Process Chemistry and Chemical Engineering Department, Central Institute of Medicinal and Aromatic Plants, (Council of Scientific and Industrial Research), P.O. CIMAP, Lucknow-226015, Uttar Pradesh, India.
Eur J Med Chem. 2010 Nov;45(11):5150-6. doi: 10.1016/j.ejmech.2010.08.027. Epub 2010 Aug 14.
Six novel cleomiscosin A (a coumarino-lignoid), derivatives have been synthesized for the first time by using electrophilic substitution reaction to give nuclear nitrated and halogenated derivatives of cleomiscosin A in good yields. Structures of these compounds were established on the basis of IR, (1)H NMR, (13)C NMR and Mass spectral data. Some of the synthesized derivatives were tested for in-vitro target based anti-inflammatory study using primary macrophages cell culture bioassay system. The results showed that the compounds 1a, 3a and 4a (1 and 10 μg/mL) exhibited potent anti-inflammatory activity.
首次通过亲电取代反应合成了 6 种新型的 cleomiscosin A（香豆素-木脂素）衍生物，以高产率得到了 cleomiscosin A 的核硝化和卤化衍生物。这些化合物的结构是基于红外光谱（IR）、（1）H NMR、（13）C NMR 和质谱数据确定的。对一些合成的衍生物进行了基于原发性巨噬细胞细胞培养生物测定系统的体外靶向抗炎研究。结果表明，化合物 1a、3a 和 4a（1 和 10 μg/mL）表现出很强的抗炎活性。
