Synthesis and biological evaluation of (--)-linarinic acid derivatives as neuroprotective agents against OGD-induced cell damage

Arch Pharm (Weinheim). 2012 Jun;345(6):423-30. doi: 10.1002/ardp.201100424. Epub 2012 Mar 22.

Abstract

A series of novel (-)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid derivatives were designed and synthesized. All of the prepared compounds were screened for their neuroprotective effects using an in vitro oxygen glucose deprivation (OGD) model of ischemic stroke. Some of the target compounds exhibited moderate to excellent protective potency. In particular, compounds 9d, 9e, 9g, and 9h showed significant protective effects in the SH-SY(5) Y cell line at all three concentrations tested.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Brain Ischemia / drug therapy
  • Brain Ischemia / pathology
  • Cell Culture Techniques
  • Cell Hypoxia / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Culture Media
  • Dose-Response Relationship, Drug
  • Glucose* / deficiency
  • Humans
  • Models, Biological
  • Molecular Structure
  • Neurons / drug effects*
  • Neurons / pathology
  • Neuroprotective Agents / chemical synthesis*
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology
  • Oxygen* / metabolism
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Pyrroles / pharmacology
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Reperfusion Injury / pathology
  • Reperfusion Injury / prevention & control
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Culture Media
  • Neuroprotective Agents
  • Pyrroles
  • Quinazolines
  • Glucose
  • Oxygen