Copper(II) mixed-ligand complexes containing 1, 10-phenanthroline, adenine and thymine: Synthesis, characterization and antibacterial activities

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Copper Complexes ◽  
Antimicrobial Agents ◽  
Conductivity Measurement ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
E Coli ◽  
In Vivo Cytotoxicity

New copper complexes, [Cu(phen)2(Thy)]2Cl and [Cu(phen)2(Ad)]2Cl (phen = 1,10-phenantroline, Ad (Adenine, a purine nucleobase) and Thy (Thymine, a pyrimidine nucleobase)), were synthesized and characterized by atomic absorption spectroscopy (AAS), conductivity measurement, UV-visible and infrared (IR) techniques. The complexes were tested for their antimicrobial activity against two gram positive and two gram negative bacterial strains. The results of in vitro antimicrobial activities were compared with the commercially available antimicrobial agents (ciprofloxacin and chloramphenicol). This comparative study has demonstrated that [Cu(phen)2(Thy)]2Cl inhibited the growth of methicillin resistant Staphylococcus aureous (MRSA), Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumonia) better than chloramphenicol by 11.25%, 19.41% and 25.35%, respectively. It also showed better activities than ciprofloxacine on MRSA and K. pneumoniae by 2.50% and 12.13%, respectively. Similarly, [Cu(phen)2(Ad)]2Cl demonstrated better inhibitions than chloramphenicol against MRSA, E. coli and K. pneumoniae by 11.24%, 2.48% and 9.06%, respectively. Therefore, after in vivo cytotoxicity investigations, these complexes could be considered as potential antimicrobial agents.

scholarly journals Synthesis of sulfonamides bearing 1,3,5-triarylpyrazoline and 4-thiazolidinone moieties as novel antimicrobial agents

2020 ◽  
Vol 85 (2) ◽  
pp. 155-162
Author(s):  
Thi-Dan Thach ◽  
Thi Le ◽  
Thien-Annguyen Nguyen ◽  
Chi-Hien Dang ◽  
Van-Su Dang ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Significant Inhibition ◽  
Mercaptoacetic Acid ◽  
Bacterial Strains ◽  
Reference Drug ◽  
E Coli ◽  
Yeast Strains ◽  
Microbial Strains

Two series of sulfonamides were synthesized from 4-hydrazinylbenzenesulfonamide as the key starting material. 1,3,5-Triarylpyrazoline sulfonamides (2a?i) were obtained by cyclocondensation of various chalcones in 53? ?64 % yields, while 4-thiazolidinone derivatives (4a?e) were synthesized by cyclocondensation between mercaptoacetic acid and different phenylhydrazones in 43?62 % yields. The synthesized compounds were characterized based on FTIR, 1H-NMR, 13C-NMR and HRMS data. The sulfonamides were evaluated for their in vitro antimicrobial activities against four bacterial strains (E. coli, P. aeruginosa, B. subtillis and S aureus), two filamentous fungal strains (A. niger and F. oxysporum) and two yeast strains (C. albicans and S. cerevisiae). Seven pyrazolines, 2a?c and 2e?h, exhibited significant inhibition of different microbial strains. Among them, compound 2b displayed good antifungal activity against A. niger (MIC value at 12.5 ?g mL-1) over the reference drug.

scholarly journals Synthesis and Assessment of Antibacterial Activities of Ruthenium(III) Mixed Ligand Complexes Containing 1,10-Phenanthroline and Guanide

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Atakilt Abebe ◽  
Tizazu Hailemariam
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activities ◽  
Drug Resistant ◽  
E Coli ◽  
Antibiotic Drugs ◽  
Wide Range ◽  
In Vivo Cytotoxicity ◽  
Better Than

