scholarly journals Synthesis, Evaluation and Characterization of Some 1,3,4-Triazole-2-one Derivatives as Antimicrobial Agents

2012 ◽  
Vol 9 (4) ◽  
pp. 2407-2414 ◽  
Author(s):  
Mahabaleshwaraiah Neelgundmath ◽  
Oblennavar Kotresh

A series of novel compounds like 3[(phenyl substituted)-5-methyl-1(Benzosulphonylamine)]-1,3,4-triazole-2-ones II(a-f) were synthesized by treating 4-amino-1-phenyl-3-methyl-5-oxo-1,2,4-triazoles with benzene sulphonyl chloride using pyridine as solvent. Similarly by using 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles and acetic anhydride as starting material 3[(phenyl substituted)-5-methyl-1(acetylamino)]-1,3,4-triazole-2-ones III(a-f) were synthesized and also 3[(phenyl substituted)-5-methyl-1(chloroacetyl)]-1,3,4-triazole-2-ones I(a-f) were synthesized by treating 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles with chloroacetyl chloride in presence of a non-polar solvent like benzene. Elemental analysis, GCMS, IR, and1H NMR confirmed the structures of the newly synthesised compounds. The newly synthesized compounds are also screened for their antibacterial, antifungal and anti-inflammatory activities.

2002 ◽  
Vol 06 (02) ◽  
pp. 114-121 ◽  
Author(s):  
L. A. Tomachynski ◽  
V. Ya. Chernii ◽  
S. V. Volkov

The reaction of PcMCl 2 ( M = Zr , Hf ) with β-diketones is reported. 1 H NMR and elemental analysis suggest the substitution of two Cl atoms for two β-diketone fragments takes place as a result of this reaction and the complexes PcM(β-dik)2 are formed. All obtained complexes are stable and highly soluble in most organic solvents. The data from 1 H and 19 F NMR, and UV-vis spectroscopy suggest the coordination of two β-diketone ligands in a cis geometry about the central atom of the macrocycle. It was shown bis(β-diketonato)zirconium(IV) and hafnium(IV) phthalocyanines containing β-diketones with donor or acceptor groups or with bulky substituents can be obtained.


Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>


1997 ◽  
Vol 41 (11) ◽  
pp. 2389-2393 ◽  
Author(s):  
Y Kashida ◽  
M Kato

Fluoroquinolone antibacterial agents have been reported to induce tendon lesions in juvenile rats. In the present study, we characterized fluoroquinolone-induced Achilles tendon lesions by comparing the effects of 10 fluoroquinolones and examining the potential of one of these antimicrobial agents, pefloxacin, to induce tendon lesions when coadministered with one of nine anti-inflammatory compounds. Among the 10 fluoroquinolones tested, fleroxacin and pefloxacin were the most toxic, inducing lesions at a dose of 100 mg/kg of body weight or more, while lomefloxacin, levofloxacin, and ofloxacin or sparfloxacin and enoxacin induced lesions at 300 mg/kg or more and 900 mg/kg, respectively. In contrast, norfloxacin, ciprofloxacin, and tosufloxacin had no effect even at the high dose of 900 mg/kg. The severity of the Achilles tendon lesions appeared to correlate with the structure of the substituent at the seventh position. Furthermore, pefloxacin-induced tendon lesions were inhibited by coadministration with dexamethasone and N-nitro-L-arginine methyl ester. Phenidone (1-phenyl-3-pyrazolidinone) and 2-(12-hydroxydodeca-5,10-diynyl)3,5,6-trimethyl-1,4-benzoqui none (AA861) also decreased the incidence of tendon lesions. In contrast, catalase, dimethyl sulfoxide, indomethacin, pyrilamine, and cimetidine did not modify these tendon lesions. These results suggest that nitric oxide and 5-lipoxigenase products partly mediate fluoroquinolone-induced tendon lesions.


1980 ◽  
Vol 35 (7) ◽  
pp. 802-807 ◽  
Author(s):  
Michael Kopp ◽  
Luise R. Krauth ◽  
Richard Ratka ◽  
Klaus Weidenhammer ◽  
Manfred L. Ziegler

The reaction of cis-(C6H5CN)2PtCl2 and Na2PtCl4 with the dienes 1,4-pentadiene and 2,5-diphenyl-1,5-hexadiene yields the species cis-(1,4-pentadiene) PtCl2 and cis-(2,5-diphenyl-1,5-hexadiene)PtCl2, respectively. The compounds have been fully characterized by elemental analysis, IR, 1H-NMR, mass spectroscopy and by X-ray methods


2018 ◽  
Vol 2018 ◽  
pp. 1-8
Author(s):  
Fangfang Cheng ◽  
Bingbing Wang ◽  
Yanzhi Xia

A novel amphipathic chitosan derivative, O-acetyl-chitosan acetic ester (ACHA), was synthesized by the reaction of chitosan with acetic acid in the presence of thionyl chloride. The physicochemical properties of ACHA were characterized by FTIR, 1H NMR, TGA, and XRD. The yield (Y) of ACHA was 79.4%, and the degree of acetylation (DA) of ACHA was 1.04. Compared to CS, ACHA could be dissolved in many organic solvents, deionized water, and aqueous solution. Our results showed that ACHA exhibited a superior antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. These findings indicated that ACHA was preferable for use as antimicrobial agents in wound healing, food preservative, and tissue engineering.


