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Chirality In Organic Molecules And Importance In Pharmaceuticals
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  • Country: Australia

Chirality is a key notion in organic chemistry. It refers to the geometric structure of geometry. This character prevents it from overlapping on its mirror copy. The study of this character is important in many fields. One can see its importance in the pharmaceutical industry. 

The chirality of molecules plays an important role in this field. It has a profound impact on their biological activity. It also influences how effective a medicine is.  In this sample paper, we will discuss the topic and its role in the pharmaceutical sector.

Understanding Chirality

Chirality comes from the Greek word "cheir". In English it means hand. It is used to describe things that are mirror reflections of one another. However, they can not be superimposed such as left and right hands. 

A molecule is regarded as chiral in chemistry if it can't be superimposed on its mirror copy. Usually, these molecules contain a carbon atom. The atom is attached to four different substituents. It is known as a chiral or stereogenic centre. 

Chiral Centers

A carbon atom generally forms the chiral centre. It has four distinct groups connected to it. This leads to the formation of two mirror images. These images are non-superimposable and known as enantiomers. 

These enantiomers are designated as either (R)- or (S)-. This designation is based on the Cahn-Ingold-Prelog priority rule. The principle helps to determine the arrangement of substitutes around the chiral centre. 

Diastereomers and Enantiomers

Chiral molecules are found to exist as Enantiomer pairs. These pairs are non-superimposable mirror images of one another. Enantiomers have similar physical characteristics. Some of them are - the same melting temperatures and solubility. However, they rotate plane-polarized light in opposite directions. This feature is called optical activity. 
In addition to it, they can have multiple chiral centres. Its formation is known as diastereomers. They are stereoisomers which are not mirror images of each other. And thus they vary in physical and chemical properties. 

The Significance Of Chirality In Pharmaceuticals

One cannot stress the importance of chirality in pharmaceuticals. The biological activity of Chiral medications is dependent on enantiomers. 
It means that one enantiomer may be therapeutically active.

On the other hand, the other may be inactive or even hazardous. It is important to understand the concept of chirality. It helps in the development of safe medications. 

Specific Enantiomer Activity

Different biological molecules react differently. For example, enzymes and receptors are chiral. However, they interact differently with each enantiomer of a drug. This property leads to different effects in medications.

For instance, there are two enantiomers of the medication thalidomide. They were sold as sedatives and treatments for morning sickness in the 1950s and 1960s.  
(S)-enantiomer is teratogenic in nature. It can cause serious birth defects.

On the other hand, the  (R)-enantiomer has therapeutic properties. The side effect reflects how important it is to do a proper study of chirality. It is essential for safety and efficacy. 

Pharmacokinetics and Pharmacodynamics

Pharmacokinetics refers to absorption,  distribution, metabolism and excretion of drugs. It is affected by chirality. Pharmacodynamics refers to the mechanism of action and effects of drugs. Chirality also has an impact on it.

Enantiomers can follow different metabolic pathways. It results in differences in how long they take to act as well as possible side effects.

For example, there are two enantiomers of the beta-blocker propranolol. They are (R)-propranolol and (S)-propranolol. The (S)-enantiomer mainly causes the drug's beta-blocking activity.

The R enantiomer performs different pharmacokinetic functions.  Therefore, if you want to realise the best therapeutic outcomes, a comprehensive understanding of chirality is essential. 

Regulator and Manufacturing Considerations

There are regulatory guidelines that cover the importance of chirality. It is reflected in manufacturing practices too. There are regulatory agencies that monitor information on new drugs. They demand complete details on the chirality. 

These agencies include the Therapeutic Goods Administration (TGA) in Australia and the Food and Drug Administration (FDA) in the US. These agencies focused on the synthesis, separation and analysis of enantiomers. It also covers their pharmacological and toxicological properties. 

There are many advanced techniques to produce pure enantiomers. Manufacturers frequently use them for separation and production.

Some of the latest methods adopted by manufacturers are

  • Asymmetric synthesis,

  • biocatalysis, and 

  • chiral chromatography 

These techniques are used to guarantee safety and efficacy. 

Chiral Pharmaceutical Case Studies

There is no doubt regarding the importance of chirality. Below are some case studies that showcase the role of chirality in drug development. 


Thalidomide is a standing example of the side effects. It showcases the downsides of neglecting chirality. It was first used as a sedative and antiemetic. 
However later it was discovered that its (S)- enantiomer causes serious birth defects. After this discovery, it was withdrawn from the market. The case highlights the importance of proper case analysis. It showcases the whole picture during drug development.


Omeprazole is used to treat gastroesophageal reflux disease. It is a proton pump inhibitor existing as two enantiomers. Its S counterpart was proven effective in reducing gastric acid secretion. It was known as esomeprazole. Due to this high effectiveness, it was sold as a separate drug. It provided more effective treatment reducing side effects.
Hence it is of no use and does not contribute to the treatment. It highlights the importance of thorough analyses to develop drugs.

Analysis Techniques for Chirality

A careful observation requires using advanced techniques. It leads to pure and effective chiral drugs. Below are some methods which are used for analysis. 

Chromatography Chiral

Chiral chromatography is used to separate enantiomers. It has been proven effective in differentiating between enantiomers. It uses phases to study their isolation and analysis.  This technique often uses gas chromatography (GC) and high-performance liquid chromatography (HPLC). 

Nuclear Magnetic Resonance (NMR) Spectroscopy 

NMR Spectroscopy is useful in giving Comprehensive details. It provides useful information regarding the stereochemistry of chiral compounds. Researchers may determine the structure and purity of enantiomers. They can examine the chemical changes and bonding factors. 


This technique measures the optical rotation of chiral compounds. It uses plane-polarised light to ascertain the specific rotation. It also helps to learn about the optical purity of enantiomers.

Obstacles And Opportunities For The Future

There have been tremendous advancements in the field of chirality. The field has bloomed with better knowledge and management. However, there are still many obstacles.  

Cost and Complexity

The production of enantiomerically pure drugs can be expensive. The process is generally long and complicated. The process typically employed approaches like asymmetric synthesis and chiral chromatography. These require expertise. The processes use expensive equipment and expertise. These factors raise the overall cost of research.

Regulatory hurdles

It isn't easy to navigate the regulations for chiral drugs. Regulatory agencies demand detailed information on the chirality of new drugs. The agencies also focus on manufacture, analysis, and pharmacological features. Fulfilling all these specifications can be time-consuming. It might also require large resources. 

Emerging technologies

Technological advancements have brought a change in production and analysis. It uses machine learning and Computational chemistry. These techniques are used to predict and optimise the characteristics of new medicines. These advancements have made it possible to make the process more efficient. They have reduced the cost and brought many developments.  


Chirality is an essential concept in organic chemistry. It plays an important role in the development of pharmaceuticals. The enantiomeric character of chiral medicines has a significant impact on their biological activity, safety, and efficacy. It is necessary to understand and manage chirality to ensure effective and safe drugs. The pharmaceutical business can use chirality to improve outcomes and patient care. 

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