from the how-to-make-a-heavy-methyl-band dept.
For years, drug discovery chemists have struggled to streamline a process that can boost a drug's potency up to 2000-fold: "magic methylation." The reaction sweeps out single hydrogen atoms and replaces them with methyl groups—reshaping the drug molecule to more easily interact with its biological targets. But carrying out this sleight of hand is so difficult that few researchers even try. Now, a team of chemists reports it has created a new catalyst that performs this delicate exchange with ease on a wide variety of druglike molecules, an advance that could lead to novel treatments for everything from cancer to infectious diseases.
"This paper is just stunning," says Tim Cernak, an organic chemist at the University of Michigan, Ann Arbor, who was not involved in the research. The new catalyst manages the reaction in one easy step—a huge improvement on previous multistep methods that were expensive and time-consuming. "This is the wish [of] every drug hunter," Cernak says. "It really is a dream reaction."
[...] This could help "across the board" in drug discovery, says David Rees, chief scientific officer of Astex Pharmaceuticals. Where adding a methyl group does increase a drug's potency, doctors may be able to give their patients less of a drug. That could improve safety and reduce side effects. Among the drugmakers he knows, Rees says, "Everyone will jump on this."
Posted in: Chemistry DOI: 10.1126/science.abb7567.