Identification, biological activity, and mechanism of the anti-ischemic quinolone analog

The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in in vivo rat MCAO model (32.1% at 0.01 mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at...

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Published in:Bioorganic & medicinal chemistry 2007-10, Vol.15 (20), p.6517-6526
Main Authors: Park, Chan-Hee, Lee, Jongwon, Jung, Hwi Young, Kim, Min Ji, Lim, Sun Ha, Yeo, Hyung Tae, Choi, Eung Chil, Yoon, Eun Jeong, Kim, Kyu Won, Cha, Jong Ho, Kim, Seok-Ho, Chang, Dong-Jo, Kwon, Do-Yeon, Li, Funan, Suh, Young-Ger
Format: Article
Language:English
Subjects:
Animals
Anti-apoptotic activity
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Anti-ischemic agents
Biological and medical sciences
Brain Ischemia - drug therapy
Brain Ischemia - pathology
Cardiovascular system
Cell Line, Tumor
Cell Survival - drug effects
Disease Models, Animal
Humans
MCAO
Medical sciences
Miscellaneous
Models, Biological
Molecular Structure
Myocardial Infarction - drug therapy
Myocardial Infarction - pathology
Neuropharmacology
Pharmacology. Drug treatments
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
Quinolines - therapeutic use
Quinolone analog
Rats
Structure-Activity Relationship
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Summary:The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in in vivo rat MCAO model (32.1% at 0.01 mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at 0.01 mg/kg) while it exhibited highly reduced anti-bacterial activity. The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in vivo rat MCAO model (32.1% at 0.01 mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at 0.01 mg/kg) while it exhibited highly reduced anti-bacterial activity. The mechanistic study revealed that the anti-ischemic activity might exert via an anti-apoptotic pathway, which implies its therapeutic uses against the ischemic cell injuries including ischemic stroke and ischemic heart disease.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2007.07.009