Eight quinoxalinone derivatives were synthesized and investigated for some neuropharmacological effects (analgesia, sedation, convulsion, anxiety, memory and psychosis) in mice and rats. In the CNS depressant activity, N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide is the most active, while the other compounds appear variously dose-dependent. Only three of the compounds showed anxiolytic effect, with N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide showing the highest activity at 2.5 mg/kg. At the dose of 30 mg/kg, 6-nitro-1,4-dihydroquinoxaline-2,3-dione showed a better anxiolytic effect in mice than diazepam (dose: 1 mg/kg), while 1,2,3,4-tetrahydroquinoxaline-2,3-dione (dose: 25 mg/kg) showed a comparative effect to diazepam. 6-Chloro-1,4-dihydro-quinoxaline-2,3-dione and N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamideshowed significant anticonvulsant action. None of the compounds showed any analgesic or antidopaminergic effect. The LD50 (24 h) calculated for the compounds were between 74 and 160 mg/kg i.p.
Studies on the synthesis of some sulfa quinoxaline has generate a considerable reputation as a result of their outstanding biochemical properties. This recent study was designed to prepared some sulfa quinoxaline hydrazone derivatives and studying their antimicrobial potency. The 3-methyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonohydrazone derivatives were synthesized by the reactions of 3-methyl-2-oxo-1,2-dihydroquinoxaline-6-sulfonohydrazide and six substituted benzaldehydes and examined for their possible antibacterial potency. The synthetic compounds exhibited wide-ranging spectrum action counter to twenty-four bacteria strains with minimum inhibitory concentrations values 0.0313 - 0. 250 mg/mL. This is a suggestion that such compounds could be used to formulate antibiotics to circumvent the problem of increasing resistance by pathogens to the existing synthetic antibiotics.
Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties.
Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The acetylcholinesterase and butyryl cholinesterase inhibitions were determined by Spectro photochemical analysis of acetylthiocholine and butyryl choline chloride.
Results: Compounds 6 (IC50 = 30±3 µg/mL) and 4 (IC50 = 141±60 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 4 (IC50 = 102±10 µg/mL), 5 (IC50 = 105 ± 20 µg/mL) and 2 (IC50 = 190 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase.
Conclusion: The considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities of the synthesized compounds makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.
Aims: This aims of this study was to continue the effort to synthesis new quinoxaline-based heterocycles and study its antibacterial properties.
Objective: This study was designed to reacts 3,6-dimethylquinoxaline-2-hydrazine with some substituted aromatic ketones and study their antibacterial properties on some locally and clinically isolated bacterial strains.
Materials and Methods: Five 3,6-dimethylquinoxaline-2-hydrazone derivatives were synthesized from the reactions of 3,6-dimethylquinoxaline-2-hydrazine with various substituted aromatic ketones. The products were then tested for their potential antibacterial properties.
Results: All the synthesized compounds were found to be active against all the bacterial strains investigated in this study. It was observed that the zones of inhibition observed for the synthesized compounds against the test organisms ranged between 15 mm and 38 mm. The MIC observed for the synthesized compounds ranged between 0.0313mg/mL and 0.125 mg/mL, while that of the standard antibiotic, streptomycin, varied between 0.0313 mg/mL and 0.500 mg/mL and those observed for tetracycline falls between 0.0313 mg/mL and 0.500 mg/mL. The minimum bactericidal concentrations exhibited by the synthesized compounds ranged between 0.0625 mg/mL and 0.250 mg/mL
Discussion and conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.
Aims: This studies aims at the synthesis of new heterocyclic systems and study its biological and pharmacological properties.
Objective: This study was designed to synthesized some quinoxaline-2,3-dione with sulfonamide moiety, characterize the synthesized compounds, and study the antimicrobial properties of the synthesized compounds on some bacterial strains.
Materials and Methods: Six quinoxaline-6-sulfonohydrazone derivatives were synthesized by reacting quinoxaline-6-sulfonohydrazine with some substituted benzaldehydes and ketones. The compounds were tested for their potential antibacterial properties.
Results: All the test compounds possessed promising antibacterial property against a panel of bacterial strains used for this study. The MIC values exhibited by these compounds ranged between 0.0313 and 0.250 mg/mL. Among the compounds tested, compound 2 showed appreciable antibacterial activity.
Discussion and Conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects towards all the bacterial strains, particularly, compound 2 This is an indication that such compounds possessing broad spectrum activities will be useful in formulating antimicrobial compounds which could be used to treat infections caused by pathogens that are now developing resistance against the available antibiotics.
