arylomycin a2

Arylomycin A2 is a synthetic antibiotic belonging to the arylomycin class of lipopeptides. It features a complex cyclic structure with a 14-membered macrocycle and an N-methylated peptide core linked to a lipopeptide tail[5][8]. Its primary mechanism of action is the inhibition of bacterial type I signal peptidase (SPase I), an enzyme essential for protein maturation in bacteria[4][7]. By blocking SPase I activity at its active site through competitive binding, arylomycin A2 disrupts protein processing and leads to bacterial cell death[5][7]. This compound exhibits potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pneumoniae; it shows limited activity against Gram-negative bacteria unless their outer membrane is compromised[7]. The drug has attracted research interest due to its novel target and potential utility in combating antibiotic-resistant infections. It was first synthesized by researchers at The Scripps Research Institute using Suzuki–Miyaura cross-coupling chemistry for biaryl bond formation[8].

Other names

arylomycin a2(8S,11S,14S)-3,18-dihydroxy-14-[[2-[[(2R)-2-[[(2R)-3-hydroxy-2-[methyl(10-methylundecanoyl)amino]propanoyl]amino]propanoyl]amino]acetyl]-methylamino]-11-methyl-10,13-dioxo-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2,4,6(20),15(19),16-hexaene-8-carboxylic acid