Sumit Maurya, Sumit Manna, Mala Singh, Dharmendra Singh, Malay Nayak, Sudip Mukherjee, Arunava Manna
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Protocatechuic Acid and its Derivatives: Synthesis, Antioxidant Properties, and Potential In Vivo Wound Healing Applications
Treatment of chronic wounds is a potential healthcare problem, affecting people globally. Traditional methods of wound healing are prone to several limitations, like infections, oxidative stress, and development of secondary wounds. Management of oxidative stress is an interesting platform to deal with chronic wounds. For this study, novel derivatives of protocatechuic acid, a naturally occurring phenolic acid, were designed by modifying the carboxylic acid moiety while preserving the hydroxyl groups for radical scavenging. So, a series of amide conjugates were synthesized by incorporating various amine moieties. Glucose conjugates were obtained through both click chemistry and direct coupling strategies and a chlorinated derivative was also prepared. The antioxidant potential of the compounds was screened using DPPH assay, followed by in vitro DCFDA assay on HEK-293T cell line. Top 5 lead molecules were checked for biocompatibility through MTT assay, which provided us with top 2 leads, Compounds 12 and 17 which were examined for a wound healing study on Wistar rats along with the starting compound 1. It was observed that Compound 17 demonstrated excellent wound tissue regeneration on day 12, as compared to the control group, suggesting the promising role of triazole and glucose moieties conjugation for relieving oxidative stress and wound management.
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Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies.
ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs.
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