A variety of major diseases, especially some emerging infectious diseases, such as severe acute respiratory syndrome (SARS) and "new coronavirus" present a major threat to public health. In addition to disease control and prevention, the research and development of effective therapeutic drugs is particularly important, and medicinal chemistry is the core and focus of drug research and development.

In recent years, with the rapid development of stereochemistry, life science and medicine, the chirality of drugs has attracted great attention in the development of synthetic and natural medicine. The enantiomer of some chiral drugs with identical or similar physicochemical properties has different pharmacology activity and different transport mechanism and metabolic behavior in organisms. The world-famous thalidomide incident happened in the 1960s is a profound lesson given by the abuse of chiral drugs.

Relying on "Guangzhou Biopharmaceutical Analytical Chemistry Key Laboratory "," Ministry of Health (State Administration of Chinese Medicine) Chinese Medicine and Photonics Technology Laboratory" and other scientific research platforms, the development goals of the direction of medicine chemistry are to develop new principles, methods and techniques in the fields of chiral separation materials, drug analysis, new chemical entities and asymmetric synthesis et al. Taking innovative chiral drugs as the main object, the basic and applied technology research is carried out to solve the key problems of chiral research in drug industry, and to perfect the methods and standards of chiral drug detection. After nearly ten years of efforts, the research direction of medicinal chemistry in the School of Chemistry of South China Normal University has gradually formed its own characteristics and dominant position at home and abroad, and has also made important contributions in gathering and cultivating talents, carrying out academic exchanges and transforming achievements.

The main research areas covered by this discipline are as follows:

 1、Design and development of chiral separation materials

To obtain novel chiral separation materials by using micro-nano-porous silica gel, porous inorganic, organometallic and polymeric materials as matrix materials,  and chemically bonding or coating with chiral recognition materials such as cyclodextrin, polysaccharides and biological macromolecules. The newly developed separation materials will be applied in high performance liquid chromatography, supercritical fluid chromatography and simulated moving bed chromatography to identify, analyze, detect and separate enantiomers of chiral drugs. Studies on separation, enrichment and analytical methodology of highly selective chiral drugs based on the synergistic recognition of molecular imprinting and nucleic acid aptamer will be carried out. The project “Porous silica gel matrix chiral separation materials and their applications” won the second prize of 2019 university technical invention award. More than 100 sci papers about the innovative theoretical achievements were published in Advanced Materials, Chemical Science, ACS Macro Letters and other academic journals, and the papers were cited more than 1000 times. The series of inventions have been industrialized in Guangzhou Yanchuang Biotechnology Development Co., Ltd. Chiral chromatographic packing products have broken the foreign monopoly and filled the domestic blank. Enterprises applying these products have increased more than 100 million yuan in tax profits. Meantime, the products won excellent Enterprise Award in China Innovation and Entrepreneurship Competition (Ministry of Science and Technology), ranked first in 2014; third prize in the second "Pearl River Angel Cup" Science and Technology Innovation and Entrepreneurship Competition (Guangdong Provincial Department of Science and Technology), ranked first in 2014.

2、Identification and Sustained Release of Chiral Drugs

Based on the chiral recognition technology of quartz crystal microbalance (QCM) biosensor and the selective binding of chiral drugs with chiral luminescent materials as probe, the qualitative and quantitative detection methods of target chiral drugs were established. Exclusion of background fluorescence effects, optical stability, low toxicity, fluorescence sensing devices and drug-loaded matrix that can truly track and observe the mechanism of cell differentiation for a long time in vivo. To confirm the effect of coordination between ions and functional small molecules on supramolecular recognition process, a light signal transduction sensor for hematopoietic stem cell labeling was developed. Related research work were financially supported by more than 20 research projects from the National Natural Science Foundation of China, provincial, municipal and industry research program. More than 100 SCI papers were published in academic journals, such as Biosensors and Bioelectronics, ACS Applied Materials and Interfaces, J Med Chem, Chem Commun, Journal of Agricultural and Food Chemistry etc. One group standard (GDPA1-2019) and five enterprise standards have been issued.

3、Synthesis and Crystallization Technology of Chiral Drugs

The synthesis of novel chiral catalysts, the study of asymmetric catalytic reactions and the synergistic application of crystalline chiral resolution methods are the key to reduce the production cost and implement quality control of chiral raw materials. By seeking economical and reasonable asymmetric synthesis process, the products of different crystal forms can be controlled by changing solvent, crystallization rate, crystallization mode, etc. The goal of chiral resolution can be realized, together with the dominant crystal drugs with high bioavailability can be obtained. Related research work were financially supported by four national scientific research projects and six provincial and municipal research program. More than 100 SCI papers were published in academic journals, such as Eur. J. Med. Chem., Bioorg. Med. Chem., Bioorg. Chem., Org. let., Angew. Chem. Int. Ed., J. Org. Chem., etc.

4、Marine Natural Medicinal Chemistry

Increased national strategic needs for the exploration and utilization of marine living resources call for development of new drug lead compounds from the marine organism. It is new opportunity and challenge for constructing our country's "blue drug bank" plan. The research goal of marine natural medicine chemistry is to discover new chemical entities with anti-tumor, anti-virus, anti-infection, anti-diabetic and other pharmacological activities through the investigation of secondary metabolites of marine microorganism. The structure optimization, synthesis and structure-activity relationship research of the lead compounds with novel structure and excellent biological activity will be carried out for the development of first-in-class drugs. Relevant research work is financially supported by the National Natural Science Foundation of China, provincial, municipal and industry research projects. More than 100 academic papers have been published in Org. Lett, Marine Drug, Bioorg. Med. Chem., Bioorg. Chem., J. Nat. Prod., J. Org. Chem. etc..