天然物をリードとした創薬

抄録

FR139317, the potent endothelin A receptor (ET_A) antagonist, was designed and synthesized using NMR conformational analysis of WS7338B, ET_A antagonist isolated from Streptomyces sp.
FR167233, the potent inhibitor against type II phospholipase A₂ (PLA₂), was synthesized based on the structure of WA8242B, the inhibitor isolated from Streptomyces sp., using the computational structural analysis of the complex of type II PLA₂ and WA8242B.
The strategies for the drug design of FR139317 or FR167233 can be applied for increasing number of natural products as the advancement of organic chemistry.