Palladium catalyzed Suzuki-Miyaura cross-coupling of 6,8-dibromo-4-chloroquinoline-3-carbaldehyde with arylboronic and arylvinylboronic acid derivatives in the presence of potassium carbonate in aqueous dioxane afforded the corresponding 4,6,8-triarylquinoline-3-carbaldehydes, exclusively. These products were transformed into 4,6,8-triaryl-3-(4-fluorophenyl)amino)-N-(quinolin-3-yl)methylenes an...

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 ...

An efficient and direct procedure for the synthesis of benzo[h]-indeno[1,2-b]-quinoline derivatives has been described. The procedure employs a three-component condensation reaction in one-pot using 2H-indene-1, 3-dione, naphthalen-1-amine,and aldehydes in the presence of catalytic amount of L-prolinein aqueous media.

Abstract: Objective(s): In recent years, the chemistry of 2-chloroquinoline-3-carbaldehydes have received considerable attention owing to their synthetic and effective biological importance which exhibits a wide variety of biological activity, N1,N4-bis((2-chloroquinolin-3-yl)methylene)benzene-1,4-diamine derivatives that synthesized from 2-chloroquinoline-3-carbaldehydes may have biological ef...

Mast cells, neutrophils and macrophages are important inflammatory cells that have been implicated in the pathogenesis of acute and chronic inflammatory diseases. To explore a novel anti-inflammatory agent, we have synthesized certain 4-anilinofuro[2,3-b]quinoline and 4-phenoxyfuro[2,3-b]quinoline derivatives and evaluated their anti-inflammatory activities by reaction of 3,4-dichlorofuro[2,3-b...

Based on the structure of natural product andrographolide, a series novel 12-quinoline substituted derivatives 9 were designed and synthesized. In preliminary biological evaluation, these synthesized compounds showed prominent anti-platelet aggregation activities in response to thrombin adenosine diphosphate (ADP) agonists. Among them, compound 9o (inhibition rate 55.73%, IC50 0.36 µM/L) had hi...

An air-stable catalyst system Ir-(P-Phos) catalyst was found to be highly effective in the asymmetric hydrogenation of quinoline derivatives. The catalyst immobilized in DMPEG was efficiently recovered and reused eight times, retaining reactivity and enantioselectivity.

Quinoline and its derivatives represent an important class of nitrogen containing heterocycles because they are useful intermediates in organic synthesis biological activities such as antiasthmatic, anti-inflammatory, anti- cancer, antimalarial activity. A quinoline eight compounds was successfully synthesized characterized by FT-IR, 1H NMR, 13C NMR mass spectral analysis. Therefore, the new wi...

An efficient and direct procedure for the synthesis of benzo[h]-indeno[1,2-b]-quinoline derivatives has been described. The procedure employs a three-component condensation reaction in one-pot using 2H-indene-1, 3-dione, naphthalen-1-amine,and aldehydes in the presence of catalytic amount of L-prolinein aqueous media.

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 w...