- Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity
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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.
- Athanassopoulos, Constantinos M.,Baltas, Michel,Grellier, Philippe,Menendez, Christophe,Mouray, Elisabeth,Papaioannou, Dionissios,Pepe, Dionissia A.,Toumpa, Dimitra,André-Barrès, Christiane
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supporting information
p. 921 - 927
(2020/07/21)
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- Biomimetic Total Syntheses of Callistrilones A, B, and D
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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
- Dethe, Dattatraya H.,Dherange, Balu D.,Das, Saikat
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supporting information
p. 680 - 683
(2018/02/09)
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- Ring opening myrtle ketone analogue as well as preparation method and application thereof to antibacterial medicines
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The invention discloses a ring opening myrtle ketone analogue as well as a preparation method and application thereof to antibacterial medicines. The structure of the ring opening myrtle ketone analogue is shown in a formula (1) in the specification, wherein in the formula (1), R is H, a C1-C15 straight chain or branched chain or naphthenic base or an aromatic group. The ring opening myrtle ketone analogue has obvious activity of resisting Methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus aureus, Bacillus cereus, B.subtilis, B.thuringiensis or Escherichia coli, so the ring opening myrtle ketone analogue can be used for preparing bacterial infection resistant medicines and is especially applied to preventing and treating clinically common MRSA infectious diseases.
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Paragraph 0029; 0061-0062
(2017/02/24)
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- Synthesis of the acylphloroglucinols rhodomyrtone and rhodomyrtosone B
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In a sequential three-component coupling syncarpic acid, 3-methylbutanal and an acylated phloroglucinol were combined to the hydroxy ketone 3. Acid catalysis converted 3 directly to the natural product rhodomyrtosone B (2). The other isomer, the antibiotic rhodomyrtone (1) was obtained from 3 in a sequence of acid-catalyzed cyclization, retro Friedel-Crafts reaction, and reacylation. In preliminary assays both compounds showed potent antibiotic activity.
- Morkunas, Marius,Dube, Linda,G?tz, Friedrich,Maier, Martin E.
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supporting information
p. 8559 - 8563
(2013/09/12)
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- Process for producing 2,2,4,4-tetra-substituted 1,3,5-cyclohexanetriones
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Process for the preparation of 2,2,4,4-tetrasubstituted 1,3,5-cyclohexanetriones of the formula I, by reaction of a cyclobutane-1,3-dione of the formula II with an O or N nucleophile and a silylating reagent, and subsequent acetylation and cyclization.
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- SYNTHESIS of SYNCARPIC ACID and RELATED β-OXO δ-ENOL LACTONE VIA SELECTIVE O- or C- ACYLATION of PREFORMED ENOLATES
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Syncarpic acid 1 and the β-oxo-δ-enol lactone isomer 2 have been prepared in two steps starting from the readily available ketoester 6.Selective C- or O-acylation of the SiMe3 or Li enolates of 6 and intramolecular cyclisation of the new adducts 8 or 9 lead to 1 and 2 in good yields (48percent and 52percent respectively starting from ethyl isobutyrate).
- Benbakkar, M.,Baltas, M.,Gorrichon, L.,Gorrishon, J. P.
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p. 3241 - 3248
(2007/10/02)
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