Novel Thiostrepton Analogs with Improved Solubility
Novel Thiostrepton Analogs with Improved Solubility
Thiostrepton (shown to the right) is a natural product with potent activity against Gram positive bacteria, including MRSA. Clinical use of Thiostrepton in humans however is precluded by the compound’s poor aqueous solubility.
Using a novel chemistry approach, a series of semi-synthetic analogs has been generated. Evaluation of these analogs demonstrates that increased solubility can be achieved while retaining antibacterial activity (table to right).
Additional analogs are under evaluation with the aim of optimizing solubility and potency for clinical utility of this compound class.
