Studies On Semi-Synthesis Of Osthol Derivatives And Their Calcium Rivalry Activities

One natural product, osthol, isolated from the seed of Cnidum monnieri (L.) Cusson, is acted as the leading compound. According to the medicinal chemistry theories, advanced techniques, new methods, and results pharmacologically screening, the relation with structure and calcium rivalry activity is researched. We want to screen the better calcium antagonists. The accomplishments were as following:Through semi-synthesizing for osthol of 7-hydroxy, 42 derivatives were synthesized. The structures of all products were identified with ¹HNMR, ¹³CNMR, EI-MS and IR. Among of them, 41 derivatives out of all synthesized compounds were new compounds. Among, 26 derivatives were screened to approach the structure basis for their calcium rivalry activities. Among these products, all compounds have certain activities. MO-1 and MO-5 have higher calcium rivalry activities for the rabbit vascular ring. From the results pharmacologically screening, It is primary understood that 7-methoxy in osthol is the key moiety for calcium rivalry activity and the bioactivity of derivatives from osthol is changed with different group substituted.