Microwave Assisted Synthesis of Some Novel 2-(3-Chlorobenzyl)-1H-Benzimidazole Derivatives and Determination of Their Antimicrobial Activity and pKa Values

WOS: 000350270800006In the present research, synthesis of new 2-(3-chlorobenzyl)-1H-benzimidazole derivatives bearing N-benzylidene, 1,2,4-triazole and N-acylhydrazone moiety is investigated. These novel compounds have been tested for their antimicrobial effects against two of Gram-positive bacterial strains, namely Bacillus subtilis and Staphylococcus epidermidis, and four Gram-negative bacterial strains which were Enterobactercloaceae, Klebsiellapneumonie, Proteus vulgaris, and Salmonella typhymirium. According to their MIC values, which reflect their activity on the bacteria, were classified in three grops: best, good and moderate. So, the best MIC values were obtained 6a and 66. on the other hand, the acidity values of pKa for 6a-d derivatives were calculated with MOPAC 2012 computer program using physico-chemical semi-empirical methods (AM1, MNDO, MNDOD, PM3, PM6, PM6-DH2, PMT and RM1) in water, ethyl alcohol, methyl alcohol, n-propyl alcohol, isopropyl akcohol, n-butyl alcohol, tert-butyl alcohol, ethylene glycol, N,N-dimethyl formamide, N,N-dimetyl sulfoxide and acetonitrile at 25 degrees C

Synthesis of Some New Ciprofloxacin Hybrids as Potential Antimicrobial Agents

WOS: 000422654000003A new series of ciprofloxacin hybrid compounds as new type of antimicrobial agents were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria

STUDY OF ANTIOXIDANT, ANTIMICROBIAL AND ANTI-XANTHINE OXIDASE ACTIVITIES OF SOME 5,6-DIMETHYL-2-(SUBSTITUTED)-1H-BENZIMIDAZOLES AND THEIR ACYLHYDRAZIDE DERIVATIVES

WOS: 000396612400004In this study, a series of 5,6-dimethy1-2-(4-fluoro/chloro/bromo/methyl/nitrobenzy1)-1Hbenzimidazoles were screened for their bovine milk xanthine oxidase (XO) inhibition, antioxidant and antimicrobial activities. Compounds 2d and 2f showed XO inhibition at various concentrations. in addition, compounds 4a, 4b, 4c, 4d, 4e and 4f exhibited highly antioxidant activity by CUPric Reducing Antioxidant Capacity (CUPRAC) method and efficient radical scavenging activity in ABTS (2,2-azinobis(3- ethylbenzothiazoline-6sulfonic acid)/Persulfate and DPPH (1,1- diphenyl-2-picrylhydrazyl) assays. Also, the synthesized compounds have been tested for their antimicrobial effects against Bacillus cereus 702 Roma, Bacillus megaterium DSM-32, Bacillus subtilis C41015, Escherichia coli ATCC 35218, Enterococcus cloaceae, Pseudomonas aeruginosa ATCC 43088, Staphylococcus aureus ATCC 25923, Yersinia pseudota ATCC911.Recep Tayyip Erdogan University Scientific Research Project Unit (BAP)Recep Tayyip Erdogan University [2014.102.02.05]; Recep Tayyip Erdogan UniversityRecep Tayyip Erdogan UniversityThis work was supported by Recep Tayyip Erdogan University Scientific Research Project Unit (BAP) under project number: 2014.102.02.05. Authors thanks to Recep Tayyip Erdogan University for this support

Synthesis of novel 2,3-disubstituted quinazolin-4(3H)-one derivatives containing hydrazone skeleton as potent urease inhibitors and their antimicrobial activities

WOS: 000485942500001A new series of quinazolinones containing hydrazone moiety were synthesized, and their inhibitory activities on urease were assessed in vitro. Most of the compounds exhibited potent urease inhibitory activity. Among the synthesized compounds, molecule 4a bearing furan ring has the best inhibitory effect against urease with IC50 = 2.90 +/- 0.11 mu g/mL. Compounds 4f, 4g, 4h, 4i, and 4j have hydroxy group on phenyl ring. Compound 4i is the most active inhibitor among these compounds with IC50 = 5.01 +/- 0.10 mu g/mL, which has 3-Cl and 4-Br on phenyl ring. Also, newly synthesized compounds had been tested for their antimicrobial effects against three of Gram-positive bacteria (Bacillus cereus 702 Roma, Staphylococcus aureus ATCC 25923, and Streptococcus pyogenes ATCC 19615) and three of Gram-negative bacteria (Escherichia coli ATCC 25922, Proteus vulgaris ATCC 13315, and Pseudomonas aeruginosa ATCC 27853). Antimicrobial activity results show that compounds 4a, 4h, 4j, 4f, and 4l have the lowest minimum inhibitory concentration (MIC) value of 1000 mu g/mL to all tested bacteria. the other compounds have the MIC value of >1000 mu g/mL to all tested bacteria

