A class of hybrid molecules consisting of 4-aminoquinoline and pyrimidine were synthesized and tested for antimalarial activity against both chloroquine (CQ)-sensitive (D6) and chloroquine (CQ)-resistant (W2) strains of Plasmodium falciparum through an in vitro assay. Eleven hybrids showed better antimalarial activity against both CQ-sensitive and CQ-resistant strains of P. falciparum in comparison to standard drug CQ. Four molecules were more potent (7-8-fold) than CQ in D6 strain, and eight molecules were found to be 5-25-fold more active against resistant strain (W2). Several compounds did not show any cytotoxicity up to a high concentration (60 μM), others exhibited mild toxicities, but the selective index for the antimalarial activity was very high for most of these hybrids. Two compounds selected for in vivo evaluation have shown excellent activity (po) in a mouse model of Plasmodium berghei without any apparent toxicity. The X-ray crystal structure of one of the compounds was also determined.
A nanocomposite consisting of reduced
graphene oxide and zinc oxide
nanoparticles (RGO/ZnO) with unique structural features was developed
as an efficient, sustainable, amphiphilic, heterogeneous catalyst
for the synthesis of various 3-substituted indoles in water. The catalyst
was recycled six times without significant loss in catalytic activity.
The higher environmental compatibility and sustainability factors
such as smaller E-factor and higher atom economy make the present
methodology a true green and sustainable process for the synthesis
of various biologically important 3-substituted indoles.
Development
of nanocatalysts for a chemical reaction with ideal
values in green chemistry metrics is considered to be a challenging
task to achieve sustainable chemistry. With this aim, we herein report
a hierarchically porous sphere-like copper oxide (HS-CuO) nanocatalyst
to afford benzofuranamine and dihydro-benzofuranamine isomers with
anomalous selectivity via O-annulated A3 coupling among salicylaldehydes,
secondary amines, and alkynes followed by cycloisomerization in the
absence of base and solvent. The anomalous selectivity of benzofuran
isomers was dependent on the electronic factors of substituents on
salicylaldehyde and the type of secondary amines used in the coupling
reaction. The HS-CuO nanocatalyst was recycled five times without
significant loss in its catalytic activity. The present method offers
several advantages over the reported methods such as wide substrate
scope with anomalous selectivity in the products, high yields in short
reaction time, avoided the usage of extra reagents such as additives/bases,
and showed ideal values of green chemistry metrics such as low E-factor
and process mass intensity (PMI), high atom economy (AE), reaction
mass efficiency (RME), and carbon efficiency (CE).
A novel copper supported on hydromagnesite
(Cu/HM) nanomaterial
was prepared by a simple impregnation method at room temperature and
characterized by PXRD, SEM, TEM, EDAX, XPS, ICP-AES and FT-IR techniques.
The EDAX and XPS results revealed the presence of 8.82 wt % of copper
in (+2) oxidation state. Three-component coupling of ketone and amine
with alkyne to afford tetrasubstituted propargylamine is known as
KA2 coupling, whereas the three-component reaction of aldehydes and
amine with alkyne to give propargylamine is considered as an A3-coupling
reaction. The Cu/HM was found to be an efficient heterogeneous catalyst
for KA2 coupling reaction under solvent free condition, and A3 coupling
strategy to afford the pyrrolo[1,2-a]quinolines in
DEG as a green solvent. The high catalytic activity of Cu/HM in the
A3 coupling strategy to afford propargylamine intermediate is due
to the synergistic effect of both Cu2+ and Mg2+ active sites. The versatility of Cu/HM catalyst was also studied
for the decarboxylative A3 and KA2 coupling strategies. The present
method offers several advantages such as simple procedure for the
catalyst preparation, versatile catalytic applications, cheap precursors,
higher yield of products in short reaction time, recovery and reusability
of the catalyst.
Copper mixed oxide NPs supported on a hematite surface were achieved using a facile hydrothermal method in a single step. The catalytic potential of the Cu@Fe2O3 NPs was explored for the synthesis of aminoindolizines and pyrrolo[1,2-a]quinolines.
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