Vanillin Derivatives in Drug Design: Structure–Activity Relationship (SAR) Hotspots and Synthetic Pathways for Enhanced Pharmacological Activity
Suleiman M. Sankaranarayanan M. Theva Das K. Amran S.I. Berezin V. Andrey B. Jamalis J.
9 December 2025American Chemical Society
ACS Omega
2025#10Issue 4857846 - 57875 pp.
Drug discovery often uses privileged molecular scaffolds, such as vanillin, which are naturally found in plants for drug design and synthesis. Incorporating vanillin into standard chemical structures and synthesizing novel derivatives with active scaffolds are vital for developing effective therapeutic candidates. The aromatic ring of vanillin contains functional groups such as aldehyde, hydroxyl, and ether, which facilitate its modification and the generation of various resultant derivatives with promising biological activities. Consequently, numerous strategies have been developed and incorporated into synthetic pathways to produce biologically potent vanillin derivatives. Vanillin-based compounds have demonstrated effectiveness against a wide range of emerging infectious diseases. This review focuses on the key structure–activity relationship hotspots within vanillin derivatives that influence their biological activity. By examining the synthetic pathways developed over the past decade (2014–2025), we highlight how targeted modifications at specific SAR hotspots can enhance the therapeutic potential of these compounds, such as antitubercular, antioxidant, antimalarial, anticancer, and anti-inflammatory properties.
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Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru, Johor, 81310, Malaysia
Department of Chemistry, Sokoto State University, Birnin Kebbi Road, Sokoto, 852101, Nigeria
Medicinal Chemistry Research Laboratory, Birla Institute of Technology & Science Pilani (BITS Pilani), Pilani Campus, Pilani, 333031, India
Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Penang, Gelugor, 11800, Malaysia
Department of Biosciences, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru, Johor, 81310, Malaysia
Research and Production Center for Microbiology and Virology, Almaty, 050010, Kazakhstan
Department of Chemistry
Department of Chemistry
Medicinal Chemistry Research Laboratory
Institute for Research in Molecular Medicine
Department of Biosciences
Research and Production Center for Microbiology and Virology
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