Synthesis, Characterization and Antibacterial Activity of New Derivatives of Imidazolidine having Sulfamethoxazole Moiety

This work includes Synthesis of new series of sulfa drugs derived from sulfamethoxazole containing substituted Imidazolidine moiety. These compounds expected to have antibacterial activity, due to their Imidazolidine moiety This work includes synthesis of some new Schiff bases (II1-5) by condensation of sulfamethoxazole drug(I) with some aldehydes (1-5) (benzaldehyde, p-chloro benzaldehyde, p-nitro benzaldehyde, p-hyroxy benzaldehyde and p-N, N-dimethyl amino benzaldehyde). These Schiff bases were found to react with glycine, to prepared new imidazolidine derivatives (III1-5). The prepared compounds were characterized by physical properties, FT-IR and of the 1H-NMR spectroscopy. The preliminary study of antibacterial activity of final compounds has considered by well diffusion method. The tested compounds displayed effect against gram negative bacteria:( Acinetobacter species and Pseudomonas aeruginosa) and gram-positive bacteria (Streptococcus pyougenes and Staphylococcus aureus bacteria), which compared to DMSO as control, and good activity compared to sulfamethoxazole as standard.

2017 ◽  
Vol 9 (2) ◽  
pp. 45 ◽  
Author(s):  
Bahareh Behmaram ◽  
Naser Foroughifar ◽  
Neda Foroughifar ◽  
Sara Hallajian

The synthesis of some 1,3-diazoles and thiazoles was realized in different conditions:a) In the presence of PTSA or sulfuric acid as catalyst we obtained only diazole products(4a-d).b) In basic medium such as DABCO or sodium hydroxide and ionic liquid afforded thiazoles.c) Both products, diazoles and thiazoles were collected when using methanol as catalyst and solvent.All structures were confirmed by IR, 1H NMR and 13C NMR spectroscopy. The antibacterial activity of some synthesized compounds was investigated against Escherichia Coli (ATCC: 25922) and Serratia marcescens (ATCC: 13880) as gram negative bacteria, Bacillus sabtilis (ATCC: 6633) and Staphylococcus aureus (ATCC: 6338) as gram positive bacteria. Some of these products exhibit good activities to significant antibacterial activity.


INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (05) ◽  
pp. 44-47
Author(s):  
S. D. Bhinge ◽  
◽  
M. G Hogade ◽  
A. S Savali ◽  
H. R. Chitapurkar ◽  
...  

Petroleum ether, ethanol and aqueous extracts of the bark of Ficus glomerata (Urticaceae) were screened for their antibacterial activity using agar diffusion method. They were tested against six bacteria; three Gram-positive bacteria (Bacillus subtilis, Bacillus aureus and Staphylococcus aureus) and three Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa). The susceptibility of the microorganisms to the extracts of these plants was compared with each other and with selected antibiotics.


2017 ◽  
Vol 9 (3) ◽  
pp. 49 ◽  
Author(s):  
Hoda Pasdar ◽  
Naser Foroughifar ◽  
Bahare Hedayati Saghavaz ◽  
Mehran Davallo

A novel series of metal complexes of guanidine ligand derived from condensation of 1,1,3,3-tetramethylurea and 2-aminopyridine in present of POCl3 have been synthesized. The complexes are characterized using FTIR, UV-Vis and also molar conductance was measured. These spectroscopic studies confirmed that the ligand bonded to the metals through the nitrogen atoms. The suggested structures of the metal complexes are square planner. The ligand and its metal complexes were tested against Gram-negative bacteria; Escherichia coli, Serratia marcescens and Gram-positive bacteria; Bacillus sabtilis and Staphylococcus aureus by applying disc diffusion method. The most antibacterial activity of synthesized compounds belongs to CdL2 complex. The results of this study showed that the metal complexes have more antibacterial activity against species when compared to the parent ligand.


Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.


2018 ◽  
Vol 16 (5) ◽  
pp. 341-348
Author(s):  
On-Anong SOMSAP

Antibiotic resistance bacteria has become an increasing problem now today due to many factors. This study investigates the efficacy of Prismatomeris tetrandra K. Schum root extract as a new source of antibacterial activity for antibiotic resistant bacteria using agar well diffusion method. The results showed that S. aureus TISTR517 exhibited more sensitivity to P. tetrandra K. Schum root extract than other Gram-positive bacteria indicator strains. On the other hand, Gram-negative bacteria exhibited resistance to P. tetrandra K. Schum root extract. The study further showed the activity between P. tetrandra K. Schum root extract and gentamycin (10 µg), it revealed that MRSA142 was resistant to gentamycin (10µg) but sensitive to P. tetrandra K. Schum root extract. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) was evaluated by using S. aureus TISTR517 and MRSA142 as indicator strains. The MIC value was 0.59 mg/mL and 1.17 mg/mL for S. aureus TISTR517 and MRSA142, respectively. MBC assay demonstrated that the MBC value was 9.75 mg/mL and 150 mg/mL for S. aureus TISTR517 and MRSA142 respectively. The mode of action was investigated with the presence of P. tetrandra K. Schum root extract in the culture broth. The action of P. tetrandra K. Schum root extract was revealed of bacteriostatic activity due to the Optical density (OD) at 600 nm and Colony-Forming Units (CFU) of indicator strains were continuously decreased.


