Department of Chemistry, Indian Institute of Technology Madras , Chennai 600036, India.
Org Lett. 2015 Jan 16;17(2):194-7. doi: 10.1021/ol503135u. Epub 2014 Dec 23.
A common building block for the synthesis of amorfrutin and cajaninstilbene acid derivatives has been developed. The library of synthesized compounds has enabled identification of new nontoxic ligands of peroxisome proliferator-activated receptors (PPAR) and potential inhibitors of the transcriptional corepressor protein NCoR. The biological data holds promise in identification of new potential leads for the antidiabetic drug discovery process.
已开发出一种用于合成美洲花椒素和鸡纳异戊烯基二氢菲酸衍生物的常见构建模块。所合成化合物的文库使我们能够鉴定过氧化物酶体增殖物激活受体 (PPAR) 的新型无毒配体和转录核心抑制蛋白 NCoR 的潜在抑制剂。这些生物学数据有望为抗糖尿病药物发现过程中鉴定新的潜在先导化合物提供帮助。