A process for producing carboxylic acid anhydrides by the carbonylation reaction of a carboxylic acid ester, derived from an alcohol and a carboxylic acid, with carbon monoxide containing a small amount of hydrogen in a liquid reaction medium in the presence of a Group VIII B catalyst to produce a carboxylic acid anhydride. The reaction medium comprises the Group VIII B catalyst, an organic halide, the carboxylic acid ester, an alkali metal salt, the carboxylic acid anhydride, the carboxylic acid, and at least one ionic liquid consisting of a cation and an anion where the cation of the ionic liquid has a nitrogen-containing heterocyclic structure. The ionic liquid has at least one of the following structural forms:
The reaction rate of the carbonylation reaction is increased by the use of the specified ionic liquid promoters.
Novel Conjugated Quinoline–Indoles Compromise Plasmodium falciparum Mitochondrial Function and Show Promising Antimalarial Activity
作者:Silvia C. Teguh、Nectarios Klonis、Sandra Duffy、Leonardo Lucantoni、Vicky M. Avery、Craig A. Hutton、Jonathan B. Baell、Leann Tilley
DOI:10.1021/jm400656s
日期:2013.8.8
A novel class of antimalarial compounds, based on an indol-3-yl linked to the 2-position of a 4-aminoquinoline moiety, shows promising activity against the malaria parasite, Plasmodium falciparum. Compounds with a quaternary nitrogen on the quinoline show improved activity against the chloroquine-resistant K1 strain. Nonquaternerized 4-amino-quinolines retain significant potency but are relatively less active against the K1 strain. Alkylation of the 4-amino group preferentially improves the activity against the chloroquine-sensitive 3D7 strain. The quinoline-indoles show only weak activity as inhibitors of beta-hematin formation, and their activities are only weakly antagonized by a hemoglobinase inhibitor. The compounds appear to dissipate mitochondrial potential as an early event in their antimalarial action and therefore may exert their activity by compromising Plasmodium mitochondrial function. Interestingly, we observed a structural relationship between our compounds and the anticancer and anthelminthic compound, pyrvinium pamoate, which has also been proposed to exert its action via compromising mitochondrial function.
Ashley et al., Proceedings of the Royal Society of London. Series B, Biological sciences, 1933, vol. 113, p. 293,298
作者:Ashley et al.
DOI:——
日期:——
MIZUYAMA K.; TOMINAGA Y.; MATSUDA Y.; KOBAYASHI G., CHEM. AND PHARM. BULL., 1979, 27, NO 12, 2879-2889
作者:MIZUYAMA K.、 TOMINAGA Y.、 MATSUDA Y.、 KOBAYASHI G.