Valliappan Kannappan

Chiral Drug Engineering: Building Safer, Smarter, and More Selective Medicines

Leave a Comment / Chiral science / By / , , , , , / November 25, 2025

Where a molecule’s handedness meets clever engineering—shaping safer, more precise, and more effective medicines. Introduction: Why Chirality Matters in Drug Engineering In the world of drug design, a subtle twist in molecular geometry can change everything. Two molecules may share the same atoms and bonding pattern yet behave like entirely different substances simply because they are arranged as non-superimposable mirror images—enantiomers. This property, known as chirality, is one of the most critical yet nuanced dimensions …

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🧭 The Molecular Grammar of Medicines: Isomerism, Chirality, and Stereochemical Relationships Explained

Leave a Comment / Chiral science, Chirality, Drug stereochemistry, Stereochemistry / By / , , , , , / November 12, 2025

“Where molecules speak, stereochemistry gives them meaning“ In pharmaceuticals, structure is language — and stereochemistry is its grammar. The way atoms arrange in 3D space shapes how drugs work, how they are regulated, and how safe they are. This Chiralpedia tutorial simplifies the molecular “grammar” behind drug behavior and innovation. When Structure Speaks Every drug molecule has a story written in its structure. Two compounds may share the same formula yet act entirely differently due …

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The Hidden Chirality in Drug Metabolites: A metabolic blind spot

Leave a Comment / Chiral science, Chirality, Drug stereochemistry / By / , , , , / October 26, 2025

“Chirality isn’t hidden — we just stopped looking closely enough” The Unseen Journey After the Dose: 💊 When a patient swallows a drug, the journey is far from over. Sometimes, the real chiral story begins after the dose. The drug molecule meets a series of enzymes — oxidases, reductases, transferases — each capable of transforming it into one or more metabolites. We often assume these are simply inactive breakdown products, but chemistry rarely plays it …

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When Drug Labels Miss the Twist: The regulatory bind spot

Leave a Comment / Chiral Pharmacology, Chiral science, Chirality / By / , , , , , / October 24, 2025

“When chemistry tells two stories, the label should tell both” Drug labels tell us what’s inside — but not always how the molecule twists. And sometimes, that subtle twist changes everything: how a drug acts, how it’s regulated, and even whether it’s safe or addictive. Chirality — the property of handedness in molecules — has always shaped pharmacology. One mirror image of a molecule (an enantiomer) can save lives, while its twin may do little …

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Part 10: Stereochemistry in Pharmaceutical Sciences – Current Trends and Future Directions

Leave a Comment / Stereochemistry / By / , , / October 6, 2025

“Beyond today – emerging trends shaping the future of stereochemistry in pharma” Introduction The landscape of stereochemistry in pharmaceutical sciences continues to evolve with scientific and technological advances. This final part looks at emerging trends and future challenges. These include: – New developments in asymmetric catalysis, such as organocatalysts (MacMillan/List catalysts) that have expanded the toolkit for chiral synthesis, and the 2021 Nobel recognition of this field – implying more green and metal-free asymmetric processes …

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Part 9: Stereochemistry in Drug Discovery and Development

Leave a Comment / Stereochemistry / By / , , / October 3, 2025

“From hit to lead to medicine – where stereochemistry shapes every stage of discovery” Introduction Stereochemistry is not only crucial in the final stages of drug production – it plays a significant role right from the discovery and lead optimization phases. In this part, we consider how medicinal chemists account for chirality when designing compounds and how structure-activity relationships (SAR) can depend on stereochemistry. We also look at how screening libraries incorporate stereochemical diversity, and …

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Ibuprofen

Leave a Comment / Chiral Pharmacology, Chiral science / By / , , / September 29, 2025

Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID). It is a monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-(2-methylpropyl)phenyl group. Hence belongs to the propionic acid derivative class of NSAIDs. It is commonly prescribed for pain, inflammation, and fever. Available as over-the-counter (OTC) and prescription medication worldwide. Chirality and Biological Activity Structurally, Ibuprofen is a chiral molecule with one stereogenic center at the α-position …

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Part 8: Stereochemistry in Biologics and Natural Products

Leave a Comment / Stereochemistry / By / , / October 3, 2025

“Nature’s stereochemists – chirality in biologics, peptides, and natural products” Introduction Stereochemistry is inherent in biological macromolecules and natural products. This part explores chirality beyond small synthetic drugs – specifically, in biologics (peptides, proteins, nucleic acids) and in natural product-derived drugs. We examine how nature’s biosynthetic machinery imparts stereochemistry with high fidelity (e.g., enzymes produce single enantiomers of amino acids, sugars, complex polyketides). We discuss examples of drugs that are derived from natural chirality (like …

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Part 7: Analytical Techniques for Stereochemistry

Leave a Comment / Stereochemistry / By / , , , / October 2, 2025

“Measuring handedness – tools and techniques that bring chirality into focus” Introduction Ensuring the correct stereochemistry and measuring stereochemical purity is a crucial aspect of pharmaceutical quality control and research. This part covers the major analytical techniques used to distinguish and quantify enantiomers and diastereomers in drug substances and products. Key techniques include: We’ll discuss how these techniques are applied in practice: e.g., during process development, a chiral HPLC method is developed to monitor enantiomeric …

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Part 6: Resolution of Enantiomers

Leave a Comment / Stereochemistry / By / , , / October 2, 2025

“Separating the inseparable: how chemists resolve mirror-image molecules.” Introduction Despite advances in asymmetric synthesis (Part 5), sometimes we still end up with a racemic mixture of enantiomers. When direct stereoselective routes are impractical, chemists must separate the enantiomers – a process known as resolution. This part examines classical and modern methods for resolving enantiomers, their pros and cons, and how they are applied in pharmaceutical contexts. We will cover: We’ll also discuss the racemic mixture …

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