scholarly journals Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity

2020 ◽  
Vol 10 (03) ◽  
pp. 408-413
Author(s):  
Shaker M. Alwan ◽  
Shayma L. Abdulhadi ◽  
Amera Abbas
Keyword(s):  
Antimicrobial Activity ◽  
Pyridine Ring ◽  
Copper Complexes ◽  
Dna Gyrase ◽  
Acid Group ◽  
Dna Bases ◽  
Carboxyl Group ◽  
Carboxylic Acid Group ◽  
Ft Ir ◽  
Bactericidal Agent

Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory results compared with levofloxacin. This has indicated that the presence of the carbonyl of C-3 carboxyl moiety is not essential, as levofloxacin carboxamides showed interesting copper complexes indicating that they retain the activity of levofloxacin, since its activity depends on binding to DNA gyrase via magnesium binding.

The inner salt 4-carboxy-2-(pyridinium-4-yl)-1H-imidazole-5-carboxylate monohydrate

2006 ◽  
Vol 62 (7) ◽  
pp. o2751-o2752 ◽  
Author(s):  
Ting Sun ◽  
Jian-Ping Ma ◽  
Ru-Qi Huang ◽  
Yu-Bin Dong
Keyword(s):  
Carboxylic Acid ◽  
Dihedral Angle ◽  
Title Compound ◽  
Acid Group ◽  
Planar Structure ◽  
Carboxyl Group ◽  
Carboxylic Acid Group ◽  
Pyridyl Group ◽  
Compound C

In the title compound, C10H7N3O4·H2O, one carboxyl group is deprotonated and the pyridyl group is protonated. The inner salt molecule has a planar structure, apart from the carboxylic acid group, which is tilted from the imidazole plane by a small dihedral angle of 7.3 (3)°.

scholarly journals Synthesis of bis-azobenzene derivatives with reactive bromohexyl unit and carboxylic acid group based on Disperse Yellow 7

2020 ◽  
Vol 11 (4) ◽  
pp. 298-303
Author(s):  
Alina Madalina Darabut ◽  
Olha Hennadiivna Purikova ◽  
Yevheniia Volodymyrivna Lobko
Keyword(s):  
Carboxylic Acid ◽  
Molecular Electronics ◽  
Azo Dye ◽  
Analytical Techniques ◽  
Acid Group ◽  
Carboxylic Acid Group ◽  
Acid Moiety ◽  
Ft Ir ◽  
Hydrolysis Of ◽  
Azobenzene Derivatives

In this work, two types of azobenzene derivatives based on Disperse Yellow 7 (DY7, 4-[4-(phenylazo)phenylazo]-o-cresol) were synthesized, which are bis-azobenzenes bearing flexible functional 6-bromohexyl chain or carboxylic acid moiety. The first one was synthesized by alkylation of DY7 with an excess of 1,6-dibromohexane in the presence of a mild base (K2CO3). The second one (azo dye with carboxylic acid functionality) was obtained by the alkaline hydrolysis of the ester bond of the newly obtained DY7 derivative with the ethoxycarbonyl group. The synthesized compounds were characterized by different spectral analytical techniques such as 1H NMR, 13C NMR, FT-IR, and UV-Vis. They can be employed for the synthesis of a wide variety of azo-based materials, which may be suitable for photochromic systems and molecular electronics applications.

scholarly journals Crystal structure of 4-aminobenzoic acid–4-methylpyridine (1/1)

2015 ◽  
Vol 71 (2) ◽  
pp. o125-o126 ◽  
Author(s):  
M. Krishna Kumar ◽  
P. Pandi ◽  
S. Sudhahar ◽  
G. Chakkaravarthi ◽  
R. Mohan Kumar
Keyword(s):  
Crystal Structure ◽  
Hydrogen Bond ◽  
Carboxylic Acid ◽  
Hydrogen Bonds ◽  
Pyridine Ring ◽  
Acid Group ◽  
Aminobenzoic Acid ◽  
Carboxylic Acid Group ◽  
Title 1 ◽  
Bond Forming

In the title 1:1 adduct, C6H7N·C7H7NO2, the carboxylic acid group is twisted at an angle of 4.32 (18)° with respect to the attached benzene ring. In the crystal, the carboxylic acid group is linked to the pyridine ring by an O—H...N hydrogen bond, forming a dimer. The dimers are linked by N—H...O hydrogen bonds, generating (010) sheets.

scholarly journals Synthesis, Crystal Structure, and Hirshfeld Surface Analysis of Ciprofloxacin-Salicylic Acid Molecular Salt

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Ravikumar Nagalapalli ◽  
Shankar Yaga Bheem
Keyword(s):  
Salicylic Acid ◽  
Acid Group ◽  
X Ray Diffraction ◽  
Carboxylic Acid Group ◽  
X Ray ◽  
Hydrogen Bonding Interactions ◽  
Hirshfeld Surfaces ◽  
Ft Ir ◽  
Molecular Salt ◽  
Ft Ir Spectroscopy

In the present study, ciprofloxacin-salicylic acid molecular salt has been synthesized and preliminarily characterized by FT-IR spectroscopy. The single crystal X-ray diffraction (SCXRD) reveals the proton transfer from carboxylic acid group of salicylic acid to piperazine moiety in ciprofloxacin confirming the formation of new molecular salt. The molecular packing of the molecular salt is mainly supported by N+–H⋯O−, O–H⋯O, C–H⋯F, C–H⋯π, and π-π interactions. The 3D Hirshfeld surfaces and the associated 2D fingerprint plots were investigated for intermolecular hydrogen bonding interactions.

