Chemical synthesis breakthrough holds promise for future antibiotics
5 replies, posted
https://www.colorado.edu/today/2018/12/20/chemical-synthesis-breakthrough-holds-promise-future-antibiotics
Antibiotic-resistant infections afflict over 2 million people annually
and result in over 23,000 deaths in the U.S. each year, according to the
Centers for Disease Control and Prevention (CDC). A 2018 study by the
CDC’s European counterpart found that drug-resistant superbugs were
responsible for 33,000 deaths across Europe in 2015.
I'd hate to be a downer because I think the chemistry is really cool and could have applications for many other things, but I'm pretty sure that total synthesis has never been used to produce complex molecules in any kind of industrial scale. And before we get ahead of ourselves, I don't know if this has even been tested in animals, just cell lines. I don't have an issue with any of the researchers, just the people marketing the research.
Off the top of my head, carbapenems are fully synthetic. I'm quite sure there are other "complex" drugs that are fully synthetic as well, including those that were derived from natural products.
This particular reaction is more for exploratory chemistry than production. When you're trying to find a new drug, you whip up a bunch of variants on one core idea - in this case, the idea was "some kind of thiopeptide to use against MRSA", and so you'd want to synthesize as many variants as you can, and test them. What they've done here is made thiopeptide total synthesis easy enough that you could feasibly synthesize a few hundred at lab scale. Test them all and that shows you which ones you should take to trials, and if that goes well, bring it to a process chemist to optimize for widescale production.
They do make some claims about the new reaction being potentially useful at full scale. Indeed, metal-catalyzed reactions are pretty nice for industrial-scale chemistry, so I'm not inclined to disagree with them. So they've taken a step that previously was too slow for even bench chemistry, and turned it into something that might even get used at scale. The final drug won't be a total synthesis, of course, but this step might remain.
I don't fully understand a lot of the chemistry stuff in this thread, but on the face of it this seems like a pretty neat development - here's hoping it pays off with something actionable.
Im happy for the progress but you should always be wary of media articles reporting on papers
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