Drug building blocks refer to small molecular compounds developed for the design and construction of drug active substances. Generally, the molecular weight is less than 300, and it has the characteristics of novel structure and diverse varieties.
- What are the applications of building blocks in drug development?
Drug building blocks are the cornerstones of drug molecule construction. Generally, researchers in drug development companies connect these drug building blocks together to obtain new compounds through chemical synthesis. Then, a large number of experiments are carried out with the obtained new compounds for screening and optimization into promising compounds and lead compounds, so as to finally determine clinical candidates.
- What are the common types of drug building blocks?
Common drug building blocks mainly include saturated alicyclic building blocks, aromatic heterocyclic building blocks, special saturated ring building blocks, four-membered ring drug building blocks and other products.
- What are the substituted functional groups of the building block?
Our building blocks feature a wide range of functional group modifications including alcohols, alkenes, alkynes, amines, arenes, boronic acids, esters, carbonyls, fluorides, halides, nitrogen compounds, oxygen compounds, phosphorus compounds, sulfur compounds and heterocyclic building blocks.
- What role do building blocks play in new drug development?
In the development of new drugs, building blocks are mainly involved in the following steps: (1) Arbitrary combination of molecular building blocks; (2) Screening of hitting compounds (HIT); (3) Determination of lead compound (LEAD) through structural optimization; (4) Determination of clinical candidates by further optimization of lead compounds.
- Which building blocks are more popular in medicinal chemistry?
First, amines (especially secondary amines), acids, boronic acids, boronic esters are ranked highest. Second, commonly used reagents are aryl halides, alkyl or benzyl halides, aldehydes, alcohols and anilines. Finally, there are sulfonyl halides, ketones and isocyanates. Isocyanates and sulfonyl halides are useful in medicinal chemistry but are given lower priority due to instability in long-term storage. In addition, a few reagents such as hydrazine and lactams are also prioritized.
- What are the main competition barriers of molecular building blocks industry?
The main competition barrier of the molecular building blocks industry lie in the purity level and variety richness of molecular building blocks. On the one hand, companies should have strong R&D capabilities and be able to carry forward-looking stocking in a timely manner based on global new drug R&D capabilities. At the same time, enterprises should also carry out a large number of stockings to meet the one-stop purchasing needs of customers.
- What is the application scale of molecular building blocks in drug development ?
Drug molecular building blocks are mainly divided into above kilogram and below kilogram. Products below the kilogram level are mostly used in the preclinical research and development stage of new drugs for splicing and screening, and the dosage is mostly milligrams to grams. Until the drug development enters the clinical stage, the number of categories used in the screening of molecular blocks gradually shrinks, but the product dosage will quickly increase to more than kilograms.
- What are the targets of molecular building blocks?
Molecular building blocks can be widely used in most popular targets related to major fields such as cancer, cardiovascular and cerebrovascular diseases, endocrine system, antiviral, metabolism, nervous system, inflammation/immune system, etc.
- What are the synthetic techniques of molecular building blocks?
The synthesis technology of molecular building blocks mainly includes asymmetric synthesis technology, coupling reaction technology, catalysis technology, continuous reaction technology, crystal form screening technology and other technologies.
