Mycophenolate mofelite (MMF), an immunosuppressant and prodrug of mycophenolic acid (MPA), is used extensively in transplant medicine and more specifically after bone marrow transplantation to prevent acute rejection and other severe complications such as mucositis. Despite extensive research, a mucositis-specific pain treatment has yet to be developed in order to improve the conditions of patients treated by chemo- and radiotherapy. Herein, we present the synthesis of a small series of isobenzofuran analogues identified during a screening campaign as possible mucositis mediators