Simple new platform for creating antibiotics developed

Scientists have created a new, simplified platform for antibiotic discovery that can lead to the development of new medicines and also help fight bacteria which are resistant to existing drugs.
Researchers developed a platform where they assemble eight (chemical) building blocks by a simple process to make macrolide antibiotics - which inhibit the growth of bacteria - without using erythromycin, the drug upon which all others in the class have been based since the early 1950s.
Erythromycin, which was discovered in a soil sample from the Philippines in 1949, has been on the market as a drug by 1953.
"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 G Myers, professor at the Harvard University.

"That process is semisynthesis, modifying the naturally occurring substance," Myers said.
In contrast, the process described in the new study involves using "eight industrial chemicals, or substances derived from them," Myers said, 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, the researchers said.
"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, two of the 350 compounds reported on in the study have, in initial testing, shown efficacy against a bacterium that has become resistant to vancomycin, which is known as the antibiotic of last resort, he said.
Some of the 350 compounds reported on in the study will undergo more extensive testing to evaluate their potential as candidate drugs.
The study was published in the journal Nature.