ORGN 470 |
| Bioactive microbial natural products have a wide range of new skeletons and diverse and unique biological activities. This is creating a potentially lucrative source of promising candidates for new drugs. The Kitasato Institute has been discovering over 340 novel bioactive microbial metabolites. Among them, 16 compounds are commercially important biological reagents and 6 compounds are globally-used medicines. Avermectin (or its derivative, ivermectin) is the most effective, broad-spectrum antiparasitic ever developed. Used as an anthelmintic in animal health, it has been donated free for human use and is being used to eliminate River Blindness and Elephantiasis from Africa and South America. Furthermore, erythromycin (EM), a macrolide antibiotic, shows strong gastrointestinal motor stimulating (GMS) activity, that is a agonist of gastrointestinal hormone, motilin. A series of EM derivatives were synthesized under unique reversed conception to search for a “Motilide” defined as motilin-like macrolide with potent GMS activity. This is now on phase II trial. |
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Modern Natural Products Chemistry and Drug Discovery
1:25 PM-5:00 PM, Wednesday, 29 March 2006 Georgia World Congress Center -- C303/304/305, Oral
Division of Organic Chemistry |