Recent Advances on Nitrones Design for Stroke Treatment.

Abstract

The recent advances of tetramethylpyrazine nitrones and quinolylnitrones for the treatment of stroke have been reviewed and compared with other agents, showing promising therapeutic applications. As a result of a functional transformation of natural product ligustrazine, (Z)-N-tert-butyl-1-(3,5,6-trimethylpyrazin-2-yl)methanimine oxide (6) is a multitarget small nitrone showing potent thrombolytic activity and free radicals scavenging power, in addition to nontoxicity and blood-brain barrier permeability. Similarly, antioxidant (Z)-N-tert-butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine oxide (17) is a novel agent for cerebral ischemia therapy as it is able to scavenge different types of free radical species, showing strong neuroprotection and reduced infarct size.

• Authors: José Marco-Contelles
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 63 Issue 22 Pg. 13413-13427 (11 25 2020) ISSN: 1520-4804 [Electronic] United States
• PMID: 32869989 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Neuroprotective Agents
• Nitrogen Oxides
• nitrones

Topics

• Animals
• Drug Design
• Humans
• Neuroprotective Agents (chemical synthesis, therapeutic use)
• Nitrogen Oxides (chemical synthesis, therapeutic use)
• Stroke (drug therapy, pathology)
• Treatment Outcome