Complexes of Cu (II) with a-Ketoglutaric Acid and 1- (o-tolyl) Biguanide Synthesis, characterization and biological Activity

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Copper Complexes ◽  
Substrate Adhesion ◽  
Inert Substrate

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.

Synthesis, SAR, In-Silico appraisal and Anti-Microbial Study of substituted 2-aminobenzothiazoles derivatives

2019 ◽  
Vol 15 ◽  
Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari
Keyword(s):  
Antimicrobial Activity ◽  
In Silico ◽  
Docking Study ◽  
Moderate Activity ◽  
Molecular Docking Study ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
In Silico Molecular Docking

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.

scholarly journals Exonuclease VII repairs quinolone-induced damage by resolving DNA gyrase cleavage complexes

2021 ◽  
Vol 7 (10) ◽  
pp. eabe0384
Author(s):  
Shar-yin N. Huang ◽  
Stephanie A. Michaels ◽  
Brianna B. Mitchell ◽  
Nadim Majdalani ◽  
Arnaud Vanden Broeck ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Biology ◽  
Excision Repair ◽  
Dna Gyrase ◽  
Nuclease Activity ◽  
Bacterial Strains ◽  
Functional Importance ◽  
Quinolone Antibiotics ◽  
Repair Pathways ◽  
Exonuclease Vii

The widely used quinolone antibiotics act by trapping prokaryotic type IIA topoisomerases, resulting in irreversible topoisomerase cleavage complexes (TOPcc). Whereas the excision repair pathways of TOPcc in eukaryotes have been extensively studied, it is not known whether equivalent repair pathways for prokaryotic TOPcc exist. By combining genetic, biochemical, and molecular biology approaches, we demonstrate that exonuclease VII (ExoVII) excises quinolone-induced trapped DNA gyrase, an essential prokaryotic type IIA topoisomerase. We show that ExoVII repairs trapped type IIA TOPcc and that ExoVII displays tyrosyl nuclease activity for the tyrosyl-DNA linkage on the 5′-DNA overhangs corresponding to trapped type IIA TOPcc. ExoVII-deficient bacteria fail to remove trapped DNA gyrase, consistent with their hypersensitivity to quinolones. We also identify an ExoVII inhibitor that synergizes with the antimicrobial activity of quinolones, including in quinolone-resistant bacterial strains, further demonstrating the functional importance of ExoVII for the repair of type IIA TOPcc.

scholarly journals Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 162
Author(s):  
Ahmed Ragab ◽  
Sawsan A. Fouad ◽  
Ola A. Abu Ali ◽  
Entsar M. Ahmed ◽  
Abeer M. Ali ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Growth ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Dhfr Inhibitors ◽  
Positive Controls

Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.

scholarly journals Biofoam of Spittlebug, Poophilus costalis (Walker): Preferential Sites, Temperature Regulation, Chemical Composition and Antimicrobial Activity

Insects ◽  
2021 ◽  
Vol 12 (4) ◽  
pp. 340
Author(s):  
Kitherian Sahayaraj ◽  
Balakrishnan Saranya ◽  
Samy Sayed ◽  
Loko Yêyinou Laura Estelle ◽  
Koilraj Madasamy
Keyword(s):  
Antimicrobial Activity ◽  
Chemical Composition ◽  
High Performance ◽  
Host Plants ◽  
Ground Level ◽  
College Campus ◽  
The Other ◽  
Mimosa Pudica ◽  
Ft Ir ◽  
Gas Chromatography Mass Spectroscopy

The foam produced by nymphs of Poophilus costalis on eleven different host plants belonging to eight families on St. Xavier’s College campus in India was studied over five months. The chemical composition and antimicrobial activity of these biofoams were investigated. The results revealed that P. costalis preferred Theporsia purpurea and Mimosa pudica for laying their eggs and producing foam, over the other tested plants. P. costalis produce their foam on either nodes or internodes on monocotyledons (30%) (p < 0.05), whereas on dicotyledons, they produce more foam on the stems (63.8%) than on the leaves (6.2%) (p < 0.01). The number of nymphs in each piece of foam from P. costalis varied from 1 to 3 (mean = 1.8 per plant). They produced their foam (5.7 to 45.2 cm) from the ground level on a plant. The length and breadth of a piece of foam ranged from 1.0 to 3.9 cm and 0.6 to 4.7 cm, respectively. The foam tended to be cooler than the environment. Qualitative profiling showed that the foam consists of carbohydrates, including maltose; trypsin; amino acids; protease. The foam was also analyzed using a spectrophotometer, Fourier transform infrared spectroscopy (FT-IR), gas chromatography–mass spectroscopy (GC-MS), and high-performance liquid chromatography (HPLC). The antimicrobial activity of the biofoam was the greatest against Staphylococcus aureus, the growth of which was reduced by 55.9 ± 3.9%, suggesting that the foam could be used as an antimicrobial product. However, no activities were observed against Fusarium oxysporum and Candida albicans.

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