scholarly journals Syntheses of 2-(6’-Fluorobenzothiazol-2’-ylamino)-4, 6-(disubstituted thiouriedo)-1,3-pyrimidine Derivatives as Antimicrobial Agents

2011 ◽  
Vol 8 (1) ◽  
pp. 240-244 ◽  
Author(s):  
Anoop K. Pathak ◽  
Viney Chawla ◽  
Shailendra K. Saraf

A new series of 1,3-pyrimidine derivatives (3a-f) have been synthesized by reacting 2,4,6-Trichloropyrimidine with nucleophilic reagents 2-amino-6-fluorobenzothiazole (1) in the presence of acetone. The (4,6- dichloro-pyrimidin-2-yl)-amine (2) so produced was then reacted to two moles of phenylthiourea derivatives to yield title compounds (3a-f). The structural assessment of the compounds (3a-f) was made on the basis of spectral data. The synthesized compounds were screened for theirin vitrogrowth inhibiting activity against different strains of bacteriaviz.,B. subtilis, E. coli, P. aeruginosaandS. aureususing agar diffusion technique. Compounds3cand3fexhibited highest antibacterial activity.

2019 ◽  
Vol 24 ◽  
pp. 2515690X1988627 ◽  
Author(s):  
Mekonnen Sisay ◽  
Negussie Bussa ◽  
Tigist Gashaw ◽  
Getnet Mengistu

Medicinal plants are targeted in the search for new antimicrobial agents. Nowadays, there is an alarmingly increasing antimicrobial resistance to available agents with a very slow development of new antimicrobials. It is, therefore, necessary to extensively search for new agents based on the traditional use of herbal medicines as potential source. The antibacterial activity of 80% methanol extracts of the leaves of Verbena officinalis (Vo-80ME), Myrtus communis (Mc-80ME), and Melilotus elegans (Me-80ME) was tested against 6 bacterial isolates using agar well diffusion technique. In each extract, 3 concentrations of 10, 20, and 40 mg/well were tested for each bacterium. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were also determined. Vo-80ME and Mc-80ME exhibited promising antibacterial activity against Staphylococcus aureus with the highest zone of inhibition being 18.67 and 26.16 mm, respectively at concentration of 40 mg/well. Regarding gram-negative bacteria, Vo-80ME exhibited an appreciable activity against Escherichia coli and Salmonella typhi. Mc-80ME displayed remarkable activity against all isolates including Pseudomonas aeruginosa with the maximum zone of inhibition being 22.83 mm. Me-80ME exhibited better antibacterial activity against E coli, but its secondary metabolites had little or no activity against other gram-negative isolates. The MIC values of Vo-80ME ranged from 0.16 to 4.00 mg/mL. The lowest MIC was observed in Mc-80ME, with the value being 0.032 mg/mL. Mc-80ME had bactericidal activity against all tested bacterial isolates. Mc-80ME showed remarkable zone of inhibitions in all tested bacterial isolates. Besides, Vo-80ME showed good antibacterial activity against S aureus, E coli, and S typhi. Conversely, Me-80ME has shown good activity against E coli only. Generally, M communis L and V officinalis have good MIC and MBC results.


2021 ◽  
Vol 6 (3) ◽  
pp. 189-195
Author(s):  
Hary Widjajanti ◽  
Christina Vivid Handayani ◽  
Elisa Nurnawati

