| Drug Discovery from Natural Products |
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* Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd. (5-2-3 Tokodai, Tsukuba 300-2698, Japan) |
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FR139317, the potent endothelin A receptor (ETA) antagonist, was designed and synthesized using NMR conformational analysis of WS7338B, ETA 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. | ||
| Key words: Natural products, Endothelin antagonist, PLA2 inhibitor, Conformational analysis, Structure-activity relationships | ||
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