7181-79-5Relevant articles and documents
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.
Ring opening myrtle ketone analogue as well as preparation method and application thereof to antibacterial medicines
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Paragraph 0029; 0061-0062, (2017/02/24)
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.
Process for producing 2,2,4,4-tetra-substituted 1,3,5-cyclohexanetriones
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, (2008/06/13)
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.