申请人:Shaw Jared
公开号:US20090221568A1
公开(公告)日:2009-09-03
FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.
FtsZ是细菌中类似于微管蛋白的有前途的新靶点,可用于开发新型抗生素。已经表明,多酚类物质能够抑制FtsZ的GTP酶活性,从而抑制有丝分裂期间Z环的形成。本发明提供了新型的多酚类化合物,可以通过所述的二氢松香素和2′″-羟基-5″-苄基异乌金醇-B的合成来获得。这些新型化合物在治疗感染,特别是由革兰氏阳性菌引起的感染方面具有用途。还提供了制备本发明化合物的方法。这些化合物通过对松树素或芹菜素核心结构进行苄基化来制备。还提供了制药组合物和使用这些化合物治疗疾病的方法。这些化合物可以筛选抗微生物活性以及其他生物活性,如抗肿瘤、抗炎、免疫抑制和细胞毒性活性。