Discovery of an 8-aza-5-thiaProstaglandin E1 analog as a highly selective EP4 receptor agonist.
作者： Tohru Kambe , Toru Maruyama , Atsushi Naganawa , Masaki Asada , Akiteru Seki
DOI: 10.1248/CPB.59.1494
关键词:
摘要: For the purpose of discovering an orally available EP4 subtype-selective agonist, a series 8-aza prostaglandin E1 (PGE1) analogs were synthesized and evaluated for their affinity PGE2 receptor subtypes. Additionally, structure–activity relationships these compounds studied. Among tested compounds, PGE1 analog 6 8-aza-5-thiaPGE1 12 had highly potent affinity, good functional activity, excellent subtype-selectivity. Furthermore, demonstrated stability in human liver microsomes. As result, we concluded that two could be promising chemical leads agonist.
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