The antibiotic resistance of phatogenic bacteria has become a serious health problem and has encouraged the search for novel and effective antimicrobial metabolites. Meanwhile, endophytic fungi have great potential as a natural source for antimicrobial agents. The endophytic fungi that live in plant tissue produces secondary metabolites which potentially act as an antibacterial compound. The isolation of fungi for antibacterial sources reduces the large amount of plant as a source of antibacterial agents. Hence, this study aims to obtain endophytic fungi isolates from Paederia foetida L. that are capable of producing secondary metabolites as antibacterial, carry out in vitro tests to verify the antibacterial properties of secondary metabolites of the Paederia foetida L. endophytic fungi, and identify the potential of Paederia foetida L. endophytic fungi in producing antibacterial compounds. The antibacterial activity was tested against Escherichia coli ATCC8739 and Staphylococcus aureus ATCC6538 while seven isolates of endophytic fungi that potentially produced antibacterial were obtained from Sembukan (P. foetida L.). The results showed that antibacterial activities of SL1, SL4 and SL6 secondary metabolites against S. aureus ATCC6538 and E. coli ATCC8739 were moderate to strong activities. Furthermore, the Minimum Inhibition Concentration (MIC) of secondary metabolites extract of SL1 against S. aureus ATCC6538 value was 250 ????g/mL while the values of MIC extract of SL4 against S. aureus ATCC6538 and E. coli ATCC8739 were 125 ????g/mL and 250 ????g/mL respectively and MIC extract of SL6 against E. coli ATCC8739 value was 125 ????g/mL. The secondary metabolites extract of SL1 isolate were alkaloid and tannin, SL4 were phenolic and alkaloid while SL6 isolate were alkaloid and terpenoid. Hence, endophytic fungi SL1 isolate was identified as Fusarium sp., SL4 as Dematophora sp., and SL6 isolate as Acremonium sp.


2018 ◽  
Vol 34 (4) ◽  
pp. 2026-2030 ◽  
Author(s):  
Sarrah Sattar Jabbar

In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.


2016 ◽  
Vol 29 (1) ◽  
pp. 37-40
Author(s):  
Amna Ali ◽  
M Saleem Haider ◽  
Sobia Mushtaq ◽  
Ibatsam Khokhar ◽  
Irum Mukhtar ◽  
...  

The antimicrobial agents of bacteria isolated from different rhizosphere of fruits and vegetables soil in Lahore. Of ten species, five were gram-negative (Escherichia coli, Pseudomonas fluorescence, Klebsiella pneumoniae, Salmonella typhii, Brachybacterium faecium); other five were gram positive and identified as Bacillus farraginis, Kurthia gibsonii, Aureobacterium liquefaciens, Curtobacterium albidum, Micrococcus lylae. The antagonistic potential of bacterial strains was assessed by the well diffusion technique and results indicating varying degree of biocontrol activity against pathogenic strain of X. campestris. Out of ten bacterial species, E. coli (gram negative) and C. albidum (gram positive) showed a high prevalence of resistance with reduction of 4.2cm and 4.1cm zone diameter respectively. The minimum inhibitory volume (MIV) to two bio-agents was determined for X. campestris from range 10-100 ?L. E. coli (volume required to inhibit < 20 ?L) and C. albidum (volume required to inhibit < 40 ?L) exhibited good activity against pathogen. These results provide information on the prevalence of resistant bacterial strains with the MIV of organisms and indicate the possibility of using these bacterial species as bio-agent against X. campestris.Bangladesh J Microbiol, Volume 29, Number 1, June 2012, pp 37-40


Author(s):  
Sergey S. Patrushev ◽  
Lyubov G. Burova ◽  
Anna A. Shtro ◽  
Tatyana V. Rybalova ◽  
Dmitry S. Baev ◽  
...  

