Department of Chemistry, University of Lucknow, Lucknow 226 007, India.
Bioorg Med Chem Lett. 2011 Nov 1;21(21):6398-403. doi: 10.1016/j.bmcl.2011.08.095. Epub 2011 Aug 31.
Various oxygen containing 1,4-naphthoquinone derivatives have been synthesized chemoselectively by an economical, viable green methodology approach using water as solvent with or without surfactants such as Triton X-100, SDS, LD (laundry detergent), and TBAB, a phase transfer catalyst and evaluated for their in vitro antifungal and antibacterial activity. The antifungal profile of 3, 4a, 4b, and 6 indicated that compounds 3a, 3b, 4b, 6a, and 6c have potent antifungal activity compared to clinically prevalent antifungal drugs Fluconazole and Amphotericin-B against Sporothrix schenckii, Trichophyton mentagraphytes, and Candida parapsilosis and compound 3b has been found to be a lead antifungal agent for further study.
已经通过经济、可行的绿色方法，以水为溶剂，选择性地合成了各种含氧 1,4-萘醌衍生物，其中使用或不使用表面活性剂如 Triton X-100、SDS、LD（洗涤剂）和 TBAB（相转移催化剂）。评估了它们的体外抗真菌和抗菌活性。化合物 3、4a、4b 和 6 的抗真菌谱表明，与临床常用的抗真菌药物氟康唑和两性霉素 B 相比，化合物 3a、3b、4b、6a 和 6c 对申克孢子丝菌、须癣毛癣菌和近平滑假丝酵母具有更强的抗真菌活性，并且发现化合物 3b 是一种有前途的抗真菌先导化合物，值得进一步研究。
