Pratt L M, Beckett R P, Davies S J, Launchbury S B, Miller A, Spavold Z M, Todd R S, Whittaker M
British Biotech Pharmaceuticals Limited, Watlington Road, Cowley, Oxford OX4 6LY, UK.
Bioorg Med Chem Lett. 2001 Oct 8;11(19):2585-8. doi: 10.1016/s0960-894x(01)00509-1.
By screening a library of metalloenzyme inhibitors, the N-formyl-hydroxylamine derivative BB-3497 was identified as a potent inhibitor of Escherichia coli peptide deformylase with antibacterial activity both in vitro and in vivo. The homochiral synthesis of BB-3497, involving a novel asymmetric Michael addition reaction is described.
通过筛选金属酶抑制剂文库，N-甲酰基羟胺衍生物BB-3497被鉴定为大肠杆菌肽脱甲酰基酶的有效抑制剂，在体外和体内均具有抗菌活性。本文描述了BB-3497的纯手性合成，其中涉及一种新型不对称迈克尔加成反应。
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