【摘 要】
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Tetramic acids and their derivatives comprise a common structural feature of natural products,and are well known for their potent antibiotic,antiviral,and a
【机 构】
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Department of Chemistry University of Oxford Chemistry Research Laboratory UK
【出 处】
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中国上海第七届国际新药发明科技年会
论文部分内容阅读
Tetramic acids and their derivatives comprise a common structural feature of natural products,and are well known for their potent antibiotic,antiviral,and antifungal as well as cytotoxic activity.Those which contain structural units derived from a N-methylserine or N-methylthreonine unit include the equisetins,the oxazolomycins,the salinosporamides,and the cinnabarimides.We have shown that serine-and threonine-derived oxazolidine templates can be used for highly chemo-and diasteroselective ring closure reactions leading to tetramic acid and pyroglutamate derivatives.Recently,we have applied this synthetic methodology for the synthesis of mimics of natural products,and have been able to use this approach to identify key pharmacophores and to demonstrate that this approach can be readily used to generate libraries of compounds of promise for their antibiotic activity.We report here specifically on the identification of novel antibiotics based upon the natural products,oxazolomycin,reutericyclin and equisetin.
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