Macrolides (MALs) Hapten Design and Synthesis

Macrolides are a class of protein synthesis inhibitors with wide clinical application value. Since the earliest macrolide erythromycin was discovered in 1950, in order to obtain compounds with better availability and acid stability in medical applications, scientists have continuously synthesized new macrolide derivatives. However, most of the improvements are accompanied by severe side effects. In recent years, the development of hapten technology has introduced a new chemical platform for the synthesis and discovery of a variety of macrolide antibiotics. Creative Biolabs, through the assembly and assembly of simple chemical structural units, has established a highly efficient macrolide antibiotic design scheme and synthetic pathway, which represents the renaissance of macrolide drugs, helping researchers to develop new and safe therapeutic agents and enhance hope for a fight against serious human infectious diseases.

Summary of macrolide antibiotic development by semisynthesis. Fig.1 Summary of macrolide antibiotic development by semisynthesis. (Seiple, 2016)

Introduction of Macrolides

Natural products are the main source of most antibacterial drugs today, providing us with a large number of antibiotics for medical use. However, natural products are generally defective in terms of safety and efficacy. At present, the main means of discovering and manufacturing new antibiotics is semi-synthetic or chemical modification of natural products derived from fermentation. Macrolide antibiotics have been proven to be safe and effective for the treatment of infectious diseases in humans. They generally have one or more side glycoside residues and have the potential for modification. Most of the current macrolide antibiotic products are manufactured by chemically modifying erythromycin, but erythromycin cannot be stably present in the human body and is easily rearranged to produce side effects. Creative Biolabs designs and prepares macrolide haptens through synthetic methods. We confer antigenicity through subsequent European Union modification, making it a reliable tool for antibody production. We can currently provide the following services:

  • Design and Synthesis of Haptens for Tylosin
  • Tylosin is a macrolide antibiotic obtained from the culture medium of Streptomyces macrophages. It has an extensive antibacterial spectrum. It is widely used to treat bacterial infections in various animals, including beef cattle, pigs, and poultry. However, tylosin has a low metabolic rate after administration, and its residues are widely distributed in the body fluids and tissues of livestock. Long-term intake will bring potential risks to human health.

    Creative Biolabs provides hapten design and synthesis services that mimic tylosin to the greatest extent. Our reasonably designed hapten highly overlaps with the target molecule in the three-dimensional structure and brings stable immunogenicity to induce an immune response. It is possible to immunize mice through different hapten strategies to prepare and screen high-quality monoclonal antibodies.

  • Design and Synthesis of Haptens for Tilmicosin
  • Tilmicosin is a semi-synthetic derivative of tylosin and tylosin. Its antibacterial spectrum is similar to tylosin, but its bactericidal effect on gram-negative bacteria, mycoplasma, and pasteurization is better than tylosin. Tilmicosin can be used to control mycoplasma avian influenza and mastitis in lactating cattle. With the maturation of our hapten synthesis technology, haptens for tilmicosin designed by Creative Biolabs are more similar in properties to their targets, have stable immunogenicity, and can produce more specific antibodies.

If you want to inquire more about the design and synthesis of macrolide haptens, please contact us.


  1. Seiple, I, B.; et al. A platform for the discovery of new macrolide antibiotics[J]. Nature. 2016, 533(7603): 338-345.
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