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Papers of the Week

Papers: 8 Jan 2022 - 14 Jan 2022

Pharmacology/Drug Development

2021 Dec 24




Insights into Structural Modifications of Valproic Acid and Their Pharmacological Profile.


Mishra M K, Kukal S, Paul P R, Bora S, Singh A, Kukreti S, Saso L, Muthusamy K, Hasija Y, Kukreti R
Molecules. 2021 Dec 24; 27(1).
PMID: 35011339.


Valproic acid (VPA) is a well-established anticonvulsant drug discovered serendipitously and marketed for the treatment of epilepsy, migraine, bipolar disorder and neuropathic pain. Apart from this, VPA has potential therapeutic applications in other central nervous system (CNS) disorders and in various cancer types. Since the discovery of its anticonvulsant activity, substantial efforts have been made to develop structural analogues and derivatives in an attempt to increase potency and decrease adverse side effects, the most significant being teratogenicity and hepatotoxicity. Most of these compounds have shown reduced toxicity with improved potency. The simple structure of VPA offers a great advantage to its modification. This review briefly discusses the pharmacology and molecular targets of VPA. The article then elaborates on the structural modifications in VPA including amide-derivatives, acid and cyclic analogues, urea derivatives and pro-drugs, and compares their pharmacological profile with that of the parent molecule. The current challenges for the clinical use of these derivatives are also discussed. The review is expected to provide necessary knowledgebase for the further development of VPA-derived compounds.