稠合四氢异喹啉-亚氨基咪唑啉的设计与合成
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines.
作者信息
Moas-Héloire Valeria, Renault Nicolas, Batalha Vania, Arias Angela Rincon, Marchivie Mathieu, Yous Said, Deguine Noémie, Buée Luc, Chavatte Philippe, Blum David, Lopes Luisa, Melnyk Patricia, Agouridas Laurence
机构信息
Université de Lille, F-59000 Lille, France; UDSL, EA 4481, UFR Pharmacie, F-59000 Lille, France.
Instituto de Medecina Molecular, 1640-028, Lisbon, Portugal.
出版信息
Eur J Med Chem. 2015 Dec 1;106:15-25. doi: 10.1016/j.ejmech.2015.10.030. Epub 2015 Oct 19.
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolines" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
为了鉴定新的优势结构，我们描述了由四氢异喹啉-乙内酰脲核心衍生的环状胍化合物“四氢异喹啉-亚氨基咪唑啉”的五步合成法。为了评估这种新的最小结构以及用胍部分取代羰基的影响，我们评估了它们对腺苷A2A受体的亲和力，并与四氢异喹啉-乙内酰脲化合物的亲和力进行了比较。
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