Gleave D M, Brickner S J, Manninen P R, Allwine D A, Lovasz K D, Rohrer D C, Tucker J A, Zurenko G E, Ford C W
Pharmacia & Upjohn, Kalamazoo, MI 49001, USA.
Bioorg Med Chem Lett. 1998 May 19;8(10):1231-6. doi: 10.1016/s0960-894x(98)00194-2.
A series of conformationally restricted, [6,5,5] and [6,6,5] tricyclic fused oxazolidinones were synthesized and tested for antibacterial activity. Several compounds in the trans-[6,5,5] series demonstrated potent in vitro and in vivo activity. This work provides valuable information regarding the preferred conformational orientation of the oxazolidinones at the binding site.
合成了一系列构象受限的[6,5,5]和[6,6,5]三环稠合恶唑烷酮,并对其抗菌活性进行了测试。反式-[6,5,5]系列中的几种化合物表现出强大的体外和体内活性。这项工作提供了有关恶唑烷酮在结合位点的优选构象取向的有价值信息。