Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles

详细信息    查看全文

• 作者：Jianke Li ; Brian D. Wakefield ; J. Craig Ruble ; Cory M. Stiff ; Donna L. Romero ; Keith R. Marotti ; Michael T. Sweeney ; Gary E. Zurenko ; Douglas C. Rohrer ; Atli Thorarensen
• 关键词：Anthranilic acid ; Antibacterial ; Protein binding ; Human serum albumin
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 April 2007
• 年：2007
• 卷：17
• 期：8
• 页码：2347-2350
• 全文大小：148 K

文摘

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.