Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):444-8. doi: 10.1016/j.bmcl.2010.10.120. Epub 2010 Oct 30.
Sodium bisulfite has been reported first time for the synthesis of 2,5-disubstituted 1,3,4-oxadiazole using microwave and conventional method in ethanol-water. The yields obtained are in the range of 90-95% using microwave and 87-91% using conventional method. All the synthesized compounds (8a-8s) are novel and were evaluated for their in vitro antifungal activity. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Some of the compounds from the series like 8k was equipotent with miconazole against Candida albicans and Fusarium oxysporum. Also compound 8n was equipotent with miconazole against F. oxysporum.
亚硫酸氢钠首次被报道用于在乙醇-水介质中通过微波和常规方法合成 2,5-二取代 1,3,4-噁二唑。使用微波时，收率在 90-95%之间，使用常规方法时，收率在 87-91%之间。所有合成的化合物（8a-8s）都是新型化合物，并对其进行了体外抗真菌活性评估。通过比较它们的 MIC 值与咪康唑和氟康唑，对该系列化合物进行了构效关系研究。该系列中的一些化合物，如 8k，对白色念珠菌和尖孢镰刀菌的活性与咪康唑相当。化合物 8n 对尖孢镰刀菌的活性也与咪康唑相当。
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