发现选择性吲哚类前列腺素 D₂受体拮抗剂。
Discovery of selective indole-based prostaglandin D₂ receptor antagonist.
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.
出版信息
Bioorg Med Chem. 2011 Aug 1;19(15):4574-88. doi: 10.1016/j.bmc.2011.06.014. Epub 2011 Jun 16.
PMID:21737285
Abstract
A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D₂ receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure-activity relationship study is presented.
摘要
合成了一系列 N-苯甲酰基-2-甲基吲哚-3-乙酸，并将其作为前列腺素（PG）D₂受体拮抗剂进行了生物学评价。一些选定的化合物在口服给药后可显著抑制豚鼠结膜卵清蛋白（OVA）诱导的血管通透性。呈现了构效关系研究。
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