ORGN 490 |
| Antagonism of the RGD binding domain of the integrin vitronectin receptor, avb3, by potent, selective, small-molecule mimetics may result in an effective treatment for osteoporosis. The evolution of small molecule RGD peptidomimetics to a centrally-constrained zwitterionic antagonist suitable for clinical development will be described. The identification of potential sites of oxidative metabolism of our clinical candidate allowed subtle structural modifications to be incorporated providing a compound with an enhanced pharmacokinetic profile. Structure-activity relationships of the series will be described as well as the synthesis of the modified clinical candidate. |
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Technical Achievements in Organic Chemistry Awards
9:30 AM-12:00 PM, Wednesday, 31 August 2005 Washington DC Convention Center -- Ballroom C, Oral
Division of Organic Chemistry |