Abstract
Cinnamic acid-nitric oxide (NO) donor hybrids have attracted attention, in recent years, as new pharmacological agents to treat multifactorial diseases. In the present study, hybrid oxime 5 was synthesized and its anti-lipid peroxidation and anti-lipoxygenase activities were evaluated. The new compound showed remarkable anti-LOX activity, while its antioxidant activity was quite good in comparison to the appropriate reference compounds. The examined derivative seems to be orally active in accordance to Lipinski’s rule of five. Compound 5 can be considered as a leading structure for the design and synthesis of new hybrids.
Highlights
Inflammation is the normal response of the body to several stimuli
Many well-known non-steroidal anti-inflammatory drugs (NSAIDs) are aimed at inhibiting COX, while LOX has been the target of new compounds [4,5]
The natural hydroxy substituted cinnamic derivatives present several biological activities. Synthetic modifications in their structure lead to cinnamic acid derivatives with a vital role in the formation of commercially important molecules which are necessary for the production of different bioactive compounds and drugs
Summary
Inflammation is the normal response of the body to several stimuli. This response includes the release of antibodies and proteins, as well as increased blood flow to the damaged area. The natural hydroxy substituted cinnamic derivatives present several biological activities Synthetic modifications in their structure lead to cinnamic acid derivatives with a vital role in the formation of commercially important molecules which are necessary for the production of different bioactive compounds and drugs. Due to the importance of new, more active molecules, the present study is focused on the design and synthesis of one new cinnamic acid hybrid molecules, incorporating an NO. Due to the importance of new, more active molecules, the present study is focused on the design and synthesis of one new cinnamic acid hybrid molecules, incorporating an NO donor groudponeo.gr.,gtrhoeupoxei.mg.,etghreoouxpim. The compound (4) was tested as well, for the comparison of the structures This compound exhibited no activity, which is underlined by the importance of the oxime group in the inhibition of LOX. The IC50 value of the compound (5) against LOX was found to be 50 μM (Table 2)
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