24632-44-8Relevant articles and documents
1,8-Naphthyridines IX. Potent anti-inflammatory and/or analgesic activity of a new group of substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6- carboxamides, of some their Mannich base derivatives and of one novel substituted 5-amino-10-oxo-10H-pyrimido[1,2-a][1,8]naphthyridine-6-carboxamide derivative
Di Braccio, Mario,Grossi, Giancarlo,Alfei, Silvana,Ballabeni, Vigilio,Tognolini, Massimiliano,Flammini, Lisa,Giorgio, Carmine,Bertoni, Simona,Barocelli, Elisabetta
, p. 394 - 405 (2014)
A new group of 5-(alkylamino)-9-isopropyl[1,2,4]triazolo[4,3-a][1,8] naphthyridine derivatives bearing a CONHR group at the 6-position (1c-g), designed to obtain new effective analgesic and/or anti-inflammatory agents, were synthesized and tested along with three new 9-alkyl-5-(4-alkyl-1-piperazinyl)- N,N-diethyl [1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides (2b-d). Besides, a new class of analogues of compounds 1 and 2, bearing a Mannich base moiety at the 9-position (12a-d), as well as the novel N,N-diethyl-5- (isobutylamino)-8-methyl-10-oxo-10H-pyrimido[1,2-a][1,8]naphthyridine-6- carboxamide (15) were prepared and tested. Compounds 1c-g exhibited very interesting anti-inflammatory properties in rats, whereas compounds 2b-d and 15 proved to be endowed with prevalent analgesic activity frequently associated with sedative effects in mice. On the contrary, the Mannich bases 12a-d resulted inactive. The most effective (80% inhibition of oedema) and potent (threshold dose 1.6 mg kg-1 with 31% inhibition of oedema) anti-inflammatory compound 1d did not show gastrolesive effects following 100 mg kg-1 oral administration in rats.
Synthesis, biological activities and docking studies of piperazine incorporated 1, 3, 4-oxadiazole derivatives
Bhati, Shipra,Kumar, Vijay,Singh, Simranjeet,Singh, Joginder
, p. 197 - 205 (2019/05/08)
New series of 1, 3, 4-oxadiazoles incorporating piperazine scaffolds in a single molecular framework has been reported. The structures of the synthesized derivatives were assigned by IR, NMR and mass spectral techniques. The hybrid compounds were evaluated for their antimicrobial, antitubercular and antioxidant activities. The observed MIC values of anti-tubular activities for the molecule 3a, 3b, 3c, 3d and 3e were 6.25, 3.12, 3.12, 1.60 and 50.0 μg/ml respectively. As compared to ascorbic acid (IC50 = 62.91 μg/ml), molecule 3a exhibited better antioxidant activities (IC50 = 36.72 μg/ml). Also, all molecules have shown significant antimicrobial activities. In addition, docking simulations were performed to study ligand-protein interactions and to determine the probable binding conformations. In drug likeness model study compound 3b possessed maximum drug likeness model score (0.75) similar to the standard drug streptomycin. The compound 3a, 3b and 3c were emerged as potential derivatives in the series and could serve as lead compound for the development of potential therapeutic agents.
