Synthesis and Structure-Activity Relationship Study of Novel Nitrodiphenylurea Antibiotics

According to the World Health Organization, tuberculosis (TB) is the leading cause of death by infectious disease. Tuberculosis is caused by the bacteria Mycobacterium tuberculosis and occurs globally. Additionally, in 2017, TB was reported in all 50 states. Due to the scope of TB, strict observation of patients is required to ensure adherence to the current drug regimen. However, most reported cases are in developing countries where proper care is difficult. With the emergence of multidrug-resistant TB exhibiting resistance to current treatments, novel antibiotics are needed. Recently, our lab discovered a family of diphenyl ureas that exhibit antimicrobial activity against several bacterial strains, including Mycobacterium. Based on our lab’s previous results, we have synthesized several diphenyl urea derivatives to examine their structure-activity relationship. Herein, we report the synthesis of the diphenyl ureas with varying nitro positions, chain-lengths, and sites of variation