scholarly journals Synthesis and Spectral Identification of Three Schiff Bases with a 2-(Piperazin-1-yl)-N-(thiophen-2-yl methylene)ethanamine Moiety Acting as Novel Pancreatic Lipase Inhibitors: Thermal, DFT, Antioxidant, Antibacterial, and Molecular Docking Investigations

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2253 ◽  
Author(s):  
Ismail Warad ◽  
Oraib Ali ◽  
Anas Al Ali ◽  
Nidal Amin Jaradat ◽  
Fatima Hussein ◽  
...  
Keyword(s):  
Molecular Orbital ◽  
Schiff Bases ◽  
Theoretical Calculations ◽  
Antimicrobial Activities ◽  
Disk Diffusion Test ◽  
Physical Measurements ◽  
Dpph Method ◽  
Ic50 Values ◽  
High Yields

Three new tetradentate NNNS Schiff bases (L1–L3) derived from 2-(piperidin-4-yl)ethanamine were prepared in high yields. UV–Visible and FTIR spectroscopy were used to monitor the dehydration reaction between 2-(piperidin-4-yl)ethanamine and the corresponding aldehydes. Structures of the derived Schiff bases were deduced by 1H and 13C NMR, FTIR, UV–Vis, MS, EA, EDS, and TG-derived physical measurements. DFT/B3LYP theoretical calculations for optimization, TD-DFT, frequency, Molecular Electrostatic Potential (MEP), and highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) / were performed for L2. The in vitro antimicrobial activities of the three Schiff bases were evaluated against several types of bacteria by disk diffusion test using Gentamicin as the standard antibiotic. Schiff bases revealed good antioxidant activity by the DPPH method, and the IC50 values were compared to the Trolox standard. Pancreatic porcine lipase inhibition assay of the synthesized compounds revealed promising activity as compared to the Orlistat reference.

scholarly journals BSA binding affinity, free radical scavenging capacity and antibacterial activity of new Silver(I) complexes with Schiff base ligands

2020 ◽  
Vol 9 (3) ◽  
pp. 12
Author(s):  
Emir Horozić ◽  
Maida Šljivić Husejnović ◽  
Adem Bajrić ◽  
Merima Ibišević ◽  
Enida Karić ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Schiff Bases ◽  
Conformational Changes ◽  
Radical Scavenging ◽  
Bacterial Strains ◽  
Antimicrobial Screening ◽  
Dpph Method ◽  
Vis Spectroscopy ◽  
Ic50 Values

In this work, four silver(I) complexes with Schiff bases derived from ninhydrin and selected amino acids (methionine, histidine, cysteine, and phenylalanine) were synthesized. The aim of this study is to determine the potential biological activity of these complexes. FTIR and UV/VIS spectroscopy were used for structural characterization of the products. Antioxidant activity was examined in vitro using DPPH method. Antimicrobial screening was performed by diffusion technique on reference bacterial strains from the ATCC collection. Interaction with bovine serum albumin (BSA) was examined using UV/VIS spectroscopy. Based on the obtained spectral data, it is assumed that all Schiff bases coordinate the Ag(I) ion as a tridentate ONO donor ligand. The antioxidant activity of the synthesized compounds is extremely high, with a range of IC50 values of 0.023-0.06 mg/mL. Antimicrobial screening determined the inhibitory ability of almost all complexes for concentrations of 1 and 2 mg/mL, with zones of inhibition in the range of 9-19 mm. Examination of the interaction of BSA with Ag(I) complexes revealed the same change in the absorption maximum (hyperchromic shift) in the region of about 205 nm, which indicates that the interaction of BSA and the complex results in conformational changes of BSA.  

scholarly journals Chemical Analysis and Evaluation of Antioxidant, Antimicrobial, and Photoprotective Activities of Schinopsis brasiliensis Engl. (Anacardiaceae)

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Sarah Raquel Gomes de Lima-Saraiva ◽  
Fernanda Granja da Silva Oliveira ◽  
Raimundo Gonçalves de Oliveira Junior ◽  
Camila de Souza Araújo ◽  
Ana Paula de Oliveira ◽  
...  
Keyword(s):  
High Performance ◽  
Ethanolic Extract ◽  
Antimicrobial Activities ◽  
Physicochemical Analysis ◽  
Minimal Bactericidal Concentration ◽  
Native Plant ◽  
Protection Factor ◽  
Dpph Method ◽  
High Concentrations

Schinopsis brasiliensis Engl. is a native plant of Caatinga which has high concentrations of compounds capable of absorbing ultraviolet light, suggesting its potential application for the development of sunscreen preparations. After its identification and collection, this vegetable drug was submitted to a physicochemical analysis through the preparation of ethanolic extract. The phytochemical screening and analysis of extracts were carried out by high-performance liquid chromatography (HPLC) evaluation. The antioxidant activity of the extract was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and β-carotene bleaching test. Inhibitory hemolytic activity and morphological deformation of erythrocytes induced by H2O2 were also demonstrated and the antimicrobial activity was analyzed by the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) method. For the in vitro determination of the sun protection factor (SPF), the spectrophotometric method was used. From the analyses carried out with this species, this plant showed significant results for the antioxidant and antimicrobial activities, as well as sunscreen action. Important flavonoids were identified. These data are an important step for the development of new photoprotective cosmetic with Caatinga species, revealing importance and representing another incentive for the preservation of the species involved and analyzed in the study.

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.

