Professor Rod Andrade of Temple University will be speaking on November 2, 2016 at 4:10 PM in Neville Hall, Room 003.
"Discovery of Novel Macrolide Antibiotics"
There is an urgent need to discover new drugs to address the pressing problem of antibiotic resistance. This talk chronicles a 10-year hypothesis-driven journey aimed at the discovery and development of novel antibiotics that address resistance. The first part of the talk deals with the synthesis and biological evaluation of desmethyl analogues 4-7 of the FDA-approved ketolide antibiotic telithromycin (3), which itself is synthesized from clarithromycin (2) and ultimately derived from the flagship macrolactone glycoside (macrolide) antibiotic, erythromycin (1).
The second part of the talk discusses our discovery and application of the bacterial ribosometemplated in situ click synthesis of solithromycin, which is the best-in-class ketolide antibiotic currently in Phase III clinical trials. It is the most potent macrolide antibiotic discovered to date and serves as a benchmark in terms of potency and selectivity. We have demonstrated the ribosome is capable of selectively templating the synthesis of its own inhibitor, thus opening new vistas for antibiotic discovery.