In this work, two complexes of ruthenium(III) ([Ru(phen)2Cl2]Cl·2H2O and [Ru(phen)2(G)Cl]2Cl·H2O) were synthesized from 1,10-phenanthroline alone as well as from both 1,10-phenanthroline and guanide. The synthesis was checked using halide test, conductance measurement, and spectroscopic (ICP-OES, FTIR, and UV/Vis) analysis. Their in vitro antibacterial activities were also investigated on two Gram-positive (Staphylococcus aureus (S. aureus) and methicillin resistant Staphylococcus aureus (MRSA)) and two Gram-negative (Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumoniae)) bacteria. These complexes showed wide-range better activities than the commercially available controls (Chloramphenicol and Ciprofloxacin) against even the most drug resistant K. pneumoniae. [Ru(phen)2(G)Cl]2Cl·H2O inhibited S. aureus, MRSA, E. coli, and K. pneumoniae by 17.5%, 27.4%, 16%, and 52%, respectively, better than Chloramphenicol. It also inhibited these pathogens by 5.9%, 5.1%, 2.3%, and 17.2%, respectively, better than Ciprofloxacin. Similarly, [Ru(Phen)2(Cl)2]Cl·2H2O inhibited these pathogens by 11%, 8.7%, 0.1%, and 31.2%, respectively, better than Chloramphenicol. Therefore, after in vivo cytotoxicity investigations, these compounds can be considered as potential antibiotic drugs.

scholarly journals A PRELIMINARY OBSERVATION ON AN EXPLICIT ANTIMICROBIAL ACTION OF MANGROVE PLANTS ON PSEUDOMONAS AERUGINOSA

2019 ◽  
pp. 226-230
Author(s):  
TAMANNA SULTANA ◽  
ARUP KUMAR MITRA ◽  
SATADAL DAS
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antibacterial Activities ◽  
Microtiter Plate ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Mangrove Plant ◽  
E Coli ◽  
Mangrove Plants

Objectives: Due to emerging drug-resistant microorganisms throughout the world, newer antimicrobial agents should be looked for. Plants are enriched with different bioactive chemicals. In this study, we searched antibacterial activities of some mangrove plant extracts against Pseudomonas aeruginosa, Staphylococcus aureus, and Escherichia coli. Methods: In the present study, the antimicrobial activity of the leaves of Bruguiera gymnorhiza, Excoecaria agallocha, Avicennia alba, and Aegialitis rotundifolia was evaluated against a few reference pathogenic bacterial strains, namely, P. aeruginosa ATCC 27853, E. coli ATCC 25922, S. aureus ATCC 29213, and multidrug-resistant bacterial strains E. coli extended-spectrum beta-lactamases strain. Aqueous, ethanolic, methanolic, and dimethyl sulfoxide (DMSO) extracts were studied. The antimicrobial activities of the organic solvent extracts on the various test microorganisms were investigated using agar well diffusion technique followed by determination of minimum inhibitory concentration values by serial dilution in a microtiter plate. Results: Ethanol and DMSO extracts of B. gymnorhiza exhibited promising antimicrobial activity followed by extracts of A. alba and E. agallocha. Among all microorganisms studied, P. aeruginosa ATCC 27853 showed significant growth inhibition with ethanol and DMSO extracts. Conclusion: Extracts of some mangrove plants, particularly, B. gymnorhiza showed very good antimicrobial activities against common microbial agents causing human infections and in general mangrove plants appear to act better on P. aeruginosa.

scholarly journals The Disulfide Bond of the Peptide Thanatin Is Dispensible for Its Antimicrobial ActivityIn VivoandIn Vitro

2016 ◽  
Vol 60 (7) ◽  
pp. 4283-4289 ◽  
Author(s):  
Bo Ma ◽  
Chao Niu ◽  
Ying Zhou ◽  
Xiaoyan Xue ◽  
Jingru Meng ◽  
...  
Keyword(s):  
Disulfide Bond ◽  
Umbilical Vein ◽  
Low Cost ◽  
Survival Rates ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Content Type ◽  
E Coli

