Fig. 1. Analogs of armeniaspirol to probe antibiotic activity via inhibition of ClpXP and ClpYQ (A) 5-chloroarmeniaspirol inhibits the ATP-dependent proteases ClpXP and ClpYQ in Gram-positive bacteria, which dysregulates the divisome and leads to cell division arrest. (B) Summary of structure–activity relationships for armeniaspirol. Functional groups highlighted in blue are essential for antibiotic activity. R indicates sites amenable to substitution. (C) 5-chloroarmeniaspirol sites R1 and R2 were selected for detailed structure–activity relationship.
