Researchers Synthesize Compounds For New Class Of Antibiotics

In a recent issue of the Journal of Organic Chemistry, the research team reported that they have chemically synthesized myxopyronin A and B, two natural compounds known to block replication of drug-resistant strains of bacteria. Before this breakthrough, the compounds could only be isolated from their bacterial source, a process that yielded quantities too small to be usable.

From a therapeutic standpoint, the compounds look particularly promising because of their selectivity. Harmful bacteria contain DNA-dependent polymerase enzymes, as do humans. Myxopyronin A and B attack the bacterial enzymes while leaving the human host alone.

In recent years, the incidence of infectious diseases has soared, along with deaths resulting from them. At the same time, the need for new antibiotics has risen steadily as bacteria have developed a resistance to existing drugs. The worldwide market for anti-infective drugs is now estimated to be $34 billion, and it is still growing.

"This is an exciting opportunity for the development of a new type of antibiotic," says James Panek, a professor of chemistry who led Boston University's participation in the project. "The chemical synthesis provides us with the means for generating the materials that can lead to new pharmaceuticals."

Scriptgen, a Waltham, MA, company that develops drugs to control the expression of genes, is now developing the processes for converting the raw materials of myxopyronin A and B into viable antibiotics.

"This is a significant breakthrough from a chemistry point of view, but it's the first step in the process, " said Michael G. Palfreyman, Vice President of Research and Development at Scriptgen. "Now we need to take myxopyronin and make it more drug-like. The synthesis was designed to allow us to make many analogs--many different candidates--so that doctors can choose the best one for the desired activity."