7511-08-2Relevant articles and documents
3-aryl-indolinones derivatives as antiplasmodial agents: synthesis, biological activity and computational analysis
Luczywo, Ayelen,González, Lucía G.,Aguiar, Anna C. C.,Oliveira de Souza, Juliana,Souza, Guilherme E.,Oliva, Glaucius,Aguilar, Luis F.,Casal, Juan J.,Guido, Rafael V. C.,Asís, Silvia E.,Mellado, Marco
, (2021/03/18)
Malaria is an infectious illness, affecting vulnerable populations in Third World countries. Inspired by natural products, indole alkaloids have been used as a nucleus to design new antimalarial drugs. So, eighteen oxindole derivatives, aza analogues were obtained with moderate to excellent yields. Also, the saturated derivatives of oxindole and aza derivatives via H2/Pd/C reduction were obtained in good yields, leading to racemic mixtures of each compound. Next, the inhibitory activity against P. falciparum of 18 compounds were tested, founding six compounds with IC50 20 μM. The most active of these compounds was 8c; however, their unsaturated derivative 7c was inactive. Then, a structure-activity relationship analysis was done, founding that focused LUMO lobe on the specific molecular zone is related to inhibitory activity against P. falciparum. Finally, we found a potential inhibition of lactate dehydrogenase by oxindole derivatives, using molecular docking virtual screening.
Activity-directed expansion of a series of antibacterial agents
Chow, Shiao,Clarke, Justin E.,Leggott, Abbie,Nelson, Adam,O'Neill, Alex J.,Warriner, Stuart L.
, p. 8047 - 8050 (2020/08/03)
The feasibility of using activity-directed synthesis to drive antibacterial discovery was investigated. An array of 220 Pd-catalysed microscale reactions was executed, and the crude product mixtures were evaluated for activity against Staphylococcus aureus. Scale-up of the hit reactions, purification and evaluation, enabled expansion of a class of antibacterial quinazolinones. The novel antibacterials had MICs from 0.016 μg mL-1 (i.e. 38 nM) to 2-4 μg mL-1 against S. aureus ATCC29213. This journal is
Manganese-Catalyzed α-Alkylation of Ketones, Esters, and Amides Using Alcohols
Chakraborty, Subrata,Daw, Prosenjit,Ben David, Yehoshoa,Milstein, David
, p. 10300 - 10305 (2018/10/20)
Herein we report the manganese-catalyzed C-C bond-forming reactions via α-alkylation of ketones, amides, and esters, using primary alcohols. β-Alkylation of secondary alcohols by primary alcohols to obtain α-alkylated ketones is also reported. The reactions are catalyzed by a (iPr-PNP)Mn(H)(CO)2 pincer complex under mild conditions in the presence of (catalytic) base liberating water (and H2 in the case of secondary alcohol alkylation) as the sole byproduct.
