论文部分内容阅读
目的:发现新的肽脱甲酰基酶(PDF)抑制剂先导化合物。方法:在异(?)唑环杂原子作为电子对供体替代羰基氧原子与受体形成氢键的新思路指导下,设计并合成了一系列新型含异(口恶)唑的β-戊基-丁二酰异羟肟酸衍生物,其结构经核磁共振(NMR)、质谱(MS)等证明,并对部分该类化合物进行了体外抑菌实验。结果:体外抑菌实验表明,该类化合物具有一定的抗菌活性。结论:以异(口恶)唑环杂原子作为电子对供体替代肽分子中的羰基氧原子与受体形成氢键的设想是成立的,为进一步优化本类化合物结构,乃至对类肽新药的设计具有重要意义。
PURPOSE: To discover novel peptide deacetylase (PDF) inhibitor lead compounds. Methods: A series of novel β-amyl oxazoles with different azoles were designed and synthesized under the guidance of heteroleptic ring heteroatoms as electron donors to substitute oxygen atoms of carbon atoms for hydrogen bonding with acceptor. The structure of the base-succinylhydroxamic acid derivatives was proved by NMR and MS, and some of these compounds were tested in vitro. Results: In vitro antibacterial experiments show that these compounds have some antibacterial activity. CONCLUSION: The assumption that the heteroaromatic azole ring heteroatom serves as an electron donor to substitute the carbonyl oxygen atom in the donor molecule for the hydrogen bond with the acceptor is established. In order to further optimize the structure of this class of compounds, The design is of great importance.