A series of novel quinoline-3-carboxamide derivatives 10-17 and 23-27 were designed and synthesized as cholesteryl ester transfer protein (CETP) inhibitors. All of them exhibited activity against CETP. Particularly, compounds 24 and 26 displayed the best activity against CETP with the same inhibitory rate of 80.1%.

Novel series of quinoline derivatives incorporating cyclopropyl ring and sulfone linkage as substituents have been synthesized, oxidation ethyl-2-cyclopropyl-4-(substituted phenylthio)quinoline-3-carboxylate was carried out to set phenyl sulfonyl)quinoline-3-carboxylate. An ecofriendly synthesis by the reaction glacial acetic acid 30% hydrogen peroxide at room temperature. The synthesized evalu...

Despite more than 25 years of research, the molecular targets of quinoline-3-carboxamides have been elusive although these compounds are currently in Phase II and III development for treatment of autoimmune/inflammatory diseases in humans. Using photoaffinity cross-linking of a radioactively labelled quinoline-3-carboxamide compound, we could determine a direct association between human S100A9 ...

In the title compound, C(19)H(13)N(3)O, the dihedral angle between the two quinoline systems is 11.54 (3)°. The mol-ecular conformation is stabilized by intra-molecular N-H⋯N and C-H⋯O hydrogen bonds, with N-H⋯N being bifurcated towards the two N atoms of the two quinoline rings. In the crystal, there are weak intermolecular π-π inter-actions present involving the quinoline rings [centroid-cent...

Quinoline-triazoles 2-((4-(diethoxymethyl)-1H-1,2,3-triazol-1-yl)methyl)quinoline (1), 2-((4-(m-tolyl)-1H-1,2,3-triazol-1-yl)methyl)quinoline (2) and 2-((4-(p-tolyl)-1H-1,2,3-triazol-1-yl)methyl)quinoline (3) have been prepared with CuAAC click reactions and used as a model series to probe the relationship between lattice H-bonding interaction and crystal direction of growth. Crystals of 1-3 ar...

Quinoline is a hepatocarcinogen in rats and mice and a well-known mutagen in bacteria after incubation with rat liver microsomes. The specific cytochrome P450 enzymes involved in quinoline metabolism in human and rat liver microsomes were determined using cDNA-expressed cytochrome P450s, correlations with specific cytochrome P450-linked monooxygenase activities in human liver microsomes and inh...

The Friedländer reactions of acetylbenzenes and 2-acetylpyridine with 3-aminonaphthalene-2-carbaldehyde afforded the corresponding 2-phenylbenzo[g]quinoline and 2-(pyrid-2-yl)benzo[g]quinoline, respectively. The same reactions of 3-aminonaphthalene-2-carbaldehyde with 1,2-, 1,3-, 1,4-di- and 1,3,5-triacetylbenzenes, however, afforded a series of corresponding (benzo[g]quinolin-2-yl)benzenes as ...