新型高效的DNA促旋酶B香豆素抑制剂的合成及体外评价
Synthesis and in vitro evaluation of novel highly potent coumarin inhibitors of gyrase B.
作者信息
Laurin P, Ferroud D, Klich M, Dupuis-Hamelin C, Mauvais P, Lassaigne P, Bonnefoy A, Musicki B
机构信息
Medicinal Chemistry, Infectious Disease, Romainville, France.
出版信息
Bioorg Med Chem Lett. 1999 Jul 19;9(14):2079-84. doi: 10.1016/s0960-894x(99)00329-7.
The design, synthesis, and in vitro biological activity of a series of novel coumarin inhibitors of gyrase B is presented. Replacement of the 3-acylamino residue (3-NHCOR) of coumarin drugs with reversed isosteres C(=O)R, C(=N-OR)R', COOR, CONHR and CONHOR leads to highly potent analogues which displayed excellent inhibition of the negative supercoiling of the relaxed DNA and antibacterial activity.
本文介绍了一系列新型喹诺酮B抑制剂香豆素的设计、合成及其体外生物活性。用反向电子等排体C(=O)R、C(=N-OR)R'、COOR、CONHR和CONHOR取代香豆素药物的3-酰基氨基残基(3-NHCOR)，得到了高效类似物，这些类似物对松弛DNA的负超螺旋具有优异的抑制作用和抗菌活性。
Zotero 插件