7073-22-5Relevant articles and documents
The Biomimetic Total Syntheses of the Antiplasmodial Tomentosones A and B
Dong, Chunmao,Hu, Yingjie,Huo, Luqiong,Liu, Hongxin,Tan, Haibo,Wu, Guiyun,Yuan, Yunfei,Zhang, Xiao
, p. 8007 - 8011 (2020)
The first biomimetic total syntheses of natural phloroglucinols tomentosones A and B and their analogues have been accomplished. The synthetic strategy primarily referred to the potential biosynthetic precursors and their possible sequence of segments ass
Total syntheses of ericifolione and its analoguesviaa biomimetic inverse-electron-demand Diels-Alder reaction
Chen, Huiyu,Huo, Luqiong,Li, Changgeng,Tan, Haibo,Wang, Sasa,Zheng, Anquan,Zhou, Tingting
supporting information, p. 270 - 273 (2022/01/03)
Driven by bioinspiration and appreciation of the structure of ericifolione, a biomimetic tautomerization/intermolecular inverse-electron-demand hetero Diels-Alder reaction cascade sequence promoted by sodium acetate to rapidly construct sterically hindere
Application of myrtle ketone compound in preparation of novel coronavirus SARS-CoV-2 medicine
-
Paragraph 0045; 0048; 0051-0052, (2021/12/07)
The invention discloses application of myrtle ketone compounds in preparation of novel coronavirus SARS-CoV-2 medicaments. The myrtle ketone compound has obvious inhibition effect on novel coronavirus SARS-CoV-2. Mechanisms include, but are not limited to, inhibition of new coronavirus SARS-CoV-2 into cells, preventing the replication of new coronavirus SARS-CoV-2 in the host cell, and timely modulating apoptosis of infected cells. To the myrtle ketone compound provided by the invention, the novel coronavirus SARS-CoV-2 has a remarkable inhibiting effect, and the cytotoxicity is relatively small. It can therefore be used for the prophylaxis or treatment of neoplastic pneumonitis. The invention is expected to provide new candidate drug molecules for clinic treatment of nebrodensis.
Peachy ketones and their application in the preparation of anti-flu virus drugs
-
Paragraph 0049-0052; 0055-0056, (2021/12/07)
The present invention discloses myrtle ketone compounds and their applications in the preparation of anti-influenza virus drugs. The myrtle ketone compounds of the present invention have a significant inhibitory effect on influenza viruses, the mechanism of action of which includes (but is not limited to) inhibiting influenza viruses entering cells, preventing the replication of influenza viruses in host cells, and timely regulating the apoptosis program of infected cells. The myrtle ketone compounds provided by the present invention have inhibitory effects on both influenza A and B viruses, the activity is better than the positive drug ribavirin (Ribavrin), and therefore can be used to prevent or treat influenza. The present invention is expected to provide a new active lead compound or drug candidate molecule for the clinical treatment of influenza.
Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity
Athanassopoulos, Constantinos M.,Baltas, Michel,Grellier, Philippe,Menendez, Christophe,Mouray, Elisabeth,Papaioannou, Dionissios,Pepe, Dionissia A.,Toumpa, Dimitra,André-Barrès, Christiane
supporting information, p. 921 - 927 (2020/07/21)
A series of novel hybrids of artemisinin (ART) with either a phytormone endoperoxide G factor analogue (GMeP) or chloroquine (CQ) and conjugates of the same compounds with the polyamines (PAs), spermidine (Spd), and homospermidine (Hsd) were synthesized and their antiplasmodial activity was evaluated using the CQ-resistant P. falciparum FcB1/Colombia strain. The ART-GMeP hybrid 5 and compounds 9 and 10 which are conjugates of Spd and Hsd with two molecules of ART and one molecule of GMeP, were the most potent with IC50 values of 2.6, 8.4, and 10.6 nM, respectively. The same compounds also presented the highest selectivity indexes against the primary human fibroblast cell line AB943 ranging from 16 372 for the hybrid 5 to 983 for the conjugate 10 of Hsd.
