ArticleMolecules (Basel, Switzerland)2014
Multitarget molecular hybrids of cinnamic acids.
Article in Molecules (Basel, Switzerland), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- Design, Synthesis, Biological Evaluation, and In Silico Studies of Novel Multitarget Cinnamic Acid Hybrids.Molecules (Basel, Switzerland) · 2025Article
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- Exploring acetaminophen prodrugs and hybrids: a review.RSC advances · 2024Review
- Synthesis and Antioxidant Activities of Novel Pyrimidine Acrylamides as Inhibitors of Lipoxygenase: Molecular Modeling and In Silico Physicochemical Studies.Molecules (Basel, Switzerland) · 2024Article
- Composition, Organoleptic Characteristics, Fatty Acid Profile and Oxidative Status of Cow's Milk and White Cheese after Dietary Partial Replacement of Soybean Meal with Flaxseed and Lupin.Animals : an open access journal from MDPI · 2023Article
- Exploring the Medicinal Potential ofPlants (Basel, Switzerland) · 2023Article
- Design and Synthesis of Coumarin Derivatives as Cytotoxic Agents through PI3K/AKT Signaling Pathway Inhibition in HL60 and HepG2 Cancer Cells.Molecules (Basel, Switzerland) · 2022Article
- Effects of Cornus and Its Mixture with Oregano and Thyme Essential Oils on Dairy Sheep Performance and Milk, Yoghurt and Cheese Quality under Heat Stress.Animals : an open access journal from MDPI · 2021Article
- Biological Activities and ADMET-Related Properties of Novel Set of Cinnamanilides.Molecules (Basel, Switzerland) · 2020Article
- 5-(4Molecules (Basel, Switzerland) · 2020Article
- Synthesis and Spectrum of Biological Activities of Novel N-arylcinnamamides.International journal of molecular sciences · 2018Article
- Multifunctional Cinnamic Acid Derivatives.Molecules (Basel, Switzerland) · 2017Article
- Synthesis and Pharmacochemistry of New Pleiotropic Pyrrolyl Derivatives.Molecules (Basel, Switzerland) · 2015Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In an attempt to synthesize potential new multitarget agents, 11 novel hybrids incorporating cinnamic acids and paracetamol, 4-/7-hydroxycoumarin, benzocaine, p-aminophenol and m-aminophenol were synthesized. Three hybrids-2e, 2a, 2g-and 3b were found to be multifunctional agents. The hybrid 2e derived from the phenoxyphenyl cinnamic acid and m-acetamidophenol showed the highest lipoxygenase (LOX) inhibition and analgesic activity (IC50 = 0.34 μΜ and 98.1%, whereas the hybrid 3b of bromobenzyloxycinnamic acid and hymechromone exhibited simultaneously good LOX inhibitory activity (IC50 = 50 μΜ) and the highest anti-proteolytic activity (IC50= 5 μΜ). The hybrid 2a of phenyloxyphenyl acid with paracetamol showed a high analgesic activity (91%) and appears to be a promising agent for treating peripheral nerve injuries. Hybrid 2g which has an ester and an amide bond presents an interesting combination of anti-LOX and anti-proteolytic activity. The esters were found very potent and especially those derived from paracetamol and m-acetamidophenol. The amides follow. Based on 2D-structure-activity relationships it was observed that both steric and electronic parameters play major roles in the activity of these compounds. Molecular docking studies point to the fact that allosteric interactions might govern the LOX-inhibitor binding.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.