Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists |
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Authors: | Xiao Yufang Araldi Gian Luca Zhao Zhong Brugger Nadia Karra Srinivasa Fischer David Palmer Elizabeth |
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Institution: | Department of Medicinal Chemistry, EMD Serono Research Institute, Inc., Rockland, MA 02370, USA. yufang.xiao@emdserono.com |
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Abstract: | Analogs of PGE(2) with introduction of diene groups at the omega-side chain have been synthesized and evaluated for their binding affinity for EP(2) and EP(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP(4) receptor over other known receptors. |
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