Design and synthesis of indolo[2,3-a]quinolizin-7-one inhibitors of the ZipA-FtsZ interaction.
作者信息
Jennings Lee D, Foreman Ken W, Rush Thomas S, Tsao Desiree H H, Mosyak Lidia, Li Yuanhong, Sukhdeo Mohani N, Ding Weidong, Dushin Elizabeth G, Kenny Cynthia Hess, Moghazeh Soraya L, Petersen Peter J, Ruzin Alexey V, Tuckman Margareta, Sutherland Alan G
机构信息
Wyeth Research, Department of Medicinal Chemistry, 401N. Middletown Rd, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2004 Mar 22;14(6):1427-31. doi: 10.1016/j.bmcl.2004.01.028.
The binding of FtsZ to ZipA is a potential target for antibacterial therapy. Based on a small molecule inhibitor of the ZipA-FtsZ interaction, a parallel synthesis of small molecules was initiated which targeted a key region of ZipA involved in FtsZ binding. The X-ray crystal structure of one of these molecules complexed with ZipA was solved. The structure revealed an unexpected binding mode, facilitated by desolvation of a loosely bound surface water.
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