Background: Natural sesquiterpene lactones are an important class of heterocyclic compounds in drug discovery since they are possessed a wide range of biological properties including antibacterial activity. Objective: The objective of this study was to synthesize of isoalantolactone derivatives with a furo[2,3-d]pyrimidin-2-оne moiety and to evaluate their antibacterial and antiviral activity. Methods: The Sonogashira cross-coupling and subsequent Ag-catalyzed cyclization reactions were the main routes of synthesis. The antibacterial activity and the ability to inhibit biofilms formation on E. coli, S. aureus, A. viscosus, P. aeruginosa and E. faecalis bacterial strains were evaluated. A study of the molecular interactions of new compounds with the multiple virulence factor regulators was performed using docking simulations. The antiviral activity against influenza A virus and human orthopneumovirus H-2А was also studied. Results: The in vitro antibacterial activity for 4 (MIC = 58.33±4.41 μg/mL) concerning E. coli and 5 (MIC = 96.5±3.25 μg/mL) against A. viscosus and the inhibition of biofilm formation for compounds 2, 4, and 5 on E. coli, S. aureus, P. aeruginosa and E. faecalis bacterial strains has been of interest for the search of improved antimicrobial agents. Compound 3 was endowed with antiviral activity to human orthopneumovirus H-2А with SI >33. The activity of the new type of hybrid compounds is depended on the substituent in the 6th position of furo[2,3-d]pyrimidin-2-one fragment. Conclusion: The decoration of isoalantolactone with a furo[2,3-d]pyrimidin-2-one fragment led to perspective antiviral and antimicrobial agents. Due to antimicrobial activity, pyridine-4-yl substituted isoalantolactone-furopyrimidinone hybrid is considered as a candidate compound to participate in further research.


2017 ◽  
Vol 5 (2) ◽  
pp. 256-260 ◽  
Author(s):  
Shiv Nandan Sah ◽  
Sunil Regmi ◽  
Man Kumar Tamang

Various medicinal plants are common in use in Nepal for the treatment of different diseases. Nowadays, drug resistance has emerged as a major problem for various infections, in such case plants can be used as alternative for the production of new antimicrobial agents. Thuja (in Nepali: dhupi) is a small evergreen genus of the Cupressaceae family. This species is widely cultivated as a common ornamental plant in Nepal and India. This study examined the antibacterial activity of Thuja leaves extract on gram positive (Staphylococcus aureus and Streptococcus spp.) and gram-negative bacteria (E. coli and Pseudomonas aeruginosa). Thuja leaves were collected from different localities of Dharan, and dried under shade for 10 days. They were then grinded using mechanical grinder. Leaf extract (oleoresin) was obtained by soxhlet extraction technique using mixture of Ethyl acetate, Ethanol and chloroform in the ratio 40:30:30 as the solvent. The antibacterial activity of Thuja oleoresin was tested using both Agar well diffusion as well as disc diffusion technique. Minimum Inhibitory Concentration(MIC) was  determined by agar well diffusion on MHA plates. Thuja oleoresin showed distinct antibacterial activity towards all four isolates on both agar well and disc diffusion methods. MIC for Pseudomonas aeruginosa and Streptococcus spp. was found to be 12.5 µl whereas for E. coli and Staphylococcus aureus, MIC was 25 µl. Thus from our results, it is concluded that Thuja leaves have antibacterial effects and can be a potential source for production of antibacterial drugs.Int. J. Appl. Sci. Biotechnol. Vol 5(2): 256-260


2008 ◽  
Vol 5 (s1) ◽  
pp. S1008-S1014
Author(s):  
Jyoti Sharma ◽  
Sabir Hussain ◽  
Mohammad Amir

New series of 4-(substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-4H-1,2,4-triazole-3-thiol(4a-c),N³-(4-substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-4H-1,2,4-triazole-3,4-diamine(5a-c)andN-(4-substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-1,3,4-thiadiazol-2-amine(6a-g)have been synthesized and the structures of the new compounds were established on the basis of IR,1H NMR spectral data.In vitroantimicrobial activity (MIC activity) was evaluated and compared with standard drugs of loxacin and ketoconazole. Compounds5aand6ein the series have shown interesting antibacterial activity against bothS. aureus(gram-positive) andE. coli(gram-negative) organisms. In this paper, we also describe studies leading to identification of antifungal agents. In the gratifying result, most of the compounds were found to have moderate antimicrobial activity.


