scholarly journals Synthesis, Characterization of Thiazolidin-4-one, Oxazolidin-4-one and Imidazolidin-4-one Derivatives from 6-Amino-1,3-dimethyluracil and evaluation of their Antioxidant and Antimicrobial Agent

2021 ◽  
Vol 26 (4) ◽  
Author(s):  
Huda Al-Adhami ◽  
Suaad M. H. Al-Majidi
Keyword(s):  
Antimicrobial Agent ◽  
Schiff Bases ◽  
Chloroacetic Acid ◽  
Antimicrobial Activities ◽  
Mercaptoacetic Acid ◽  
One Pot ◽  
Subsequent Step ◽  
Antioxidant And Antimicrobial Activities

In this study, a new series of 6-amino-1,3-dimethyluracil derivative with 6-(3-substituted N-benzylidene)-1,3-dimethyl pyrimidine-2,4-dione-6-yl derivatives which were synthesized by using one pot synthesis. The reaction of 6-amino-1,3-dimethyluracil and different aromatic aldehyde in ethanol yielded Schiff bases (1-6). In the subsequent step reaction of Schiff bases )1-6) with 2-mercaptoacetic acid, 2-chloroacetic acid and 2-amino acetic acidn in Tetrahydrofuran yielded five membered heterocyclic rings of 6-amino-1,3-dimethyluracil derivative which includes: 2,3-thiazolidin-4-one (7-12), 2,3-oxazolidin-5-one (13-18), 2,3-imidazolidin-4-one (19-24) derivatives. The structures of newly synthesized compounds were confirmed by their physicochemical and spectral means FTIR, 1HNMR and 13CNMR. The synthesized compounds were evaluated in vitro for antioxidant and antimicrobial activities against four types of bacteria and four types of fungi

scholarly journals Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2696 ◽  
Author(s):  
Teran ◽  
Guevara ◽  
Mora ◽  
Dobronski ◽  
Barreiro-Costa ◽  
...  
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Drug Candidates ◽  
Development Of Resistance ◽  
Schiff Base Derivatives ◽  
Wide Range ◽  
Derivatives Of

Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded.

Characterization of bis‐Schiff bases synthesized using ZnFe 2 O 4 nanoparticles as catalyst, and examination of their antibacterial and in vitro cytotoxic properties

2020 ◽  
Vol 34 (4) ◽  
Author(s):  
Hamed Maaref ◽  
Enayatollah Sheikhhosseini ◽  
Mohammad Mehdi Foroughi ◽  
Mohammad Reza Akhgar ◽  
Shohreh Jahani
Keyword(s):  
Schiff Bases

scholarly journals Chemical analysis and evaluation of antioxidant and antimicrobial activities of fruit fractions ofMauritia flexuosaL. f. (Arecaceae)

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e5991 ◽  
Author(s):  
Carla de Fatima Alves Nonato ◽  
Débora Odília Duarte Leite ◽  
Rafael Caldas Pereira ◽  
Aline Augusti Boligon ◽  
Jaime Ribeiro-Filho ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Antifungal Drugs ◽  
Resistant Bacteria ◽  
Array Detector ◽  
Chloroform Fraction ◽  
Standard Samples ◽  
Antioxidant And Antimicrobial Activities

BackgroundFruit consumption is currently considered beyond the nutritional aspects because of the important roles in disease prevention and benefits to health. The objective of this study was to characterize the chemical profile and evaluate the antioxidant and antimicrobial properties of different fractions obtained from fruit pulps ofMauritia flexuosa(MFFs).MethodsInitially, chloroform, ethyl acetate and ethanol fractions were obtained from the pulps. Quantifications of total phenols and flavonoids were performed using the methods of Folin-Ciocalteu and complexation with aluminum chloride, respectively. Standard samples were used to identify and quantify phenolic acids and flavonoids using high-performance liquid chromatography with a diode-array detector (HPLC-DAD). The antioxidant capacity of the fractions was verified by sequestration of the free radical 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and iron chelating activity. The antimicrobial activity was determined using the microdilution method and the modulating activity was determined using sub-inhibitory concentrations of the fractions in association with antibiotics.ResultsThe chemical analyzes revealed the presence of catechin, caffeic acid, rutin, orientin, quercetin, apigenin, luteolin and kaempferol, where all are present in the ethyl acetate fraction. The fractions exhibited moderate antioxidant and antimicrobial activities against Gram-positive andCandidastrains in addition to modulating the activity of conventional antibiotics. The most expressive result was obtained from the association of the chloroform fraction with cefotaxime, which produced a synergistic effect, reducing the minimum inhibitory concentration (MIC) of the antibiotic from 1,024 to 256 μg/mL.DiscussionThe fractions presented a constitution rich in phenolic compounds, especially flavonoids. The data obtained demonstrated that the fractions presented moderate antioxidant activity by acting both as primary and secondary antioxidants. The fractions presented antimicrobial and antibiotic potentiating activities, being the first record of modulating effect of fractions of this species against the studied microbial strains, but failed in modulating the activity of antifungal drugs, indicating that this plant has the potential to be used in the development of therapeutic alternatives against resistant bacteria. The constitution phenolic the fractions may be responsible for their pharmacological properties in vitro.

