Title:Cinnamate Hybrids: A Unique Family of Compounds with Multiple Biological Activities
Volume: 19
Issue: 13
Author(s): Eleni Pontiki*, Aikaterini Peperidou, Ioannis Fotopoulos and Dimitra Hadjipavlou-Litina*
Affiliation:
- Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, 54124,Greece
- Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, 54124,Greece
Keywords:
Cinnamate hybrids, anti-Alzheimer activity, anti-inflammatory activity, anticancer activity, antimicrobial activity.
Abstract: Cinnamic acid derivatives are widely distributed in nature presenting a wide range of biological
activities: antiseptic, stimulant, carminative and insecticidal activities. Hydroxy- cinnamic acids,
especially caffeic, ferulic and chlorogenic, present various biological activities and they are synthesized
in nature through the phenylpropanoid pathway.
Additionally, the cinnamoyl moiety is present in various drugs such as a) Ozagrel, an imidazole π -
substituted cinnamic acid acting as a thromboxane A2 synthase inhibitor, used therapeutically for treating
acute ischemic stroke, b) Cinnarizine, Cinanserin and Tranilast, a series of antiallergic agents etc.
During the last decade, scientists have focused on multifunctional molecules instead of a single molecule
hitting one target. Multi-target drugs can be beneficial for the treatment of complex and multifunctional
diseases. A variety of multi-target drugs contain the cinnamic acid moiety due to its biological
importance and combination of biological activities e.g. antioxidant, antiiflammatory, anticancer,
antituberculosis, antifungal, antimalarial, antiatherogenic, antimicrobial activities. Recently for the
treatment of complex diseases hybrid drugs combining two pharmaceutical moieties in one molecule
have been developed. These molecules are more medically effective than their individual components.
In this review, a survey of cinnamate hybrids, that is molecules that combine the cinnamic acid moiety
with at least a second pharmacophore with or without a linker, acting as “multi-target” agents, is given.
The hybrids are listed in terms of their biological activity and applications as anti-Alzheimer, anticancer
agents as well as for cardiovascular diseases, as antivirals, antimalarials etc.
