90104-86-2Relevant academic research and scientific papers
Anti-influenza drug discovery: Structure-activity relationship and mechanistic insight into novel angelicin derivatives
Yeh, Jiann-Yih,Coumar, Mohane Selvaraj,Horng, Jim-Tong,Shiao, Hui-Yi,Kuo, Fu-Ming,Lee, Hui-Ling,Chen, In-Chun,Chang, Chun-Wei,Tang, Wen-Fang,Tseng, Sung-Nain,Chen, Chi-Jene,Shih, Shin-Ru,Hsu, John T.-A.,Liao, Chun-Chen,Chao, Yu-Sheng,Hsieh, Hsing-Pang
experimental part, p. 1519 - 1533 (2010/08/20)
By using a cell-based high throughput screening campaign, a novel angelicin derivative 6a was identified to inhibit influenza A. (H1N1) virus induced cytopathic effect in Madin-Darby canine kidney cell culture in low micromolar range. Detailed structure-activity relationship studies of 6a revealed that the angelicin scaffold is essential for activity in pharmacophore B, while meta-substituted phenyl/2-thiophene rings are optimal in pharmacophore A and C. The optimized lead 4-methyl-9-phenyl-8-(thiophene-2-carbonyl)-furo[2,3-h] chromen-2-one (8g, IC50 = 70 nM) showed 64-fold enhanced activity compared to the high throughput screening (HTS) hit 6a. Also, 8g was found effective in case of influenza A (H3N2) and influenza B virus strains similar to approved anti-influenza drug zanamivir (4). Preliminary mechanistic studies suggest that these compounds act as anti-influenza agents by inhibiting ribonucleoprotein (RNP) complex associated activity and have the potential to be developed further, which could form the basis for developing additional defense against influenza pandemics.
Photo-induced Reactions: Part IV-Studies on Photo Fries Migration of Some Coumarins
Kulshrestha, S.K.,Dureja, P.,Mukerjee, S.K.
, p. 1064 - 1067 (2007/10/02)
Photo-Fries migration as an alternative route to acylcoumarins has been investigated. 7-Acetoxy- and 7-furoyloxy-coumarins give 6-acylcoumarins as the major products in contrast to Lewis acid mediated Fries migration where 8-acyl derivatives are the major products.The benzoates on the other hand give 6- and 8-acylcoumarins in equal proportions.The method is not suitable for the preparation of long chain unsaturated acyl derivatives of coumarins because in such cases photolytic deesterification is the main route.
