A simple, clean and efficient method for the synthesis of spiro[pyrimido[4,5-b]quinoline-5,5'-pyrrolo[2,3-d]pyrimidine]-pentaone derivatives by condensation reaction of 6-amino-uracils and isatins in aqueous media is reported. These products were evaluated in vitro for their antibacterial activities.

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%.

α-Enone 1, reacts with hydrazines, hydroxylamine hydrochloride, thiourea, diethylmalonate, malononitrile ethyl cyanoacetate to give the corresponding indazole, oxime, isoxazole, quinazoline, chromene and quinoline derivatives. The structures of all the synthesized compounds were confirmed by micro analytical and spectral data. The antimicrobial and the antitumor activities of some of the synthe...

The lack of novel drugs in development and the combination increased incidence drug-resistant strains bacteria has created need for search new antimicrobials as well original strategies to fight bacterial resistance. In this context, a series polyamine quinoline derivatives were prepared biologically evaluated, identifying compounds able sensitize doxycycline activity towards Gram-negative P. a...

Quinoline derivative SGI-1027 (N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide) was first described in 2009 as a potent inhibitor of DNA methyltransferase (DNMT) 1, 3A and 3B. Based on molecular modeling studies, performed using the crystal structure of Haemophilus haemolyticus cytosine-5 DNA methyltransferase (MHhaI C5 DNMT), which suggested that the quinoline...

DNA intercalators belong to aromatic heterocyclic compounds interacting reversibly with DNA. These compounds have been used extremely as cytotoxic agents against cancer. In this study, the synthesis and biological activity of some novel derivatives of cyclopenta [b] quinoline-1, 8-dione as new intercalating agent were investigated. Twenty novel derivatives of cyclopenta [b] quinoline-1, 8-dione...

The regioselective 2,2,2-trifluoroethoxylation at the C5 position of amides derived from 8-aminoquinoline has been developed. In presence PIDA, an unprecedented and undirected transition metal-free transformation was achieved using readily available appealing 2,2,2-trifluoroethanol as fluorinated source. selective distal array in moderate to good yields (12 examples, up 61 % yield). This approa...

Isatin (2,3-dioxindole) is a benzopyrrole derivative that belongs to large class of heterocyclic chemicals. derivatives are essential synthetic substrates can be utilized as starting materials build wide range heterocycles with diverse applications in pharmaceutical sciences. therefore have recently gained lot attention. This review emphasizes on the Schiff base from isatin, isatin quinoline/fl...

Aryl free-radicals generated at the C-7 position of ethyl indole-2-carboxylates bearing N-allyl and propargylic groups triggered intramolecular cyclizations to furnish a new class of Duocarmycin analogues, formal ethyl pyrrolo[3,2,1-ij]quinoline-2- carboxylate derivatives, through the less favorable 6-endo-trig cyclization mode.