Song Lijun, Risseeuw Martijn D P, Froeyen Matheus, Karalic Izet, Goeman Jan, Cappoen Davie, Van der Eycken Johan, Cos Paul, Munier-Lehmann Hélène, Van Calenbergh Serge
Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteemweg 460, B-9000 Ghent, Belgium.
Medicinal Chemistry (Rega Institute), Department of Pharmaceutical and Pharmacological Sciences, KU LEUVEN, Minderbroedersstraat 10 blok x-box 1030, 3000 Leuven, Belgium.
Bioorg Med Chem. 2016 Nov 1;24(21):5172-5182. doi: 10.1016/j.bmc.2016.08.041. Epub 2016 Aug 24.
We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1-14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure-activity relationship, which is helpful for further optimization.
我们报道了基于革兰氏阳性细菌TMPK抑制剂先导化合物1设计并合成的一系列非核苷类结核分枝杆菌胸苷酸激酶（MtbTMPK）抑制剂（1-14）。已开发出一种实用的合成方法来制备这些类似物。几种化合物显示出有前景的MtbTMPK抑制活性，并有助于建立构效关系，这对进一步优化有帮助。
