扁平霉素类似物的合成与生物学评价
Synthesis and biological evaluation of platensimycin analogs.
作者信息
Shen Hong C, Ding Fa-Xiang, Singh Sheo B, Parthasarathy Gopalakrishnan, Soisson Stephen M, Ha Sookhee N, Chen Xun, Kodali Srinivas, Wang Jun, Dorso Karen, Tata James R, Hammond Milton L, Maccoss Malcolm, Colletti Steven L
机构信息
Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1623-7. doi: 10.1016/j.bmcl.2009.02.006. Epub 2009 Feb 7.
Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity.
扁平霉素（1）因其对延伸缩合酶（FabF）的抑制作用而具有抗菌活性，这是一种新的作用模式，可能会在新一代抗生素的研发上带来突破。药物化学研究工作主要集中在对扁平霉素烯酮部分的修饰上，有几种类似物对FabF显示出显著活性并具有抗菌活性。
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