Kashanna Jajula, Kumar Rathod Aravind, Kishore Ravada, Kumar Duddukuri Nandan, Kumar Alleni Suman
Department of Chemistry, Rajiv Gandhi University of Knowledge Technologies, Basar, 504107, India.
Semiochemical Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500007, India.
Chem Biodivers. 2018 Nov;15(11):e1800277. doi: 10.1002/cbdv.201800277. Epub 2018 Oct 26.
Novel 2,3-dihydrofuran derivatives were synthesized through a tandem Knoevenagel-Michael cyclization in good yield by reacting α-tosyloxy ketone, 5,5-dimethyl-1,3-cyclohexanedione, and various aldehydes in the presence of phthalazine in acetonitrile. These compounds were subjected to in vitro antibacterial screening against eight micro-organisms by using diffusion method and also in vitro cytotoxicity screening against four human cancerous cell lines by applying MTT assay. Some of the compounds showed impressive activities.
通过在乙腈中，使α-甲苯磺酰氧基酮、5,5-二甲基-1,3-环己二酮与各种醛在酞嗪存在下发生串联Knoevenagel-迈克尔环化反应，以良好的产率合成了新型2,3-二氢呋喃衍生物。采用扩散法对这些化合物针对8种微生物进行了体外抗菌筛选，并通过MTT法对4种人类癌细胞系进行了体外细胞毒性筛选。部分化合物显示出令人印象深刻的活性。
