18607-90-4Relevant articles and documents
Compound with HMG-CoA reductase inhibitory activity, pharmaceutical composition and application thereof
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Paragraph 0032; 0040-0043, (2021/05/05)
The invention belongs to the field of biological medicines, and particularly discloses a compound shown as a formula I and used for treating and/or preventing HMG-CoA reductase related diseases or pharmaceutically acceptable salt or ester of the compound. The invention also discloses a pharmaceutical composition containing the compound. In addition, the invention also provides an application of the compound as an HMG-CoA reductase inhibitor and in preparation of drugs for treating and/or preventing HMG-CoA reductase related diseases. The compound provided by the invention has relatively strong activity of inhibiting HMG-CoA reductase, the prepared medicine is expected to have a relatively good effect on treating and/or preventing dyslipidemia and atherosclerosis, and the compound is relatively simple in structure and relatively low in expected price. In addition, the structure of the compound provided by the invention is completely different from that of the existing statins, and the phenomenon of drug resistance to the existing statins can be overcome.
Synthesis and antifungal activity of 2-hydroxy-4,5-methylenedioxyaryl ketones as analogues of kakuol
Musso, Loana,Dallavalle, Sabrina,Merlini, Lucio,Farina, Gandolfina
experimental part, p. 887 - 897 (2011/04/22)
In a study aiming to determine the structural elements essential to the antifungal activity of kakuol, we synthesized a series of 2-hydroxy-4,5- methylenedioxyaryl ketones, and we assayed their in vitro antifungal activity. The most sensitive target organisms to the action of these class of compounds were Phytophthora infestans, Phytium ultimum, Cercospora beticola, Cladosporium cucumerinum, and Rhizoctonia solani. Most of the analogs showed a remarkable in vitro activity, and some of them appeared significantly more effective than the natural product. The biological activity was mainly affected by introducing structural modification on the carbonyl moiety of the natural-product molecule. In particular, compound 5a, bearing a C=C bond conjugated to the C=O group, was found active with a MIC value of 10 μg ml-1 against Cladosporium cucumerinum. The results suggest that 2-hydroxy-4,5-methylenedioxyaryl ketones can be considered promising candidates in the development of new antifungal compounds.