2021 ◽  
Vol 37 (2) ◽  
pp. 413-418
Author(s):  
Sachin Govind Bibave ◽  
S. J. Takate ◽  
A.E. Athare

Theβ-dike toneis synthesizedvia the named Baker-Venkataraman. In currenttask, β-dike tone ligand mixed with different metal nitrates and form different metal complexes such as Ni(II), Fe(III), Cr(III). Ligand gives tautomerism, this tautomerism process was examined with the help ofFTIR.Because of enol assist as ligand in the metal complexes preparation. The preparedmetal complexearede scribed by various techniques like elemental analysis, FTIR, DTA, TGA, magnetic properties and molar conductivities. Different properties of complexes are studied such as antioxidant, antibacterial, anti-inflammatory and anti fungal properties.


1986 ◽  
Vol 64 (4) ◽  
pp. 751-759 ◽  
Author(s):  
Daniel Cozak ◽  
Abdelhakim Mardhy ◽  
André Morneau

The reaction of CpTi(CO)2 (1), Cp2TiCl (2), and Cp2TiCl2 (3) (Cp = η5-C5H5) with purine (PuH) and adenine (AdH) in organic solvents is described. The compound 1 reacts with both molecules in an oxidative fashion giving Cp2Ti(C5H3N4)(C5H4N4) (4) and (Cp2Ti)2(C5H3N5) (5) with concomitant liberation of molecular carbon monoxide and hydrogen (4:1) following a first order rate law in metal complex. The compound 2 forms an adduct compound Cp2TiCl(C5H4N4) (6) with PuH. Monosubstituted derivatives Cp2TiCl(C5H3N4) (7) and Cp2TiCl(C5H4N5) (8) are formed from the reaction of the deprotonated bases with 3. In addition to the usual elemental analysis, the characteristic ir, 1H nmr, epr, and ms results are given for the new compounds.


2009 ◽  
Vol 2009 (7) ◽  
pp. 448-451 ◽  
Author(s):  
Hanan M. Refaat ◽  
Omneya M. Khalil ◽  
Suzan M. Abuel-Maaty

In this study, a novel series of 6-oxopyridazinyl benzazoles and 3, 6-dioxopyridazinyl benzazoles were prepared from the starting compounds, 2-hydrazinobenzimidazole, 2-hydrazinobenzothiazole and 2-hydrazinobenzoxazole by reaction with butyric acid derivatives and cyclic anhydrides respectively. The structures of the new compounds were confirmed by elemental analysis as well as 1H NMR, IR and MS data. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity using carrageenan induced paw edema at dose 100 mg kg−1 using indomethacin as a reference standard and were found to be bioactive.


2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Sebastián Pizarro ◽  
Guillermo Saá ◽  
Francisco Gajardo ◽  
Alvaro Delgadillo

The synthesis of a new heterobinuclear cobaloxime with 4-(2-ferrocenylvinyl)pyridine, fcvpy, is reported. The complex [CoCl(dmgH)2(fcvpy)], where dmgH2is dimethylglyoxime and dmgH is dimethylglyoximato, has been characterized by1H-NMR, UV-Vis, cyclic voltammetry, and elemental analysis. The cyclic voltammogram of this complex shows a fc/fc+reversible wave at +0.58 V versus Ag/AgCl, one irreversible wave,Epc= −0.54 V versus Ag/AgCl, assigned to the reduction of Co(III) to Co(II), and two quasireversible processes at −1.02 V and −1.10 V versus Ag/AgCl associated with the reduction of Co(II). The complex showed ferrocene-ligand charge transfer bands at 334 nm and 505 nm. TDDFT/B3LYP/6-31G(d) calculations support this assignation.


2001 ◽  
Vol 05 (04) ◽  
pp. 367-375 ◽  
Author(s):  
S. ZEKİ YILDIZ ◽  
HALTİ KANTEKİN ◽  
YAŞAR GÖK

New metal-free 5 and metallophthalocyanines 6-11( M = Cu , Ni , Co , Pb , Zn ) fused in peripheral positions with four 24-membered tetraoxatetraaza macrocycles were prepared by cyclotetramerization of 24,25-dicyano-4,10,13,17-tetra(toluene-p-sulfonyl)-1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22-didicontinehydrobenzo[y][3,9,12,18]tetraaza[1,7,16,22]tetraoxatetradicontine in the presence of the corresponding metal salt or a strong organic base. While the N-tosylated derivatives of the phthalocyanines are soluble in common organic solvents, the detosylated derivative of copper phthalocyaninate is soluble in water. The aggregation properties of the phthalocyanines were also investigated as a function of concentration, solvent and oxidative medium. The new compounds are characterized by a combination of elemental analysis and 1 H NMR, 13 C NMR, IR, UV-vis and MS spectral data.


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