ABSTRACTThanatin (THA) displays potent antibiotic activity, especially against extended-spectrum-β-lactamase (ESBL)-producingEscherichia colibothin vitroandin vivo, with minimal hemolytic toxicity and satisfactory stability in plasma. However, the high cost of thanatin significantly limits its development and clinical application. To reduce the cost of peptide synthesis, a formulation of cyclic thanatin (C-thanatin) called linear thanatin (L-thanatin) was synthesized and its activity was evaluatedin vivoandin vitro. Results showed that C-thanatin and L-thanatin MICs did not differ against eight Gram-negative and two Gram-positive bacterial strains. Furthermore, the survival rates of ESBL-producing-E. coli-infected mice were consistent after C-thanatin or L-thanatin treatment at 5 or 10 mg/kg of body weight. Neither C-thanatin nor L-thanatin showed toxicity for human red blood cells (hRBCs) and human umbilical vein endothelial cells (HUVECs) at a concentration as high as 256 μg/ml. Results of circular dichroism spectroscopy indicated that the secondary structure of L-thanatin is extremely similar to that of C-thanatin. Membrane permeabilization and depolarization assays showed that C-thanatin and L-thanatin have similar abilities to permeabilize the outer and inner membranes and to induce membrane depolarization in ESBL-producingE. coli. However, neither of them caused significant HUVEC membrane permeability. These findings indicate that the two peptides have similar effects on bacterial cell membranes and that the disulfide bond in thanatin is not essential for its antimicrobial activitiesin vivoandin vitro. L-thanatin is thus a promising low-cost peptide candidate for treating ESBL-producingE. coliinfections.

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

scholarly journals DPPH-Scavenging and Antimicrobial Activities of Asteraceae Medicinal Plants on Uropathogenic Bacteria

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Phan-Canh Trinh ◽  
Le-Thi-Thanh Thao ◽  
Hoang-Tran-Viet Ha ◽  
TuAnh Nguyen
Keyword(s):  
Antimicrobial Agents ◽  
Natural Antioxidants ◽  
Ethyl Acetate Fraction ◽  
Antimicrobial Activities ◽  
Chrysanthemum Morifolium ◽  
Bacterial Strains ◽  
Ageratum Conyzoides ◽  
Potent Effect ◽  
E Coli ◽  
Dpph Scavenging

Asteraceae species were widely applied in traditional medicines in Asian countries as sources of natural antioxidants and antimicrobial agents. This study aimed to evaluate DPPH-scavenging capacities and antimicrobial activities of nine Asteraceae species collected from Southern Vietnam. Antioxidant and antimicrobial activities were determined by standard protocols. Essential oils from Ageratum conyzoides, Helianthus annuus, and Artemisia vulgaris indicated significant inhibitory effects on Staphylococcus aureus and Candida spp. Crude extracts and fractions from Taraxacum officinale, Chrysanthemum morifolium, A. conyzoides, and Tagetes erecta showed inhibitory ability on at least one testing bacterial strains including S. aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. In a study on clinical isolates, ethyl acetate fraction from A. conyzoides flower displayed the most potent effect on uropathogenic E. coli and K. pneumoniae with MIC at 1.25–10 mg/ml and 5–12.5 mg/ml, respectively. DPPH-scavenging assay indicated that T. erecta extract had the lowest IC50 (17.280 μg/ml) and is 2.4 times higher than vitamin C (7.321 μg/ml). This study revealed that A. conyzoides has good potential against uropathogenic E. coli and K. pneumoniae, and therefore could be applied for prophylactic treatment of urinary infection.

scholarly journals Preventive antimicrobial action and tissue architecture ameliorations of Bacillus subtilis in challenged broilers

2021 ◽  
Vol 14 (2) ◽  
pp. 523-536
Author(s):  
Essam S. Soliman ◽  
Rania T. Hamad ◽  
Mona S. Abdallah
Keyword(s):  
Bacillus Subtilis ◽  
Broiler Chickens ◽  
Trichophyton Mentagrophytes ◽  
Antimicrobial Activities ◽  
Lymphoid Hyperplasia ◽  
Bursa Of Fabricius ◽  
Tissue Architecture ◽  
E Coli