scholarly journals Synthesis and Biological Evaluation of Aminonaphthols Incorporated Indole Derivatives

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Saundane Anand Raghunath ◽  
Kirankumar Nandibeoor Mathada
Keyword(s):  
Radical Scavenging ◽  
Antitubercular Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Secondary Amines ◽  
Anticancer Activities ◽  
One Pot ◽  
Antioxidant Power ◽  
Mic Value

An efficient one pot condensation of naphthols (1), 2,5-disubstituted indole-3-carboxaldehydes (2), and secondary amines (3) has been achieved using dichloromethane as a solvent, stirring at room temperature. Some of the new [(disubstituted amino)(5-substituted 2-phenyl-1H-indol-3-yl)methyl]naphthalene-ols (4) derivatives were prepared in good yields. The significant features of this method are simple work-up procedure, inexpensive nontoxic solvent, shorter reaction times, and excellent product yields. The structures of newly synthesized compounds (4a–r) are confirmed by their elemental analysis, FTIR, 1H and 13C NMR, and mass spectral data. These compounds were screened for their in vitro antioxidant, antimicrobial, antitubercular, and anticancer activities. Among the synthesized compounds (4a–r), the compound 4e exhibited highest activity for radical scavenging and ferric ions reducing antioxidant power activities; compounds 4b, 4h, and 4k showed good metal chelating activity. Compounds 4n and 4q showed excellent antimicrobial activities with MIC value 08 µg/mL against tested strains. Compounds 4h, 4k, 4n, and 4q exhibited promising antitubercular activity with MIC value 12.5 µg/mL. Compounds 4k and 4q exhibited 100% cell lysis at concentration 10 µg/mL against MDA-MB-231 (human adenocarcinoma mammary gland) cell lines.

scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIMICROBIAL ACTIVITIES OF BIS(CYCLOPENTADIENYL)TITANIUM(IV) COMPLEXES WITH SCHIFF BASES DERIVED FROM5-(SUBSTITUTED ARYL)-2-HYDRAZINO-1, 3, 4-OXADIAZOLE AND INDOLINE-2, 3-DIONE

2021 ◽  
Vol 9 (09) ◽  
pp. 900-909
Author(s):  
Anupama Srivastava ◽  
◽  
Shilpi Srivastava ◽  
Om. P. Pandey ◽  
Soumitra K. Sengupta ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Electrical Conductance ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Bacterial Strains ◽  
Monoclinic Crystal ◽  
Spectral Techniques ◽  
Concentration Method

Titanium(IV) complexes of type[(η5-C5H5)2TiCl(L)] have been synthesized by the reactions of bis(cyclopentadienyl)titanium(IV)dichloride with Schiff bases (LH) derived by the condensation of 5-(substituted aryl)-2-hydrazino-1,3,4-oxadiazole and indoline-2,3-dione in tetrahydrofuranin the presence oftriethylamine. All these complexes are soluble in PhNO2, DMF and DMSO.The complexes were characterized by elemental analyses, electrical conductance, magnetic susceptibility, UV-Vis, IR, 1H NMR, 13C NMR, XRD and SEM spectral techniques. Low molar conductance values indicate that they are non-electrolytes. The spectral data indicate5-coordinate geometry for the complexes.XRD pattern indicate that the complexes have monoclinic crystal system and particle sizes were found 49.36 nm (nano-size). In vitro antifungal activity of synthesized compounds was evaluated against fungi Aspergillusniger, Aspergillusflavus,ColletotrichumfalcatumandIn vitro antibacterial activity was determined by screening the compounds against gram negative (P. aeruginosa, S.typhi) and gram positive (S. aureus and B.subtilis) bacterial strains using minimum inhibition concentration method (MIC) by serial dilution technique. The titanocene(IV) complexes have higher antimicrobial effect than the parent Schiff bases.

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