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Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2019-12-18 , DOI: 10.1080/14756366.2019.1702654
Xianqing Deng 1 , Mingxia Song 1
Affiliation  

Two series of aminoguanidines containing an alkynyl moiety were designed, synthesised, and screened for antibacterial and anticancer activities. Generally, the series 3a-3j with a 1,2-diphenylethyne exhibited better antibacterial activity than the other series (6a-6k) holding 1,4-diphenylbuta-1,3-diyne moiety antibacterial activity. Most compounds in series 3a-3j showed potent growth inhibition against the tested bacterial strains, with minimum inhibitory concentration (MIC) values in the range 0.25-8 µg/mL. Compound 3g demonstrated rapid and persistent bactericidal activity at 2 × MIC. The resistance study revealed that resistance of the tested bacteria towards 3g is not easily developed. Molecular docking studies revealed that compounds 3g and 6e bind strongly to the LpxC and FabH enzymes. Moreover, excellent activity of selected compounds against the growth of cancer cell lines A549 and SGC7901 was also observed, with IC50 values in the range 0.30-4.57 µg/mL. These findings indicate that compounds containing the aminoguanidine moiety are promising candidates for the development of new antibacterial and anticancer agents.

中文翻译:

含有炔基部分的氨基胍的合成,抗菌和抗癌活性以及对接研究。

设计,合成并筛选了两个含有炔基部分的氨基胍系列,以测定其抗菌和抗癌活性。通常,具有1,2-二苯基乙炔的系列3a-3j显示出比具有1,4-二苯基丁-1,3-二炔部分抗菌活性的其他系列(6a-6k)更好的抗菌活性。3a-3j系列中的大多数化合物显示出对测试细菌菌株的有效生长抑制作用,最小抑制浓度(MIC)值在0.25-8 µg / mL范围内。化合物3g在2×MIC下显示出快速而持久的杀菌活性。抗药性研究表明,被测细菌对3g的抗药性不容易形成。分子对接研究表明,化合物3g和6e与LpxC和FabH酶牢固结合。而且,还观察到所选化合物对癌细胞系A549和SGC7901的生长具有极好的活性,IC50值在0.30-4.57 µg / mL范围内。这些发现表明,含有氨基胍部分的化合物是开发新的抗菌剂和抗癌剂的有希望的候选者。
更新日期:2020-04-20
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