Global Discovery Chemistry, Novartis Institutes for Biomedical Research, Cambridge, Massachusetts 02139, United States.
J Med Chem. 2011 Apr 14;54(7):2517-21. doi: 10.1021/jm101602q. Epub 2011 Mar 15.
4-Aminothiazolyl analogues of the antibacterial natural product GE2270 A (1) were designed, synthesized, and evaluated for gram positive bacteria growth inhibition. The aminothiazole-based chemical template was evaluated for chemical stability, and its decomposition revealed a novel, structurally simplified, des-thiazole analogue of 1. Subsequent stabilization of the 4-aminothiazolyl functional motif was achieved and initial structure activity relationships defined.
设计、合成了抗菌天然产物 GE2270 A（1）的 4-氨基噻唑类似物，并对其抑制革兰氏阳性菌生长的活性进行了评价。评估了基于氨基噻唑的化学模板的化学稳定性，其分解揭示了 1 的一种新颖的、结构简化的去噻唑类似物。随后稳定了 4-氨基噻唑功能基序，并确定了初步的结构活性关系。
