Synthesis and Pharmacological Activities of 1,8-Naphthyridine Derivatives.

Synthesis, Anticonvulsant and Antihypertensive Activities of 8-Substituted Quinoline Derivatives

“…The increase in the carbon atom number at the 4th position of piperazine influenced the activity remarkably. In the propanol series (12)(13)(14)(15)(16)(17)(18)(19)(20), only compounds 13, 14, 19 and 20 were found to have a high degree of protection against MES-induced convulsions. 4-phenylpiperazino substituted compounds at the 3Ј position showed higher protection than the other substitutions at piperazine compounds.…”

“…We have already reported the potential anticonvulsant activity and the b-blocking activity of propanolamine, aminopropane and aminoethane from our laboratory. [14][15][16][17][18][19][20] To explore the heteroaryl and propanolamine/aminoethane combination, it was envisaged that chemical entities with both quinoline and aryloxypropanolamine/aminoethane moieties would result in compounds with interesting biological activities.…”

General Pathway for a Convenient One-Pot Synthesis of Trifluoromethyl-Containing 2-amino-7-alkyl(aryl/heteroaryl)-1,8-naphthyridines and Fused Cycloalkane Analogues

“…In parallel to the growing interest in the synthesis of 1,8-naphthyridines to provide biologically active molecules, a large number of publications have reported that several of their derivatives possess antibacterial [ 4 ], antimycobacterial [ 5 ], antitumor [ 6 ], anti-inflammatory [ 7 , 8 ], analgesic [ 8 ], antiplatelet [ 9 ], gastric antisecretary [ 10 ], local anaesthetic [ 11 ], anticonvulsant [ 12 ] and antihypertensive activity [ 13 , 14 ], besides being associated with β-adrenergic blocking properties [ 15 ]. Some 1,8-naphthyridine compounds have been patented as fungicides, bactericides, insecticides, herbicides, anxiolytic, antihypertensives, antiarrhythmics and also as immunostimulants [ 2 , 16 , 17 , 18 , 19 ].…”

Effects of anti-inflammatory [1, 2, 4]triazolo[4, 3-a] [1, 8]naphthyridine derivatives on human stimulated PMN and endothelial cells: an in vitro study

“…[ 1 , 8 ]naphthyridine derivatives have been reported to possess antibacterial [ 4 ], antymicobacterial [ 5 ], antitumoral [ 6 ], anti-inflammatory [ 7 ], antiplatelet [ 8 ], gastric antisecretary [ 9 ], antiallergic [ 10 ], local anaesthetic [ 11 ] and benzodiazepine receptor activities [ 12 ]. [ 1 , 8 ]naphthyridine derivatives are also reportedly associated with positive ionotropic [ 13 ], β-adrenergic blocking [ 14 ] and anti-hypertensive [ 15 ] activities. Recently, Roma et al [ 16 ] synthesized a series of new derivatives, the substituted 5-amino[ 1 , 2 , 4 ]triazolo [4.3- a ][ 1 , 8 ]naphtyridine-6-carboxamides, in order to obtain novel interesting anti-inflammatory agents.…”