Synthesis, Antibacterial and Antioxidant Activities of Some New Nsubstituted Azachalcone, Schiff base and Pyrazole Derivatives

WOS: 000561219600010Pyrazoles, Schiff bases and the quaternary ammonium compounds (QAC) such as N-alkyl substituted azachalcones are the important group of chemical individuals with widespread usage in many fields of science. in particular, these compounds have proven biological activities. in addition, the emergence of resistance against antibiotics used is the cause of an increasing necessity of new effective substances. Therefore, new N-alkyl substituted derivatives (4-7), 1,3,5-trisubstituted-2-pyrazoles (8-10) and Schiff bases (11-13) with biological activities such as phenolic. antioxidants or QAC were synthesized, starting from azachalcones. the structures of the compounds were elucidated with spectral methods including IR, 1H-NMR, 13C-NMR, COSY spectral data and elemental analyses. the prepared compounds were evaluated for antibacterial activity against four Gram-positive bacteria, and four Gram-negative bacteria. the minimum inhibitory concentration (MIC) of the N-alkylated azachalcone derivatives 5 and 7 (7.8 mg/mL) showed strong antimicrobial activities, especially against Bacillus cereus. Antioxidant capacities of the synthesized compounds were determined by using CU-PRAC and FRAP methods. As a result, compound 9 was observed to be more effective than other compounds

SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW TRIAZOLE BRIDGED BENZIMIDAZOLE SUBSTITUTED PHTHALONITRILE AND PHTHALOCYANINES

Sasmaz, Selami/0000-0001-5311-7550WOS: 000439133900008In this study, some new phthalonitriles and metallophthalocyanines (Zn, Ni, Co, and Cu) containing triazole bridged benzimidazole moieties were synthesized starting from 2-(3-methylbenzyl)-1H-benzimidazole Newly synthesized compounds have been tested for their antimicrobial effects against four Gram positively (Bacillus cereus 702 Roma, B. megaterium DSM-32, B. subtilis ATCC 6633, and Staphylococcus aureus ATCC 25923) and four Gram negatively (Escherichia coli ATCC 25922, Enterobacter cloaceae ATCC 13047, Pseudomonas aeruginosa ATCC 27853, and Yersinia pseudotuberculosis ATCC 911) bacteria. According to results, compounds 6, 7b, 7c, and 8a have the best activity with MIC values of 31.25 mu g/mL to B. subtilis. the second best activity belongs to compounds 4, 5, 7, 8, 7a, 8c, and 8d with the MIC value of 62.5 mu g/mL on the same bacterium. Zinc (II) phthalocyanines have better antimicrobial activity than other metallophthalocyanines against Gram (+) bacteria

Synthesis of Novel Pyrazolines, Their Boron-Fluorine Complexes, and Investigation of Antibacterial, Antioxidant, and Enzyme Inhibition Activities

WOS: 000397305600003PubMed: 280326643,5-disubstituted-2-pyrazoline derivatives (4-6), their boron-fluorine complexes (boron (3-(2'-aminophenyl), 5-(2'-/3'-/4'-pyridyl) pyrazoline, BOAPPY) (7-9) and boron 1,2'-diazaflavone complex (BODAF) (11) were synthesized starting from azachalcones (1-3) to diazaflavone (10), respectively. Biological evaluation of compounds 4-9 and 11 showed remarkable antioxidant, antibacterial, and acetylcholinesterase and tyrosinase enzyme inhibition activities. All newly synthesized compounds 4-9 and 11 showed respectable antibacterial effect with minimum inhibitory concentrations in the range of 4.7-150mg/mL.Karadeniz Technical UniversityKaradeniz Technical University; Scientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TUBITAK-113T041]This study was supported by grants from Karadeniz Technical University and the Scientific and Technological Research Council of Turkey (TUBITAK-113T041)

Synthesis, antibacterial and antioxidant activities of new 1-alkyl-4-(1-alkyl-4-oxo-1,4-dihydroquinolin-2-yl)pyridinium bromides

