Bibliographic Details
| Title: |
Efficient Synthesis of Frutinone A and Its Derivatives through Palladium-Catalyzed CH Activation/Carbonylation. |
| Authors: |
Shin, Yongje, Yoo, Changho, Moon, Youngtaek, Lee, Yunho, Hong, Sungwoo |
| Source: |
Chemistry - An Asian Journal; Apr2015, Vol. 10 Issue 4, p878-881, 4p |
| Subject Terms: |
Anti-infective agents, Palladium catalysts, Carbonylation, Phenol synthesis, Structure-activity relationships |
| Abstract: |
Frutinone A, a biologically active ingredient of an antimicrobial herbal extract, demonstrates potent inhibitory activity towards the CYP1A2 enzyme. A three-step total synthesis of frutinone A with an overall yield of 44 % is presented. The construction of the chromone-annelated coumarin core was achieved through palladium-catalyzed CH carbonylation of 2-phenolchromones. The straightforward synthetic route allowed facile substitutions around the frutinone A core and thus rapid exploration of the structure-activity relationship (SAR) profile of the derivatives. The inhibitory activity of the synthesized frutinone A derivatives were determined for CYP1A2, and ten compounds exhibited one-to-two digit nanomolar inhibitory activity towards the CYP1A2 enzyme. [ABSTRACT FROM AUTHOR] |
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| Database: |
Complementary Index |