PKS13 Inhibitors - Coumestan Derivatives

Compounds 41, 42
Chemical Class:
Benzofuran derivatives
Name of Target:
Polyketide synthase (pks13)

Whole-cell based high-throughput screen with aerobically grown Mtb H37Rv. MIC = 0.125 - 0.25 ug/ml  From Abstract:  Used "structurally related benzofurans with the aim to improve their potency and bioavailability. Herein, we report our preliminary structure−activity relationship studies around this scaffold, highlighting a natural product-inspired cyclization strategy to form coumestans that are shown to be active in serum inhibition titration assays."