Harvard chemists create new platform for antibiotic discovery

Researchers have created a new, simplified, platform for antibiotic discovery that may go a long way in solving the crisis of antibiotic resistance.

Harvard researchers have created a new, simplified, platform for antibiotic discovery that may go a long way in solving the crisis of antibiotic resistance. This is a platform where we assemble eight (chemical) building blocks by a simple process to make macrolide antibiotics without using erythromycin, the original macrolide antibiotic, and the drug upon which all others in the class have been based since the early 1950s, the researchers said. Erythromycin, which was discovered in a soil sample from the Philippines in 1949, has been on the market as a drug by 1953. Keep in mind these 10 things when you are on antibiotics.

For 60 years chemists have been very, very creative, finding clever ways to 'decorate' this molecule, making changes around its periphery to produce antibiotics that are safer, more effective, and overcome the resistance bacteria have developed, said Andrew Myers, professor of chemistry at Harvard University. That process is semisynthesis, modifying the naturally occurring substance, Myers noted.

In contrast, the process described in the new study involves using eight industrial chemicals, or substances derived from them, and manipulating them in various combinations and then testing the products against panels of disease causing bacteria. This allows us to make new "new compounds in fewer steps than was previously possible," Myers explained. The study was published in the journal Nature. One of the things that's quite encouraging about the data in our paper is that some of the structures we've made are active against clinical bacterial strains that are resistant to every known macrolide, Myers said. In fact, he added, two of the 350 compounds reported on in the paper have, in initial testing, shown efficacy against a bacterium that has become resistant to vancomycin, which is known as the antibiotic of last resort. And if you have a bug that's resistant to vancomycin, you're in trouble, Myers added.