69480-03-1Relevant articles and documents
Biomimetic total syntheses of baefrutones A-D, baeckenon B, and frutescones A, D-F
Dong, Ying-Ying,Hou, Ji-Qin,Peng, Qiu-Shi,Wang, Hao,Yu, Jiang-Hong,Zhang, Bao-Bao,Zhao, Heng
, p. 1135 - 1139 (2020/02/22)
Biomimetic total syntheses of baefrutones A-D (1-4), baeckenon B (5), and frutescones A, D-F (6-9), isolated from the leaves of Baeckea frutescens, were achieved in 9, 8, and 5 steps, respectively, in moderate to good yields (72-83%). The synthetic routes feature the Michael addition, oxidative [4 + 2] cycloaddition, and water-promoted Diels-Alder click reactions as the key steps. This study helped gain thorough mechanistic insights into the biosynthetic origins and provided a facile approach for the construction of a library of natural tasmanone-based meroterpenoid analogues. Moreover, compounds 1-9 show potent inhibitory effects against S. paratyphi and/or C. albicans with MIC values of 3.125-25 μg mL-1, and they could be promising lead molecules for the design of new antibiotic agents.
Novel diphenylmethyl compounds having mycobacterium tuberculosis inhibitory activity
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Paragraph 0270; 0271; 0276; 0277; 0303-0306, (2019/02/13)
The invention relates to novel diphenylmethyl derivatives having mycobacterium tuberculosis inhibitory activity and a preparation method thereof and particularly relates novel diphenylmethyl derivatives having activity for inhibiting replicative and non-replicating mycobacterium tuberculosis and a preparation method thereof. In particular, the invention relates to compounds shown in the formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein the variables are as described in the specification. The invention also relates to the preparation method of the compounds and their pharmaceutical compositions and a use of the compounds in preparation of drugs for treating mycobacterium tuberculosis infection-caused diseases.