Chemistry Research Laboratory, University of Oxford, Mansfield Rd, Oxford OX1 3TA, UK.
Chemistry Research Laboratory, University of Oxford, Mansfield Rd, Oxford OX1 3TA, UK.
Bioorg Med Chem Lett. 2014 Apr 15;24(8):1901-6. doi: 10.1016/j.bmcl.2014.03.013. Epub 2014 Mar 14.
The synthesis and evaluation of 3-enaminetetramic acids as antibacterial agents is reported; contrary to the analogous 3-acyltetramic acids, the enaminetetramic acid class of compound exhibits modest antibacterial activity against a limited spectrum of organisms, and even that activity is strongly dependent on the identity of the tetramate ring substituents. Moreover, these compounds appear to have a different mode of action to the analogous 3-acyltetramic acids, and appear to offer more limited opportunity for further elaboration in drug discovery.
本文报道了 3-烯胺四氢酸类化合物作为抗菌剂的合成与评价；与类似的 3-酰基四氢酸不同，烯胺四氢酸类化合物对有限范围的生物体表现出适度的抗菌活性，而且这种活性强烈依赖于四氢酸环取代基的性质。此外，这些化合物的作用模式似乎与类似的 3-酰基四氢酸不同，并且在药物发现中似乎提供了进一步精细化的机会有限。
