In recent years, because the technology of isolation, purification, structure identification and biological activity's tracking have made great progress, some alkaloids with novel structures were found continuously. These alkaloids play an important role in biopharmaceuticals by virtue of their pharmacological activities, such as antitumor, anti-inflammatory and antiviral. Usually, relatively few alkaloids are directly formulated into drugs. This is due to the low solubility and unstable metabolism of most alkaloids, which particularly hinders the development of drugs. Additionally, many alkaloids are often structurally complex, and their 'heavy' structures break Lipinski's rules and most likely will limit their absorption from the gut into the blood, thus impeding oral formulation. Therefore, it is important to improve the properties and activities of alkaloids through structural modifications to obtain the final drug candidates.
Advantages of Structural Modifications
The main advantages of modifying the structure of the alkaloids are as follows.
- Increase of low solubility
Low water solubility limits absorption and results in poor oral bioavailability. The solubility of alkaloids can generally be increased by structural modifications, such as the addition of ionizable or polar groups.
- Simplification of complex structure
Structurally complex alkaloids usually have a high molecular weight, which brings about poor oral absorbability. Therefore, it is necessary to develop simpler alkaloid compounds by using structural modifications while retaining their biological activity.
- Improvement of chemical stability
The structures of some alkaloids contain groups that are prone to oxidation and hydrolysis. This causes the alkaloids to fail easily and thus metabolized faster in the body. Chemical modification for these unstable groups can increase the stability of the drug and prolong the duration of drug action.
- Improvement of selectivity
After administration, most natural drugs undergo processes such as absorption, transport, and metabolism in the body. To improve the treatment effectiveness, it is sometimes necessary to increase the blood concentration of the drug, but the adverse side effects will also increase. Therefore, it is necessary to improve the targeting of drugs through structural modifications so that they primarily act on diseased cells.
Our Services
Alfa Chemistry strives to provide excellent service to our customers. Our professional technicians can customize the structural modification scheme of alkaloids for you according to your needs. Our services include but are not limited to the following.
- Structural modification of alkaloids according to molecular size and complexity.
- Study conformational relationships, extract pharmacophore, achieve scaffold hopping, and obtain new structural types of molecules.
- Eliminate unnecessary chiral centers and retain necessary conformations bound to the target.
- Large-scale preparation for industrialization.
Our Advantages
With many years of experience, Alfa Chemistry has the ability to provide professional alkaloid structural modification services. Once our technical experts take over your project, they will take responsibility for your project to the end. If you are interested in our services, please feel free to contact us. Alfa Chemistry is always your project partner.
