Bernardelli Patrick, Lorthiois Edwige, Vergne Fabrice, Oliveira Chrystelle, Mafroud Abdel-Kader, Proust Emmanuelle, Pham Nga, Ducrot Pierre, Moreau François, Idrissi Moulay, Tertre Anita, Bertin Bernadette, Coupe Magali, Chevalier Eric, Descours Arnaud, Berlioz-Seux Françoise, Berna Patrick, Li Mei
Pfizer Global Research and Development, 3-9 rue de la Loge 94265 Fresnes, France.
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4627-31. doi: 10.1016/j.bmcl.2004.07.010.
The optimization of 5,8-disubstituted spirocyclohexane-quinazolinones into potent, selective, soluble PDE7 inhibitors with acceptable in vivo pharmacokinetic parameters is presented.
本文介绍了将5,8-二取代螺环己烷喹唑啉酮优化为具有良好体内药代动力学参数的强效、选择性、可溶性磷酸二酯酶7(PDE7)抑制剂的过程。