Li Jianke, Wakefield Brian D, Ruble J Craig, Stiff Cory M, Romero Donna L, Marotti Keith R, Sweeney Michael T, Zurenko Gary E, Rohrer Douglas C, Thorarensen Atli
Medicinal Chemistry and Infectious Diseases Biology, Pharmacia Corporation, 301 Henrietta Street, Kalamazoo, MI 49001, USA.
Bioorg Med Chem Lett. 2007 Apr 15;17(8):2347-50. doi: 10.1016/j.bmcl.2006.12.055. Epub 2006 Dec 21.
Discovery of novel antibacterial agents is a significant challenge. We have recently reported on our discovery of novel antibacterial agents in which we have rapidly optimized potency utilizing a parallel chemistry approach. These advanced leads suffer from high affinity for human serum albumin (HSA). In an effort to decrease the affinity for HSA we have prepared a series of heterocyclic analogs, which retained antibacterial activity and demonstrated reduced affinity for HSA.
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