Multidrug-resistant tuberculosis (MDR-TB) and extensively drug resistant TB (XDR-TB) are a significant public health threat for TB control efforts. Despite efforts in last 50 years, development of new TB treatments have been limited to drug targets like cell wall biosynthesis, ATP synthesis, RNA synthesis, leading to resistance in these areas. Hence, there is a need to discover novel drugs that target other bacterial processes in order to counter the developed bacterial resistance.
Researchers at Stony Brook University have focused their drug discovery program on the bacterial septum formation and cell division protein, FtsZ. The researchers have developed novel 3rd generation trisubstituted benzimidazoles directed against FtsZ of M. tuberculosis H37Rv and the lead compound, SB-P17G-A38, shows efficacy equivalent to Isonaizid in an acute mouse model of M. tuberculosis (Figure 1). Additionally, the 3rd generation benzimidazoles improved human and mouse plasma and metabolic stability when compared to the previous lead. Together, these studies demonstrate that SB-P17G-A38 has potency against M. tuberculosis clinical strains, and that trisubstituted benzimidazoles continue to be a platform for the development of novel inhibitors with efficacy.
-Novel mechanism of action -Improved plasma and metabolic stability -Can be used in combination therapy -Bactericidal
- Antibacterial, including Tuberculosis
Iwao Ojima, Distinguished Professor, Chemistry
Seung-Yub Lee, Lab. Director, Chemistry
Available for Licensing
Sean Boykevisch, Director, Intellectual Property Partners, firstname.lastname@example.org, 6316326952
Issued patents: US (8,232,410), EU, Japan, South Africa, Mexico, Canada.