The First Racemic Total Syntheses of the Antiplasmodials Watsonianones A and B and Corymbone B
Zhang, Xiao,Wu, Guiyun,Huo, Luqiong,Guo, Xueying,Qiu, Shengxiang,Liu, Hongxin,Tan, Haibo,Hu, Yingjie
supporting information, p. 3 - 7 (2019/11/21)
The first biomimetic total syntheses of three biologically meaningful acylphloroglucinols, watsonianones A and B and corymbone B, with potent antiplasmodial activity, were performed. Their total syntheses were carried out through a diversity-oriented synthetic strategy from congener 2,2,4,4-tetramethyl-6-(3-methylbutylidene)cyclohexane-1,3,5-trione with high step efficiency. The spontaneous enolization/air oxidation of the precursor 2,2,4,4-tetramethyl-6-(3-methylbutylidene)cyclohexane-1,3,5-trione through a singlet O2-induced Diels-Alder reaction pathway to assemble the key biosynthetic peroxide intermediate is also discussed.
Method for synthesizing anti-malarial drug watsonianones A
-
Paragraph 0033-0035, (2020/02/14)
The invention discloses a method for synthesizing an anti-malarial drug watsonianones A. The method comprises the following steps: carrying out a Knoevenagel reaction catalyzed by proline on syncarpicacid and isovaleraldehyde to obtain a precursor compoun
Isolation and Synthesis of Novel Meroterpenoids from Rhodomyrtus tomentosa: Investigation of a Reactive Enetrione Intermediate
Qin, Xu-Jie,Rauwolf, Tyler J.,Li, Pan-Pan,Liu, Hui,McNeely, James,Hua, Yan,Liu, Hai-Yang,Porco, John A.
supporting information, p. 4291 - 4296 (2019/02/26)
Rhodomyrtusials A–C, the first examples of triketone-sesquiterpene meroterpenoids featuring a unique 6/5/5/9/4 fused pentacyclic ring system were isolated from Rhodomyrtus tomentosa, along with several biogenetically-related dihydropyran isomers. Two bis-furans and one dihydropyran isomer showed acetylcholinesterase (AChE) inhibitory activity. Structures of the isolates were unambiguously established by a combination of spectroscopic data, ECD analysis, and total synthesis. Bioinspired total syntheses of six isolates were achieved in six steps utilizing a reactive enetrione intermediate generated in situ from a readily available hydroxy-endoperoxide precursor.
Closed-loop myrtle ketone analogue and application thereof to antibacterial medicament
-
Paragraph 0024; 0027; 0055; 0056, (2018/12/02)
The invention discloses a closed-loop myrtle ketone analogue and application thereof to an antibacterial medicament. The structure of the closed-loop myrtle ketone analogue or a pharmaceutically-acceptable salt thereof is shown as a formula (1), wherein R is H, or a linear chain containing 1 to 15 carbon atoms, a branched chain, naphthenic base or an aryl group containing a benzene ring. The closed-loop myrtle ketone analogue can remarkably resist the bacteria of Vancomycin-resistant Enterococcus faecium (VRE), Methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus aureus, Bacilluscereus, Propionibacterium acnes, Enterococcuse faecalis or Staphylococcus epidermidis, has anti-bacterial activity equivalent to that of vancomycin which is regarded as the last barrier of anti-bacterial medicaments, and can kill the VRE which is out of control of the vancomycin. As proved by further research on the action mechanism of the closed-loop myrtle ketone analogue as well as investigation in biophysics and morphological researches, 11k can sterilize an MRSA bacterial strain through membrane hyperpolarization in order to induce the breaking of the membrane, which represents a very beneficial sterilizing mechanism. The formula (1) is shown in the description.
Biomimetic Total Syntheses of Callistrilones A, B, and D
Dethe, Dattatraya H.,Dherange, Balu D.,Das, Saikat
supporting information, p. 680 - 683 (2018/02/09)
A biomimetic total syntheses of antibacterial natural products (±)-callistrilones A, B, and D, the first triketone-phloroglucinol-monoterpene hybrids with an unprecedented [1]benzofuro[2,3-a]xanthene and [1]benzofuro[3,2-b]xanthene pentacyclic ring system
