Division of Organic Chemistry, National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):722-5. doi: 10.1016/j.bmcl.2009.11.071. Epub 2009 Dec 4.
As a part of our program to develop new antifungal agents, a series of fluconazole analogues was designed and synthesized wherein one of the triazole moieties in fluconazole was replaced with 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moiety. The new chemical entities thus synthesized were screened against various fungi and it was observed that the compounds 4a and 4i are potent inhibitors of Candida strains. The structure-activity relationship for these compounds is discussed.
作为我们开发新型抗真菌药物计划的一部分，设计并合成了一系列氟康唑类似物，其中氟康唑中的一个三唑部分被 2H-1,4-苯并噻嗪-3(4H)-酮或 2H-1,4-苯并恶嗪-3(4H)-酮部分取代。对新合成的这些化学实体进行了针对各种真菌的筛选，结果观察到化合物 4a 和 4i 是念珠菌菌株的有效抑制剂。讨论了这些化合物的构效关系。