Ludwigia abyssinica and Ludwigia decurrens are two plant species of the genus Ludwigiaused traditionally for the treatment of various skin, gastrointestinal, wound and bone joint disorders in Nigeria. The antibacterial and antifungal properties of extracts from the leaves of both plants against clinically important species of bacteria and fungi were examined. The two plant species produced activities with absolute similarity. The n-butanol extract was the most potent with maximum zone of inhibition (32.0 mm) followed by the ethyl acetate extract (12.0 to 31.0 mm) amongst other extracts (aqueous, dichloromethane and n-hexane). The n-butanol extract exhibited broad spectrum activity against all test bacteria and fungi and compared favourably with standard reference drugs – ampicillin, streptomycin and amphotericin B. The minimum inhibitory concentrations (MIC) exhibited by both n-butanol and ethyl acetate extracts against test bacteria species ranged between 0.625 to 5.0 mg ml-1 and 1.25 to 5.0 mg ml-1, respectively. The killing rate of the minimum bactericidal concentration (MBC) of n-butanol extract of L. abyssinica on Escherichia coliwas about 99.3% in 120 min while it was about 98.2% for Staphylococcus aureus. The phytochemical screening of crude extracts from the leaves of L. abyssinica and L. decurrens revealed the presence of only alkaloids and tannins. This study establishes the effective ethnomedicinal use of these plants in the treatment of various infectious diseases. There is high potential for the exploitation of the plants for development of new, novel antimicrobial agents.
Key words: Ludwigia abyssinica, Ludwigia decurrens, Onagraceae, antibacterial, antifungal, phytochemical constituent.
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Twelve phenylglyoxylic acid derivatives were synthesized, characterized and investigated for their antibacterial activity against nine Grampositive and four Gramn egative bacterial isolates. Some of the synthesized compounds exhibited broad spectrum activity against the bacterial strains, with 2�(2�(acetylamino)phen yl)�N� (2�chlorophenyl)�2�oxoacetamide (9) being the most active, having MIC values of 7.8�1000 5g/ml and MB C of 31.3�2000 5g/ ml Seven of the phenylglyoxylic acid derivatives were investigated for their antiinflammatory activity (acute inflammation, pulmonary oedema and leucocyte counts) in mice. The reduction in oedema formation was between 22�67 % for all the synthesized compounds. The compounds showed significant antiinflammatory activity with 2�(2�(acetylamino)phenyl)�N�(2,4�dich lorophenyl)�2�oxoacetamide (13) being the most acti ve, while others appear variously dosedependent.
Aims: This aims of this study was to synthesis new quinoxaline-based heterocycles and study its antibacterial properties.
Objective: This study was designed to synthesis some 3-methyl-6-nitroquinoxaline-2-one with hydrazine moiety, characterize the synthesized compounds, and study their antibacterial properties on some bacterial strains.
Materials and Methods: Six 3-methylquinoxaline-2-hydrazone derivatives were synthesized by reacting 2-hydrazinyl-3-methyl-6-nitroquinoxaline with various substituted acetophenones. The hydrazones were screened for their potential antibacterial properties.
Results: All the test compounds were found to possessed promising antibacterial properties against a panel of bacterial strains screened for this study. The MIC values exhibited by these compounds ranged between 0.0313 and 0.250 mg/mL. The lowest MBC of the compounds against the test organism was 0.0625 mg/mL while the highest MBC was 0.250 mg/mL.
Discussion and Conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.
Aim: To evaluate the antimicrobial and antioxidant activities of bioactive compounds isolated from Annona muricata (Linn.) leaf extract.
Study Design: In vitro antimicrobial assay of bioactive compounds isolated from solvent fractions of plant leaf extract against selected clinical bacterial and fungal isolates. Antioxidant assay of plant leaf extract.
Place and Duration of Study: All the work was carried out in the Departments of Chemistry and Microbiology, Obafemi Awolowo University, Ile-Ife, Nigeria between March, 2015 and January, 2016.
Methodology: Isolation of bioactive compounds was by column and thin layer chromatographic techniques. Isolated compounds were characterized by nuclear magnetic resonance spectroscopic analysis. Antimicrobial activities were evaluated by disc diffusion and broth microdilution methods while antioxidant activity was investigated using the 2,2-dipheny-1-picrylhydrazyl (DPPH) radical-scavenging assay.
Results: Two compounds kaempferol-3-O-glucoside (1) and 1-(4-Hydroxyphenyl)-3-Phenylpropan-1-one (2) were isolated from the ethyl acetate fraction of leaf extract of A. muricata. The two compounds showed broad spectrum antimicrobial activities with zones of inhibition ranging from 26.00 ± 1.73 to 31 ± 1.00 mm and 17.33 ± 1.15 to 31.33 ± 1.15 mm respectively, for compounds 1 and 2 for the test bacteria species and 15.33 ± 1.15 to 31.33 ± 1.15 mm and 17.67 ± 0.58 to 29.67 ±1.53 mm respectively, for compounds 1 and 2 for the test fungi. Minimum inhibitory concentrations ranged between 0.625-5.00 µg/mL and 1.25-5.00 µg/ml respectively, for compounds 1 and 2. Minimum bactericidal concentrations ranged between 2.5-10.00 µg/mL for both compounds which compared favourably with the reference drugs used. DPPH radical-scavenging activities were IC50 = 13.41 ± 0.64 µg/mL and 7.42 ± 0.90 µg/mL for compounds 1 and 2 respectively, compared with IC50 = 51.99 ± 1.44 µg/ml obtained for the standard ascorbic acid. The results show that both isolated compounds from A. muricata leaf possess in vitro antimicrobial and antioxidant properties and they may be useful as active ingredients in antimicrobial drug formulations and as agents for the control of free radical-related pathological disorders.
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