Author(s):  
Jignesh Priyakant Raval ◽  
Akhaja T N ◽  
Myangar K N ◽  
D R Naik

A novel new series of 2-[(4'-oxo-3'-chloro-2'-phenylazetidin-1'-yl)-aminomethyl]-3-[N-isonicotinamide-yl]-6-iodo-quinazolin-4-ones were synthesized using the reaction of chloroacetylchloride and appropriate Schiff base. The synthesized compounds were characterized on the basis of their elemental and spectral analysis (IR, 1H-NMR, 13C-NMR and mass spectrometry). All newly synthesized compounds were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv. They were also tested in vitro for antibacterial activity against selected human pathogens such as E. coli, P. aeruginosa, K. pneumoniae, S. typhi, S. aureus, S. pyogenus, B. subtilis and antifungal activity against C. albicans, A. niger, A. clavatus strains. The selected 6-iodo-quinazolinonones showed promising biological activity and could be useful as antimicrobial agents.   


Author(s):  
Touhida Ishma ◽  
H. M. Sayeed Uddin ◽  
Anik Paul ◽  
Farahnaaz Feroz ◽  
Mrityunjoy Acharjee

<p class="abstract"><strong>Background:</strong> Practice of hand washing is very important to eliminate the microbial contamination especially during the work in laboratories, hospital and even at home before taking food. Proper use of hand sanitizer can significantly reduce the rate of hospital acquired infection also.</p><p class="abstract"><strong>Methods:</strong> The current investigation was designated to identify different bacterial species from the upper skin of hands of the laboratory managements through conventional culture methods and the efficacy of the samples (Dettol, Purell and Savlon) against the isolated bacteria through agar well diffusion method and minimum inhibitory concentration (MIC)  </p><p class="abstract"><strong>Results:</strong> Different concentrations such as 25%, 50% and 100% of each of antimicrobial agents showed their antibacterial activity against <em>Staphylococcus </em>spp., <em>Klebsiella </em>spp., <em>E. coli</em> and <em>Pseudomonas</em> spp. those were isolated from the hand. 25% of Dettol exhibited 20 mm zone diameter against <em>Klebsiella</em>spp. Whereas 25% of Purell and Savlon unveiled 15 mm and 22 mm zone of inhibition against <em>E. coli</em> and <em>Pseudomonas</em> spp. respectively. In case of 100% sample of Dettol, Purell and Savlon, the highest zone diameter was observed as 55 mm, 50 mm and 45 mm against <em>Klebsiella </em>spp.,<em> Staphylococcus </em>spp., and <em>E. coli</em> consecutively. The MIC of Dettol sample was 8 µl against <em>Staphylococcus </em>spp., and <em>Pseudomonas</em> spp. In case of Purell, the MIC was 128 µl against <em>Staphylococcus</em> spp., <em>Klebsiella </em>spp. and <em>Pseudomonas </em>spp. were inhibited at 4 µl samples.</p><p class="abstract"><strong>Conclusions:</strong> The in-vitro antibacterial activity of the hand sanitizers was so satisfactory against the isolated bacteria. This finding would be very helpful for the laboratory management in order to minimize the rate of contamination during the research and supervision of the different experiment.</p>


Author(s):  
Anees A Siddiqui ◽  
Asif Husain ◽  
M Shaharyar ◽  
Mohd Rashid ◽  
Ravinesh Mishra ◽  
...  

1,3,4-oxadiazoles are important because of its versatile biological actions. In the present study, several 2-(quinoline-8-yloxymethyl)-5-aryl-1,3,4-oxadiazole derivates (IIIa-j) have been synthesized by the condensation of 8-hydroxy quinoline acetyl hydrazide (II) with various aromatic acids in presence of phosphorous oxychloride. The structures of the newly synthesized compounds have been established on the basis of elemental analysis, UV, IR, and 1H NMR spectral data. The synthesized compounds were screened for their in vitro growth-inhibiting activity against different strains of bacteria and fungi viz., S aureus, E. Coli, P. aeruginosa, C. Albicans, A. flavus, and A. fumigates, and the results were compared with the standard such as Ampicillin (50µg/ml) using agar diffusion technique. Compounds IIIc and IIIf were found to be equipotent as ampicillin when tested against the strains of E.Coli where as tested compounds IIIc, IIIf and IIIi showed good antibacterial and antifungal activity when tested against the strains of S. aureus, P. aeruginosa, and C. Albicans.


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