Synthesis and biological evaluation of a C5-biphenyl thiolactomycin library

Fifteen novel C5 analogues of thiolactomycin have been synthesised and assessed for their in vitro mtFabH and in vivo Mycobacterium bovis BCG activity, respectively. The biological analysis of this library reaffirms the requirement for a linear π-rich system containing hydrogen bond accepting substituents attached to the para-position of the C5 biphenyl analogue to generate compounds with enhanced activity.