Small-Molecules as Antibiotic Potentiating Agents

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Introduction: Antibiotic resistance is one of the biggest challenges to global public health. The Centers for Disease Control and Prevention reported that at least 2.8 million people become infected with antibiotic-resistance bacteria in the United States each year, and more than 35,000 people die as a result. Continued overuse of antibiotics can contribute to increasing the risk of antibiotic resistance. When resistance develops, there are few treatment options and, in some severe cases, no treatment options. The current strategy to address these challenges involves either developing new antibiotics and new molecules or modifying existing ones. This technology provides an alternative combination treatment approach to potentiate the effects of existing known antibiotics and reduce bacterial resistance. Technology: Georgia State University inventors have identified small molecules to sensitize bacteria toward existing antibiotics. Inventors synthesized more than 20 di-amidine compounds and screened their antibacterial activity in the presence of traditional antibiotics. The lead di-amidine compound showed broad-spectrum activity against a host of bacterial strains. These compounds themselves have limited antibacterial activity. However, experiments have shown that the lead compound sensitizes both Gram-positive and Gram-negative bacteria by up to 30-fold towards traditional antibiotics, including erythromycin, novobiocin, tetracycline, and chloramphenicol. These di-amidine compounds work as antibiotic adjuvants to lower the antibiotic doses and to re-sensitize resistant bacteria towards traditional antibiotics.