An article about fluorine #memo #medchem #journal

Recently there are many drugs that contain fluorine atom. Fluorine atom is often used in medicinal chemistry to improve potency, metabolic stability reduce toxicity etc. And the recent progress of chemistry enable to introduce fluorine atoms in many position of molecule. You know, there are many fluorination reagents.

Fluorine atom is familiar to medicinal chemists, of course I try to introduce fluorine atoms when I design new molecules.

Today, I read very useful article about fluorine atoms in drug discovery. URL is below.

https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00235

The author shows some example of instability of fluorine containing drugs.

Fig1 and 2 shows an example of instability of F containing compounds. Fluorine substituted alkyl has risk of F- releases and produce reactive metabolite.

The substitution and elimination mechanism of fluorine atom is based on organic chemistry. So medicinal chemist can predict it I think.

F atoms are very useful for drug design so drug designer need to think about not only potency, ADMET profile but also stability of designed compounds.

Chemistry is exciting!