Macherla Venkat R, Liu Jehnan, Sunga Michelle, White Donald J, Grodberg Jennifer, Teisan Sy, Lam Kin S, Potts Barbara C M
Nereus Pharmaceuticals, Inc., San Diego, California 92121, USA.
J Nat Prod. 2007 Sep;70(9):1454-7. doi: 10.1021/np0702032. Epub 2007 Sep 11.
Marine actinomycete strain NPS008920, a member of the new genus Marinispora, was isolated from a sediment sample collected in Cocos Lagoon, Guam. In natural sea water containing media, the strain produced a series of novel 2-alkylidene-5-alkyl-4-oxazolidinones, lipoxazolidinone A (1), B (2), and C (3). Compounds 1- 3 showed broad spectrum antimicrobial activity similar to that of the commercial antibiotic linezolid (Zyvox), a 2-oxazolidinone. Hydrolysis of the amide bond of the 4-oxazolidinone ring of 1 resulted in loss of antibacterial activity. The 2-alkylidene-4-oxazolidinone represents a new antibiotic pharmacophore and is unprecedented in nature.
海洋放线菌菌株NPS008920是新属Marinispora的成员，从关岛科科斯泻湖采集的沉积物样本中分离得到。在含有天然海水的培养基中，该菌株产生了一系列新型的2-亚烷基-5-烷基-4-恶唑烷酮，即脂恶唑烷酮A（1）、B（2）和C（3）。化合物1-3表现出与商业抗生素利奈唑胺（Zyvox，一种2-恶唑烷酮）相似的广谱抗菌活性。1的4-恶唑烷酮环的酰胺键水解导致抗菌活性丧失。2-亚烷基-4-恶唑烷酮代表一种新的抗生素药效基团，在自然界中是前所未有的。
