The synthesis and structure-activity-relationship (SAR) for a series of N-substituted piperazinyl carbamoyl 7-15 and piperazinyl acetyl 18-26 derivatives of tetrahydropapaverine have been carried out. The general synthetic methods of carbamoyl tetrahydropapaverine analogues involve N-substituted piperazines and carbamoyl imidazole tetrahydropapaverine as starting materials. Another route for sy...

Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...

Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...

A series of N-[2-(8-metoxy-2H-chromen-2-one)ethyl] piperazinyl quinolones containing a carbonyl related functional groups (oxo or oxyimino) on the ethyl spacer of coumarin and piperazin rings was synthesized and studied for their antibacterial and antifungal activities . The synthesis of compounds (6a-6l) was achieved through the versatile and efficient synthetic route that involved reaction of...

quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial dna gyrase and topoisomerase iv that efficiently inhibit dna replication and transcription by generating several double-stranded dna break. some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase ii and substantial dose-dependent cy...

3-Substituted 2-quinolones are obtained via a novel, metal-free transannulation reaction of 2-substituted indoles with 2-nitroalkenes in polyphosphoric acid. The reaction can be used in conjunction with the Fisher indole synthesis offering a practical three-component heteroannulation methodology to produce 2-quinolones from arylhydrazines, 2-nitroalkenes and acetophenone.

A series of 4-amino-3-[[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]thio]-5-(substituted phenyl)[1,2,4]triazoles (5a-f) and the isomeric 4-amino-2-[2-[4-(2-methoxyphenyl)-1piperazinyl]ethyl]-5-(substitutedphenyl)-2,4-dihydro-3H[1,2,4]triazole-3-thiones (6a-f) and a series of 3-[[2-[4-(2-methoxy or 2-nitrophenyl)1-piperazinyl]ethyl]thio]-5-(substituted phenyl)[1,2,4]triazoles (8a-i) were synthesi...

The Winterfeldt oxidation (NaOH, DMF, air, rt) of substituted 1,2,3,4-tetrahydro-γ-carbolines has been developed, which provides a convenient and efficient method for the synthesis of the corresponding dihydropyrrolo[3,2-b]quinolones in moderate to excellent yields (38-94%). The generality and substrate scope of this reaction are explored and a possible mechanism is proposed. The results imply ...

Novel anthranilic acid derivatives having substituted N-acyl side chains were designed and synthesized for evaluation as plasminogen activator inhibitor-1 (PAI-1) inhibitors. Compounds with a 4-diphenylmethyl-1-piperazinyl moiety on the acyl side chains in general exhibited potent in vitro PAI-1 inhibitory activity and good pharmacokinetic profiles after oral administration in rats. Compound 16...

Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...