Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss
February 2021
in “
Journal of Medicinal Chemistry
”
The study reported the synthesis and evaluation of novel analogues of UK-5099 as mitochondrial pyruvate carrier (MPC) inhibitors to treat hair loss. Researchers explored the structure–activity relationship by modifying four positions of the hit compound. They discovered that inhibitors with a 3,5-bis(trifluoromethyl)benzyl group at the N1 position showed superior activity compared to JXL001 (UK-5099) in increasing cellular lactate production. Analogue JXL069, featuring a 7-azaindole heterocycle, also demonstrated significant MPC inhibition, expanding the potential for drug design. Over 10 analogues were tested on shaved mice through topical treatment, resulting in noticeable hair growth.
