Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3537-9. doi: 10.1016/j.bmcl.2010.04.126. Epub 2010 May 18.
Head group analogues of the antibacterial and antiparasitic drug nitazoxanide (NTZ) are presented. A library of 39 analogues was synthesized and assayed for their ability to suppress growth of Helicobacter pylori, Campylobacter jejuni, Clostridium difficile and inhibit NTZ target pyruvate:ferredoxin oxidoreductase (PFOR). Two head groups assayed recapitulated NTZ activity and possessed improved activity over their 2-amino-5-nitrothiazole counterparts, demonstrating that head group modification is a viable route for the synthesis of NTZ-related antibacterial analogues.
呈现了抗菌和抗寄生虫药物硝唑尼特（NTZ）的头基类似物。合成了 39 个类似物库，并对它们抑制幽门螺杆菌、空肠弯曲菌、艰难梭菌生长的能力以及抑制 NTZ 靶标丙酮酸：铁氧还蛋白氧化还原酶（PFOR）的能力进行了检测。两种被检测的头基重现了 NTZ 的活性，并且比其 2-氨基-5-硝基噻唑对应物具有更好的活性，这表明对头基的修饰是合成 NTZ 相关抗菌类似物的可行途径。
