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Different Groups of Precursor Drug Design Services

Drug solubility is an important factor affecting oral absorption of solid preparations. In general, solid oral preparations can be absorbed only after the drug is dissolved. Poor drug solubility will lead to poor ADME process, which will lead to low oral bioavailability, poor chemical stability, difficult prescription optimization and other problems. Precursor drugs are pharmacologically inactive molecules that require enzyme or chemical transformation to release the active parent drug in the body for its pharmacological effects. Prodrug design is a method to improve the physical and chemical properties of drugs, which can improve the permeability, solubility, bioavailability and chemical stability of drugs. For a long time, CD Formulation has been committed to providing customers with high quality pharmaceutical formulations, and has also been active in providing customers with solutions for drug development, especially in terms of improving bioavailability and solubility.

Crystal structure of binding mode of compound etravirine to reverse transcripatase

Our Services

Based on prodrug design concepts, CD Formulation offers the following three services to improve drug bioavailability:

Sulfonyl Prodrug Design Services

Sulfonyl groups have unique physical and chemical properties. The introduction of sulfonyl groups can regulate the solubility and acidity of small molecules. Sulfonyl groups can provide two hydrogen bond receptors. Proper introduction of sulfonyl groups can improve the biological activity of compounds by increasing hydrogen bond interactions between small molecules and the target. Sulfonyl group structure is relatively stable, the introduction of sulfonyl group can improve the stability of drug metabolism by blocking the easy metabolic site, prolong its action time, improve its bioavailability, and thus improve the pharmacokinetic properties of small molecules.

Cyanide Prodrug Design Services

Introducing cyano-group into small molecule drugs can effectively enhance the interaction between target protein and ligand. In the development of many drug small molecules, the introduction of cyanide groups can significantly improve the binding ability between small molecules and target proteins, mainly through hydrogen bond interaction, covalent bond interaction, dipole interaction and π-π interaction.

Methyl Prodrug Design Services

The introduction of methyl into small molecules changes the physicochemical properties of drugs by affecting lipid solubility and water solubility. The pharmacodynamic properties of drugs are influenced by induction effect, change of molecular conformation and change of protein-ligand interaction. The metabolic properties of drugs are affected by ortho-effect, weak metabolism, and increased stability.

The Advantages of Our Services

The advantages of CD Formulation for different groups of precursor drug design services

How to Contact Us?

If you have a requirement about our services, please contact us by phone or email, our colleagues will reply to you within three working days.

Reference

  1. Barreiro, EJ.; et al The methylation effect in medicinal chemistry [J]. Chem Rev, 2011, 111: 5215−5246

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