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


Author(s):  
Chinyere Benardette Chinaka Ikpa ◽  
Uchechukwu C. Okoro ◽  
Collins I. Ubochi ◽  
Kieran O. Nwanorh

The 2-phenylsulphonamide derivatives of amino acids were synthesis by simple substitution of benzenesulphonylchloride (6) with amino acids (1-5) containing pharmacological active functionalities. Structures of the synthesised compounds (7a-7e) were characterised using FT-IR, NMR(1H,13C) and elemental analysis. The anti bacterial activities of the synthesised compounds were evaluated against gram positive bacteria: Staph and Streptococcus, gram negative bacteria: E-coli, Klebsiella, Proteus, and pseudomonas using 200 µl of 10 mg/ml and minimum inhibitory concentration (MIC) were also determined. The compounds exhibited effective anti bacterial properties though some are not more active than the standard drug ciprofloxacin.


2020 ◽  
Vol 10 (5) ◽  
pp. 274-292
Author(s):  
Rohit Kumar ◽  
Sushil Kumar ◽  
Mohammad Asif Khan

Recently a series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtitles and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 μg/ml and 100 μg/ml. Literature review revels that chalcones possesses various biological activities like antimicrobial, antiviral, anti-inflammatory, anticancer and sedative etc. Therefore the present study was designed on synthesis and pharmacological evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides. Target compound was synthesized by reaction of chloroacetylchloride with diphenylamine to afford 2-chloro-N, N-diphenylacetamide which further by reaction with substituted Chalcones and characterized following recrystallization and evaluated for anti-microbial potential through cup-diffusion method. In results, the target compounds were tested for activity against B. Subtilis, E.Coli and C. albicans. The chalcones having the lipophilic 4-chloro group (RKCT2) showed the greatest antimicrobial activity (zone of inhibition 20 & 22 mm against. B. subtilis, E. Coli, C. Albicans respectively. It suggests further researchers to go through anti-microbial evaluations against a more varieties of bacteria and fungi. Keywords: Schiff bases of diphenylamine derivatives, antibacterial activity, Gram-positive bacteria, 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides


2018 ◽  
Vol 6 (2) ◽  
pp. 212
Author(s):  
Elok Dea Orens Ubung Wisnu ◽  
Indah Purnama Sary ◽  
Dwi Koko Pratoko

N-phenylbenzamide is benzamide derivatives, which is potential as an antibacterial agent. N-phenyl-4-chlorobenzamide is N-phenylbenzamide derivative that substitued by chloro to the para position and it was expected to enhance the antibacterial activity. N-phenyl-4-chlorobenzamide was synthesized by reacting 1,3-diphenyilthiourea and 4-chlorobenzoil chloride. This compound has been purified and provided 53% of product with crystal shape, white color, and melting point of 195-197 oC. The purification of this compound was confirmed by TLC and the structure was identified by 1H-NMR, 13C-NMR, and FTIR spectroscopy. This compound was tested for its activity against gram positive bacteria Staphylococcus aureus and gram negative bacteria Pseudomonas aeruginosa, evaluated by well diffusion method and the result showed no activity against both Staphylococcus aureus and Pseudomonas aeruginosa.   Keywords: N-phenyl-4-chlorobenzamide, synthesis, antibacterial activity


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 30-35
Author(s):  
Naveen K. Kottakki ◽  
◽  
Amperayani K. Rao ◽  

In the current study, a series of piperine – piperazine analogues (5a to 5f) were designed and synthesized. The piperine was isolated from pepper and used for the conjugation with heterocyclic moiety for better biological activity. The piperazine heterocyclic was chosen for conjugation with piperine. The newly synthesized structures were determined by IR, 1H NMR and 13C NMR spectral data. The compounds were examined for their anti‐microbial activity against gram-positive (Bacillus subtilis) and gram-negative (Vibrio cholerae) bacteria using the agar well diffusion method. The newly synthesized compounds exhibited capable activities against V. cholerae and B. subtilis and it showed minimum inhibitory concentration. Among all the synthesized compounds, 5f has the highest activity (26 mm) against gram-positive bacteria and (29mm) against gram-negative bacteria. The remaining compounds showed appreciable antibacterial activity. The enhanced activity of the synthesized compounds may be due to the presence of conjugated amide linkage with the natural product piperine and piperazine heterocyclic molecule. The substituents present on the aromatic (nitro-substituted) ring also influenced the activity of the compound.


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