LA JOLLA, CA August 24, 2011 A team of scientists from The Scripps Research Institute have successfully reengineered an important antibiotic to kill the deadliest antibiotic-resistant bacteria. The compound could one day be used clinically to treat patients with life-threatening and highly resistant bacterial infections.
The results were published in an advanced online issue of the Journal of the American Chemical Society.
"[These results] have true clinical significance and chart a path forward for the development of next generation antibiotics for the treatment of the most serious resistant bacterial infections," said Dale L. Boger, who is Richard and Alice Cramer Professor of Chemistry at The Scripps Research Institute and senior author of the new study. "The result could not be predicted. It really required the preparation of the molecule and the establishment of its properties."
The compound synthesized is an analogue of the well-known commercial antibiotic vancomycin.
The new analogue was prepared in an elegant total synthesis, a momentous achievement from a synthetic chemistry point of view. "In addition to the elegantly designed synthesis," said Jian Xie, postdoctoral fellow in Boger's group and first author on the publication, "I am exceedingly gratified that our results could have the potential to be a great service to mankind."
A Single Atom Changes Everything
Vancomycin is an antibiotic of last resort, which is used only after treatment with other antibiotics has failed. Clinically, it is used to treat patients that are either infected with the virulent methicillin-resistant Staphylococcus aureus (MRSA), individuals on dialysis, or those allergic to beta-lactam antibiotics (penicillin, cephalosporins).
The drug was first used clinically in the 1950s, and the first vancomycin-resistant bacterial strains were isolated in the 1980s.
Vancomycin normally works
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Scripps Research Institute