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Recently, bioorganic chemistry has been applied to the broad fields of medicine and health sciences. The isolation and synthesis of useful bioorganic compounds interacting with biomolecules and affecting humans have contributed more to life sciences. Some bioorganic compounds interrupt pathogens including viruses and bacteria, etc., and can be used as drugs against them. Furthermore, recent developments in bioinformatics have enabled us to design therapeutic drugs targeting pathogens. In addition, some isolated bioorganic compounds from plants and bacteria are known to affect cell metabolism and the immune system and improve health and nutrition. Therefore, bioorganic chemistry and its related fields provide useful tools for exploring strategies for the sick and the welfare of communities. To discuss this special topic, scientists employing various approaches to study bioorganic chemistry for medicine and health sciences are invited. I am glad to have the honor to organize a Special issue for Mini-Reviews in Organic Chemistry and to experience working with eminent scientists to review research on Bioorganic Chemistry. This issue includes articles on the following topics: bioorganic molecules produced by fungi written by Dr. Megumi Kuba-Miyara and Prof. Masaaki Yasuda, recent studies on anti-influenza A virus drugs written by Drs. Kunihiro Kaihatsu and Dale L. Barnard, recent development of small-molecule HIV inhibitors written by Norihito Kawashita and colleagues, analysis of infection route of prion in intestine using inhibitor of Fc receptor written by Dr. Ryuta Uraki and colleagues. Hopefully, readers will enjoy this issue, obtain useful information for their own research, and be inspired with new ideas for future research on bioorganic chemistry.