The cinchona alkaloids cinchonidine and cinchonine belong to the most efficient chiral modifiers for the noble metal-catalyzed enantioselective hydrogenation of C=O and C=C bonds. Under reaction conditions these modifiers are coadsorbed on the noble metal surface with hydrogen. Using density functional theory, we studied the effect of coadsorbed hydrogen on the adsorption mode of cinchonidine a...

The intraerythrocytic malaria parasite constructs an intracellular haem crystal, called haemozoin, within an acidic digestive vacuole where haemoglobin is degraded. Haem crystallization is the target of the widely used antimalarial quinoline drugs. The intracellular mechanism of molecular initiation of haem crystallization, whether by proteins, polar membrane lipids or by neutral lipids, has no...

The relationship between expression of nucleoside diphosphate kinase (NDP kinase)/nm23, c-Ha-ras, and c-myc genes and metastatic potential was assessed in rat-transplantable osteosarcoma lines, derived from spontaneous and chemical carcinogen (4-hydroxyamino quinoline 1-oxide)-induced osteosarcomas in Fischer 344/NS1c rats. These osteosarcomas possess metastatic potential and highly metastatic ...

Immobilization of poly[8-methacroyloxy-quinoline] on a natural saponite surface immediately after polymer formation has been performed. The adsorption properties the modified adsorbent with resp...

The crystal structures of di-chlorido-palladium(II), -platinum(II) and -rhodium(III) complexes containing 8-(di-phenyl-phosphan-yl)quinoline, (SP-4)-[PdCl2(C21H16NP)], (1) [systematic name: di-chlor-ido-(8-di-phenyl-phosphanyl-quinoline)-palladium(II)], (SP-4)-[PtCl2(C21H16NP)]·CH2Cl2, (2) [systematic name: di-chlorido-(8-di-phenyl-phos-phanyl-quinoline)-platinum(II) dichlorometh-ane monosolvat...

Quinoline-2-carbohydrazide (3) was reacted with aryl or alkyl isothiocyanates to give the corresponding quinoline thiosemicarbazides (4a-e). Cyclization of the substituted thiosemicarbazides with sodium hydroxide led to the formation of 5-(quinolin-2-yl)2H-1, 2, 4-triazole-3(4H)-thiones (5a-e). Desulfurization of thiosemicarbazides by mercuric oxide gave 5-(quinolin-2-yl)-1, 3, 4-oxadiazol2-ami...

HIV-1 integrase (IN) is essential for virus replication and represents an important multifunctional therapeutic target. Recently discovered quinoline-based allosteric IN inhibitors (ALLINIs) potently impair HIV-1 replication and are currently in clinical trials. ALLINIs exhibit a multimodal mechanism of action by inducing aberrant IN multimerization during virion morphogenesis and by competing ...

In the title compounds, N-(5-acetyl-2-methyl-phen-yl)quinoline-2-carboxamide [C19H16N2O2, (I)], N-(5-acetyl-2-bromo-phen-yl)quinoline-2-carboxamide [C18H13BrN2O2, (II)] and N-(5-acetyl-2-ethynylphen-yl)quinoline-2-carboxamide [C20H14N2O2, (III)], the quinoline ring system is essentially planar and forms a dihedral angles of 3.68 (5) (I), 5.59 (7) (II) and 1.87 (6)° (III) with the acetyl-substit...

the first highly accelerated niementowski reaction of anhranilic acid with some amides or ketones under microwave irradiation leading to quinazolinones and quinoline derivatives is described. these reactions represent some examples of efficient microwave irradiation promoted organic condensation in which the reactions can be carried out in open vessels and provides products of high purity with ...

During their pathogenic blood stage, malaria parasites invade host erythrocytes where they digest hemoglobin. In the process, they release large quantities of potentially toxic hematin, which they convert to hemozoin. This is an insoluble microcrystalline product. The quinoline antimalarials, such as chloroquine form complexes with hematin and inhibit the formation of synthetic hemozoin (β-hema...