice , Mortality , Signal Transduction/drug effects
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