Table 1 - uploaded by Mihaela Holban
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New amidic compounds with biologic activity, derived from 5-nitroindazol-1-yl-acetic acid have been synthesised and their chemical structure was confirmed by elemental and spectral analysis (FT-IR, 1 H-NMR, 13 C-NMR and mass spectrometry). The incorporation of some of the amides into sodium alginate and pectin based microcapsules, prepared by polym...
Context in source publication
Context 1
... evaluation of the biologic activity for the synthesised amide derivatives (II-VI) and polymer particles loaded with compounds II and III consisted in determining the toxicity and antibacterial effect of the new amides of 5- nitroindazol-1-yl acetic acid (II-VI) and alginate/pectin particles loaded with compounds II or III (Table 1). ...
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Citations
A series of new sulfonamide and carbamate derivatives of 5-nitro-1H-indazole was synthesized in good yields. The structures of all the newly synthesized compounds were confirmed by IR, ¹H, ¹³C-NMR, Mass spectra and elemental analysis. The compounds 9a and 9f showed high antibacterial activity against L. bacillus and S. aureu, 9f and 9j exhibited good activity against E. coli and P. florescensa, whereas the compounds 9a, 9d. 9f and 9j showed good antifungal activity against tested fungal strains, however, compared to all the compounds 9e and 9h exhibited significant activity against A. niger and P. chrysogenum respectively.
Infectious diseases and the development of their resistance to antimicrobial agents are alarming issues worldwide and consistent efforts are being made to develop efficient antimicrobial agents. In this perspective, a series of novel ammonium and amide derivatives of pyranocoumarin and coumarin were synthesized and evaluated for their antimicrobial activity. Among them, six compounds exhibited significant activity against gram-positive bacteria Bacillus cereus (MTCC 430) and Bacillus subtilis (MTCC 121) and a gram-negative bacterium Pseudomonas aeruginosa (MTCC 741). The compound N,N,N-triethyl-10-(4,8,8-trimethyl-2-oxo-2,6,7,8-tetrahydropyrano[3,2-g]chromen-10-yloxy)decan-1-aminium bromide (16) exhibited the highest antibacterial activity with MIC value of 5 μg/ml in MDA. Compounds 17 and 18 exhibited modest antifungal activity with MIC of 6.25 μg/ml against Trichophyton rubrum (clinical isolate) in MDA. Haemolytic assay results demonstrated that three out of six compounds were safe at their respective MIC values. These results provide insights for further optimization of the scaffolds for designing the next generation of compounds as lead antimicrobial agents.
