噻二唑类作为一类新型强效和选择性磷酸二酯酶7（PDE7）抑制剂的发现。第1部分：设计、合成及构效关系研究。
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
作者信息
Vergne Fabrice, Bernardelli Patrick, Lorthiois Edwige, Pham Nga, Proust Emmanuelle, Oliveira Chrystelle, Mafroud Abdel-Kader, Royer Frederique, Wrigglesworth Roger, Schellhaas Jennifer, Barvian Mark, Moreau François, Idrissi Moulay, Tertre Anita, Bertin Bernadette, Coupe Magali, Berna Patrick, Soulard Patricia
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):4607-13. doi: 10.1016/j.bmcl.2004.07.008.
The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4.
讨论了一系列结构新颖的磷酸二酯酶7（PDE7）小分子抑制剂的合成及构效关系（SAR）研究。该系列中最佳的化合物表现出低纳摩尔级的抑制活性，并且对磷酸二酯酶4（PDE4）具有选择性。
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