Synthesis, spectral, theoretical studies and in vitro antimicrobial activities of novel diphenyltin(IV) complexes of Schiff bases derived from phenacylamine

2014 ◽  
Vol 28 (7) ◽  
pp. 537-544 ◽  
Author(s):  
Gökhan Şirikci ◽  
Nilgün Ancın ◽  
Selma Gül Öztaş ◽  
Gülgün Yenişehirli ◽  
Nurşen Altuntaş Öztaş
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Theoretical Studies

scholarly journals 1,2,4-Triazine Sulfonamides: Synthesis by Sulfenamide Intermediates, In Vitro Anticancer Screening, Structural Characterization, and Molecular Docking Study

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2324
Author(s):  
Danuta Branowska ◽  
Zbigniew Karczmarzyk ◽  
Ewa Wolińska ◽  
Waldemar Wysocki ◽  
Maja Morawiak ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Estrogen Receptor Alpha ◽  
Theoretical Calculations ◽  
Molecular Structures ◽  
Breast Cancer Cell Lines ◽  
In Vitro Tests ◽  
Molecular Docking Study ◽  
Ic50 Values

In this study, we synthesized novel sulfonamides with a 1,2,4-triazine moiety according to pharmacophore requirements for biological activity. All the synthesized compounds were tested in vitro to verify whether they exhibited anticancer activity against the human breast cancer cell lines MCF-7 and MDA-MB-231. Among them, two most active ones, having IC50 values of 50 and 42 µM, respectively, were found to show higher anticancer activity than chlorambucil used as the reference in the in vitro tests. In addition, two other compounds, which had IC50 values of 78 and 91 µM, respectively, exhibited a similar level of activity as chlorambucil. X-ray analysis carried out for two of the compounds confirmed their synthesis pathway as well as their assumed molecular structures. Furthermore, a conformational analysis was performed, and electronic parameters of molecules were characterized using theoretical calculations at AM1 and DFT level. Moreover, molecular docking revealed the mode of binding of the investigated 1,2,4-triazine sulfonamides with the human estrogen receptor alpha (ERα).

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 Hypercoordinated Organosilicon(IV) and Organotin(IV) Complexes: Syntheses, Spectral Studies, and Antimicrobial Activity In Vitro

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kiran Singh ◽  
Parvesh Puri ◽  
Yogender Kumar ◽  
Chetan Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Bases ◽  
Structural Features ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Spectral Studies ◽  
Nmr Studies ◽  
Trigonal Bipyramidal ◽  
Elemental Analyses

This paper deals with the syntheses and structural features of some new diorganosilicon(IV) and diorganotin(IV) complexes having general formulae (CH3)2MCl(L1), (CH3)2MCl(L2), (CH3)2M(L1)2, and (CH3)2M(L2)2 with new Schiff bases (M = Si and Sn). The Schiff bases HL1 and HL2 have been derived from the condensation of 3-bromobenzaldehyde with 4-amino-3-ethyl-5-mercapto-1,2,4-triazole and 4-amino-5-mercapto-3-propyl-1,2,4-triazole, respectively. The compounds have been characterized by the elemental analyses, molar conductance, and spectral (UV, IR, 1H, 13C, 29Si, and 119Sn NMR) studies. The resulting complexes have been proposed to have trigonal bipyramidal and octahedral geometries. In vitro antimicrobial activities of the compounds have been carried out.

Synthesis, characterization, DNA cleavage and in vitro antimicrobial activities of copper(II) complexes of Schiff bases containing a 2,4-disubstituted thiazole

2010 ◽  
Vol 35 (8) ◽  
pp. 917-925 ◽  
Author(s):  
Sanjay K. Bharti ◽  
Saurabh K. Patel ◽  
Gopal Nath ◽  
Ragini Tilak ◽  
Sushil K. Singh
Keyword(s):  
Schiff Bases ◽  
Dna Cleavage ◽  
Antimicrobial Activities

scholarly journals Biotinylated xanthohumol: synthesis and in vitro biological evaluation for anticancer therapy

2018 ◽  
Author(s):  
Monika Stompor ◽  
Rafał Podgórski ◽  
Marta Świtalska ◽  
Joanna Wietrzyk
Keyword(s):  
Breast Cancer ◽  
Antioxidant Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Biological Evaluation ◽  
Breast Cancer Cell Lines ◽  
Dpph Method ◽  
Ic50 Values ◽  
Mcf 7

Two biotinylated derivatives of the main hop chalcone xanthohumol (1) were prepared by a one-step synthesis via esterification using biotin and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC HCl) and 4-dimethylaminopyridine (DMAP) as coupling reagents. The products were characterized spectroscopically and their antiproliferative activity toward MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1 and Balb/3T3 cell lines was investigated using the SRB assay. For all three tested compounds the best activity was noted in the case of human (MCF-7) and mice (4T1) breast cancer cell lines (IC50 values < 9 μM). Both biotinylated derivatives showed higher anticancer activity than xanthohumol (1) towards all types of tested breast cancer cells. Double biotinylated xanthohumol (3) proved to be the most active in inhibiting cell growth, with IC50 values equal to 5.35 ± 1.5 μM for 4T1 and 8.03 ± 0.53 µM for MCF-7 cell lines. Compound 3 was also more active than 1 and 2 against liver cancer cells HepG2 (IC50 = 17.37 ± 5.1 μM), while the IC50 values for 1 and 2 were equal to 21.5 ± 2.7 and 22.1 ± 3.9 µM, respectively. 4‑O‑biotinylxanthohumol (2) was the second most active growth inhibitor, particularly with respect to MCF-7 (IC50 = 6.19 ± 1.7 μM) and 4T1 (IC50 = 6.64 ± 0.4 μM) cell lines. The antioxidant activity was evaluated using the 1.1-diphenyl-2-picrylhydrazyl radical (DPPH) method. All tested compounds (1-3) have antioxidant activity between 2.73 and 3.38 mM. It was reported for the first time that new prenylated chalcones containing the biotin moiety effectively inhibited proliferation of cancer cells in vitro.

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