Jain R, Sundram A, Lopez S, Neckermann G, Wu C, Hackbarth C, Chen D, Wang W, Ryder N S, Weidmann B, Patel D, Trias J, White R, Yuan Z
Vicuron Pharmaceuticals (formerly Versicor Inc), 34790 Ardentech Court, Fremont, CA 94555, USA.
Bioorg Med Chem Lett. 2003 Dec 1;13(23):4223-8. doi: 10.1016/j.bmcl.2003.07.020.
We report the synthesis and biological activity of analogues of VRC3375 (N-hydroxy-3-R-butyl-3-[(2-S-(tert-butoxycarbonyl)-pyrrolidin-1-ylcarbonyl]propionamide), an orally active peptide deformylase inhibitor. This study explores the structure-activity relationship of various chelator groups, alpha substituents, P(2)' and P(3)' substituents in order to achieve optimal antibacterial activity with minimal toxicity liability.
我们报告了口服活性肽脱甲酰基酶抑制剂VRC3375（N-羟基-3-R-丁基-3-[(2-S-(叔丁氧羰基)-吡咯烷-1-基羰基]丙酰胺）类似物的合成及生物活性。本研究探索了各种螯合剂基团、α取代基、P(2)'和P(3)'取代基的构效关系，以实现具有最小毒性的最佳抗菌活性。