Background and Aim: Probiotics improve intestinal balance through bacterial antagonism and competitive exclusion. This study aimed to investigate the in vitro antimicrobial activity, as well as the in vivo preventive, immunological, productive, and histopathological modifications produced by probiotic Bacillus subtilis. Materials and Methods: The in vitro antimicrobial activities of B. subtilis (5×106 CFU/g; 0.5, 1.0*, 1.5, and 2.0 g/L) were tested against Escherichia coli O157: H7, Salmonella Typhimurium, Candida albicans, and Trichophyton mentagrophytes after exposure times of 0.25, 0.5, 1, and 2 h using minimal inhibitory concentration procedures. A total of 320 1-day-old female Ross broiler chickens were divided into five groups. Four out of the five groups were supplemented with 0.5, 1.0*, 1.5, and 2.0 g/L probiotic B. subtilis from the age of 1 day old. Supplemented 14-day-old broiler chickens were challenged with only E. coli O157: H7 (4.5×1012 CFU/mL) and S. Typhimurium (1.2×107 CFU/mL). A total of 2461 samples (256 microbial-probiotic mixtures, 315 sera, 315 duodenal swabs, and 1575 organs) were collected. Results: The in vitro results revealed highly significant (p<0.001) killing rates at all-time points in 2.0 g/L B. subtilis: 99.9%, 90.0%, 95.6%, and 98.8% against E. coli, S. Typhimurium, C. albicans, and T. mentagrophytes, respectively. Broilers supplemented with 1.5 and 2.0 g/L B. subtilis revealed highly significant increases (p<0.01) in body weights, weight gains, carcass weights, edible organs' weights, immune organs' weights, biochemical profile, and immunoglobulin concentrations, as well as highly significant declines (p<0.01) in total bacterial, Enterobacteriaceae, and Salmonella counts. Histopathological photomicrographs revealed pronounced improvements and near-normal pictures of the livers and hearts of broilers with lymphoid hyperplasia in the bursa of Fabricius, thymus, and spleen after supplementation with 2.0 g/L B. subtilis. Conclusion: The studies revealed that 1.5-2.0 g of probiotic B. subtilis at a concentration of 5×106 CFU/g/L water was able to improve performance, enhance immunity, and tissue architecture, and produce direct antimicrobial actions.

scholarly journals Antibacterial activities of Camellia sinensis plant extracts against uropathogenic E. coli in vitro and in vivo

2020 ◽  
Vol 14 (6) ◽  
pp. 147-155
Author(s):  
J. N. Agbom ◽  
O. Ogbu ◽  
I. R. Iroha ◽  
I. B. Moses ◽  
A. L. Onuora ◽  
...  
Keyword(s):  
Camellia Sinensis ◽  
Plant Extracts ◽  
Antibacterial Activities ◽  
E Coli

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 1-((DIMETHYLAMINO)METHYL)-3-(4-(3-(SUBSTITUTE DPHENYL)-4-OXOTHIAZOLIDIN-2-YL)PHENYLIMINO)-5-NITROINDOLIN-2-ONES AS POTENT ANTITUBERCULAR AGENTS

2019 ◽  
pp. 200-207
Author(s):  
KOSARAJU LAHARI ◽  
RAJA SUNDARARAJAN
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Proton Nuclear Magnetic Resonance ◽  
Design And Synthesis ◽  
Group Variation

Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

scholarly journals In Vitro and In Vivo Antibacterial Activities of SM-216601, a New Broad-Spectrum Parenteral Carbapenem

2005 ◽  
Vol 49 (10) ◽  
pp. 4185-4196 ◽  
Author(s):  
Yutaka Ueda ◽  
Katsunori Kanazawa ◽  
Ken Eguchi ◽  
Koji Takemoto ◽  
Yoshiro Eriguchi ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Antibacterial Activities ◽  
Multiresistant Pathogens ◽  
E Coli ◽  
Wide Range ◽  
Agar Dilution ◽  
Resistant Strains ◽  
Mrsa Strains

ABSTRACT SM-216601 is a novel parenteral 1β-methylcarbapenem. In agar dilution susceptibility testing, the MIC of SM-216601 for 90% of the methicillin-resistant Staphylococcus aureus (MRSA) strains tested (MIC90) was 2 μg/ml, which was comparable to those of vancomycin and linezolid. SM-216601 was also very potent against Enterococcus faecium, including vancomycin-resistant strains (MIC90 = 8 μg/ml). SM-216601 exhibited potent activity against penicillin-resistant Streptococcus pneumoniae, ampicillin-resistant Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis, with MIC90s of less than 0.5 μg/ml, and intermediate activity against Citrobacter freundii, Enterobacter cloacae, Serratia marcescens, and Pseudomonas aeruginosa. The therapeutic efficacy of SM-216601 against experimentally induced infections in mice caused by S. aureus, E. faecium, E. coli, and P. aeruginosa reflected its in vitro activity and plasma level. Thus, SM-216601 is a promising candidate for nosocomial bacterial infections caused by a wide range of gram-positive and gram-negative bacteria, including multiresistant pathogens.

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