AKAR, ZEYNEP/0000-0001-9262-8070WOS: 000330603900033PubMed: 24077525New 1-alkyl-4-(1-alkyl-4-oxo-1,4-dihydroquinolin-2-yl)pyridinium bromides (3a k) were synthesized from 1,4'-diazaflavone [2-pyridin-4-ylquinolin-4(1H)-one] and evaluated for antibacterial and antioxidant activities. A rapid one-pot preparation of 1,4'-diazaflavone (2) was done from 2'-amino substituted chalcone (1) by intramolecular Michael addition using solvent-free microwave heating. New N,N'-dialkyl substituted (C-5-C-15) 1,4'-diazaflavonium bromides were synthesized from compound 2 with corresponding alkyl halides. Compounds 3a k were active against six bacteria (MIC: 7.8-500.0 mu g/mL). They also showed good antioxidant activities in DPPI-1* scavenging (SC50: 45-133 mu g/mL) and ferric reducing/antioxidant power (14-141 p.M TEAC) tests. the biological activities decreased as alkyl chain length increased. the reason behind the obvious negative effect of alkyl chain elongation is unclear and requires investigations about the intermolecular interactions of these pyridinium salts with bioassay components. (C) 2013 Elsevier Masson SAS. All rights reserved.Karadeniz Technical UniversityKaradeniz Technical University; Scientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TUBiTAK-109T388]This study was supported by grants from Karadeniz Technical University and the Scientific and Technological Research Council of Turkey (TUBiTAK-109T388)

Synthesis, aggregation and spectroscopic studies of novel water soluble metal free, zinc, copper and magnesium phthalocyanines and investigation of their anti-bacterial properties

AKCAY, Hakki Turker/0000-0002-8502-9608;WOS: 000340330900038PubMed: 24952089In this study, novel phthalonitrile derivative (3) was synthesized by the reaction between 4-nitrophthalonitrile (2) and a triazole derivative (1) containing pyridine moiety. Crystal structure of compound (3) was characterized by X-ray diffraction. New metal free and metallo-phthalocyanine complexes (Zn, Cu, and Mg) were synthesized using the phthalonitrile derivative (3). Cationic derivatives of these phthalocyanines (5, 7, 9, and 11) were prepared from the non-ionic phthalocyanines (4, 6, 8, and 10). All proposed structures were supported by instrumental methods. the aggregation behaviors of the phthalocyanines (4-11) were investigated in different solvents such as dimethylsulfoxide (DMSO), N,N-dimethylformamide (DMF), chloroform and water. Water soluble cationic Pcs (5, 7, 9, and 11) aggregated in water and sodium dodecyl sulfate was used to prevent the aggregation. the second derivatives of the UV-Vis spectra of aggregated Pcs were used for analyzing the Q and B bands of aggregated species. Thermal behaviors of the phthalocyanines were also studied. in addition, anti-bacterial properties of the phthalocyanines were investigated. We used four gram negative and two gram positive bacteria to determine antibacterial activity of these compounds. Compound 7 has the best activity against the all bacteria with 125 mu g/mL of MIC value. Compounds 4, 6, and 10 have the similar effect on the bacteria with 250 mu g/mL of MIC value. (C) 2014 Elsevier B.V. All rights reserved

Biosorption of Heavy Metals by Anoxybacillus gonensis Immobilized on Diaion HP-2MG

Soylak, Mustafa/0000-0002-1017-0244; BELDUZ, Ali Osman/0000-0003-2240-7568WOS: 000262643400005The determination of trace metal ions usually requires previous separation and preconcentration stages in order to cope with low levels and to remove the interfering components. Nowadays emphasis is given to the utilization of microorganisms because of their great ability to absorb metal ions from aqueous solution. In this paper, for this, Zn2+, Fe3+, Cu2+, Cd2+, Ni2+, Co2+, and Pb2+ ions at trace levels have been separated and preconcentrated on a column containing a bacterium, Anoxybacillus gonensis immobilized on Diaion HP-2MG as a new biosorption system prior to their atomic absorption spectrometric determinations. The effects of some analytical parameters were investigated. Optimum pH values were found to be 6 for Zn, Fe, Cu and Pb, 8 for Cd, Ni, and Co. Recoveries of Zn2+, Fe3+, Cu2+, Cd2+, Ni2+, Co2+, and Pb2+ were 953, 986, 962, 982, 972, 954 and 953 at 95% confidence level, respectively. No significant matrix interferences on the quantitative recoveries of the analyte ions were observed. Preconcentration factors of the anlayte ions were calculated as 50 for Zn, Cd and Pb, and 75 for Fe, Cu, Ni, and Co. The limits of detection for the analyte ions were in the range 0.2-1.3 g L-1. The procedure was validated by spike addition and analysis of standard reference materials