[Synthesis and biological evaluation of novel pleuromutilin derivatives with nitrogen-containing heterocycles as antibacterial agents].

Q3 Pharmacology, Toxicology and Pharmaceutics Acta pharmaceutica Sinica Pub Date : 2015-10-01
Xin-yang Wang, Min Chen, Duo Wang, Xiang-dong Chen, Yong Ling, Xiao-li Wang, Hui Wang
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引用次数: 0

Abstract

A series of new pleuromutilins derivatives were designed and synthesized through coupling 2-aminothiazole ring of WL001 with different nitrogen-containing substituted heterocycles in the side chain. Their biological activities were evaluated against both Gram-positive and Gram-negative clinical bacteria in vitro Most new compounds displayed specificity to certain strain of bacteria. Particularly, compounds with saturated nitrogen-containing heterocycles exhibited significant antibacterial activities (0.062 5-8 µg · mL(-1)) superior or similar to those of amoxicillin, tiamulin and levofloxcin. Furthermore, treatment with 15a and 15b having piperidine or morpholine residues also could effectively inhibit Gram-negative bacteria. Therefore, our novel findings may provide a new insight into the design of novel pleuromutilin derivatives and lay the basis for further studies on the treatment of drug-resistance of pathogenic bacteria.

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[含氮杂环的新型胸腺嘧啶衍生物作为抗菌剂的合成和生物学评价]。
通过将 WL001 的 2- 氨基噻唑环与侧链中不同的含氮取代杂环偶联,设计并合成了一系列新的胸腺嘧啶衍生物。大多数新化合物对某些菌株具有特异性。尤其是含饱和氮杂环的化合物,其抗菌活性(0.062 5-8 µg - mL(-1))明显优于或类似于阿莫西林、替米考林和左氧氟沙星。此外,具有哌啶或吗啉残基的 15a 和 15b 也能有效抑制革兰氏阴性菌。因此,我们的新发现可为新型胸腺嘧啶衍生物的设计提供新的思路,并为进一步研究治疗病原菌耐药性奠定基础。
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