螺喹唑啉酮类化合物作为新型、强效且选择性的磷酸二酯酶7抑制剂。第1部分。
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
作者信息
Lorthiois Edwige, Bernardelli Patrick, Vergne Fabrice, Oliveira Chrystelle, Mafroud Abdel-Kader, Proust Emmanuelle, Heuze Lamia, Moreau François, Idrissi Moulay, Tertre Anita, Bertin Bernadette, Coupe Magali, Wrigglesworth Roger, Descours Arnaud, Soulard Patricia, Berna Patrick
机构信息
Pfizer Global Research and Development, 3-9 rue de la Loge 94265 Fresnes, France.
出版信息
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4623-6. doi: 10.1016/j.bmcl.2004.07.011.
PMID:15324876
Abstract
The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes.
摘要
本文讨论了新型磷酸二酯酶7（PDE7）抑制剂螺喹唑啉酮的合成及构效关系研究。该系列中最佳化合物表现出纳摩尔级的抑制亲和力，且对其他PDE同工酶具有选择性。
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