cgs-27023a and Brain-Edema

cgs-27023a has been researched along with Brain-Edema* in 2 studies

Other Studies

2 other study(ies) available for cgs-27023a and Brain-Edema

Article	Year
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents. Bioorganic & medicinal chemistry letters, 2008, Feb-01, Volume: 18, Issue:3 The introduction and the optimization of an alpha-amino substituent based on a series of alpha-hydroxy-beta-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated. Topics: Amino Acids; Animals; Brain Edema; Disease Models, Animal; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Middle Cerebral Artery; Molecular Structure; Pyrazines; Rats; Stereoisomerism; Structure-Activity Relationship; Sulfonamides	2008
Treatment of cold injury-induced brain edema with a nonspecific matrix metalloproteinase inhibitor MMI270 in rats. Acta neurochirurgica. Supplement, 2003, Volume: 86 Blood-brain barrier (BBB) disruption is a critical event leading to vasogenic brain edema and secondary brain damage after cold injury-induced brain trauma. Matrix metalloproteinases (MMPs) are implicated in BBB disruption in this model. The purpose of this study was to examine the effects of MMI270, a synthetic nonspecific MMP inhibitor, on cold injury-induced brain edema in rats. Treatment with MMI270, a bolus injection at a dose of 30 mg/kg, was started immediately after the induction of cold injury and was continued at a dose of 40 mg/kg/day using an intraperitoneal osmotic minipump. At 24 hours after the cold injury, the brain water content and the BBB permeability to Evans Blue (EB) were determined. The secondary brain lesion was assessed using hematoxylin and eosin (H-E) staining at 7 days after the cold injury. Compared with the untreated control group, treatment with MMI270 significantly reduced the brain water content in the ipsilateral core and intermediate areas and protected the BBB integrity to EB in the ipsilateral core area. The secondary lesion was significantly smaller in the MMI270-treated animals compared with the untreated animals. Our results indicate that treatment with MMI270 in rats exhibits protection in acute brain edema formation and secondary brain lesion by attenuating the BBB permeability after cold injury. Topics: Animals; Blood-Brain Barrier; Body Water; Brain; Brain Edema; Brain Injuries; Capillary Permeability; Cold Temperature; Enzyme Inhibitors; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Parietal Lobe; Pyrazines; Rats; Rats, Sprague-Dawley; Staining and Labeling; Sulfonamides	2003

Article

Year

beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.

Bioorganic & medicinal chemistry letters, 2008, Feb-01, Volume: 18, Issue:3

The introduction and the optimization of an alpha-amino substituent based on a series of alpha-hydroxy-beta-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated.

Topics: Amino Acids; Animals; Brain Edema; Disease Models, Animal; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Middle Cerebral Artery; Molecular Structure; Pyrazines; Rats; Stereoisomerism; Structure-Activity Relationship; Sulfonamides

2008

Treatment of cold injury-induced brain edema with a nonspecific matrix metalloproteinase inhibitor MMI270 in rats.

Acta neurochirurgica. Supplement, 2003, Volume: 86

Blood-brain barrier (BBB) disruption is a critical event leading to vasogenic brain edema and secondary brain damage after cold injury-induced brain trauma. Matrix metalloproteinases (MMPs) are implicated in BBB disruption in this model. The purpose of this study was to examine the effects of MMI270, a synthetic nonspecific MMP inhibitor, on cold injury-induced brain edema in rats. Treatment with MMI270, a bolus injection at a dose of 30 mg/kg, was started immediately after the induction of cold injury and was continued at a dose of 40 mg/kg/day using an intraperitoneal osmotic minipump. At 24 hours after the cold injury, the brain water content and the BBB permeability to Evans Blue (EB) were determined. The secondary brain lesion was assessed using hematoxylin and eosin (H-E) staining at 7 days after the cold injury. Compared with the untreated control group, treatment with MMI270 significantly reduced the brain water content in the ipsilateral core and intermediate areas and protected the BBB integrity to EB in the ipsilateral core area. The secondary lesion was significantly smaller in the MMI270-treated animals compared with the untreated animals. Our results indicate that treatment with MMI270 in rats exhibits protection in acute brain edema formation and secondary brain lesion by attenuating the BBB permeability after cold injury.

Topics: Animals; Blood-Brain Barrier; Body Water; Brain; Brain Edema; Brain Injuries; Capillary Permeability; Cold Temperature; Enzyme Inhibitors; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Parietal Lobe; Pyrazines; Rats; Rats, Sprague-Dawley; Staining and Labeling; Sulfonamides

2003