Structural comparison between type I and type II antagonists: possible implications in the drug design of AT1 antagonists

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• 作者：Roumelioti ; Panagiota ; Tselios ; Theodoros ; Alexopoulos ; Konstantinos ; Mavromoustakos ; Thomas ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2000
• 出版时间：April, 2000
• 年：2000
• 卷：10
• 期：8
• 页码：755-758
• 全文大小：216 K

文摘

Analogues of sarilesin (type I AT1 antagonists), and sarmesin (type II AT1 antagonists) with homoserine (hSer) at position 8 were prepared and bioassayed. The presence of a Tyr⁴-Ile⁵-His⁶ bend found in sarmesin but not in sarilesin was identified. The obtained results coupled with conformational analysis studies, using a combination of NMR spectroscopy and computational chemistry, propose important conformational and stereoelectronic properties for agonist and antagonist activity at AT1 receptors.