scholarly journals Synthesis and In Vitro Antimicrobial Activity of 3-(5-((2-Oxo-2H-Chromen-4-yl)Thio)-4-Phenyl-Thiazol-2-yl)-2-Substitutedphenyl Thiazolidin-4-One

2015 ◽  
Vol 51 ◽  
pp. 135-143
Author(s):  
Himanshu R. Prajapati ◽  
Harshad P. Lakum ◽  
Kishor H. Chikhalia
Keyword(s):  
Antimicrobial Activity ◽  
Thioglycolic Acid ◽  
Moderate Activity ◽  
Mass Analysis ◽  
Dilution Technique ◽  
H Nmr ◽  
Microbial Strain ◽  
Broth Dilution ◽  
C Nmr

An array of 3-(5-((2-oxo-2H-chromen-4-yl) thio)-4-phenyl thiazol-2-yl)-2-substitutedphenyl thiazolidin-4-one (7a-j) have been synthesized by using acetophenone, thiourea, 4-mercaptocoumarin and thioglycolic acid. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR and mass analysis. All the newly synthesized derivatives were evaluated for their in vitro antibacterial activity (against E.coli,P.aeruginosa,S.aureus, S. pyogenes) and antifungal activity against (C. albicans, A.niger, A.clavatus) using broth dilution technique. Some of the compounds showed good to moderate activity against the specific microbial strain.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<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>

scholarly journals Approach for the Synthesis of Potent Antimicrobials Containing Pyrazole, Pyrimidine and Morpholine Analogues

2016 ◽  
Vol 69 ◽  
pp. 87-96 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Bonny Y. Patel ◽  
Bharti P. Dave
Keyword(s):  
Antimicrobial Activity ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Sar Studies ◽  
Mueller Hinton ◽  
Morpholine Derivatives ◽  
Mueller Hinton Broth ◽  
C Nmr

The present study is in the interest of some synthesized novel derivatives containing 4-(1,3-diphenyl-1H-pyrazol-4-yl)-N-(morpholinomethyl)-6-arylpyrimidin-2-amines pooled with different bio-active heterocycles such as pyrazole, pyrimidine and morpholine derivatives. The structures of newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains using Mueller-Hinton Broth dilution method. On the basis of SAR studies, it was observed that the presence of electron withdrawing groups remarkably enhanced the antimicrobial activity of synthesized compounds.

scholarly journals Synthesis and In Vitro Antibacterial and Antifungal Evaluation of Quinoline Analogue Azetidin and Thiazolidin Derivatives

2014 ◽  
Vol 39 ◽  
pp. 195-210 ◽  
Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  
Keyword(s):  
Gram Negative Bacteria ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal ◽  
Broth Dilution

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.

scholarly journals Isolation and Antimicrobial Activity of β-Sitosterol-3-O-Glucoside from Lannea Kerstingii Engl. & K. Krause (Anacardiacea)

2016 ◽  
Vol 06 (01) ◽  
pp. 004-008
Author(s):  
Njinga N. S. ◽  
Sule M. I. ◽  
Pateh U. U. ◽  
Hassan H. S. ◽  
Abdullahi S. T. ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Wide Spectrum ◽  
Diffusion Method ◽  
Dilution Method ◽  
Minimum Fungicidal Concentration ◽  
E Coli ◽  
H Nmr ◽  
Vacuum Liquid Chromatography ◽  
Broth Dilution ◽  
C Nmr

AbstractThe emergence of more and more drug resistance bacteria has led to the study of the antimicrobial activity of the compound isolated from Lannea kerstingii Engl. & K. Krause (Anacardiacea) since the active principles of many drugs found in plants are secondary metabolites. A compound was isolated using dry vacuum liquid chromatography and eluting with CHCl3 -EtOAc and monitored using TLC. 3 1 13 The glycoside was characterized using 1 H NMR and 13 C NMR spectra recorded in DMSO-d6 at 400 MHz and 125 MHz, respectively. The antimicrobial activity of the compound was determined using agar diffusion method. The minimum inhibitory concentration (MIC) and minimum bactericidal/minimum fungicidal concentration (MBC/MFC) was determined using broth dilution method. The compound isolated was found to be β-sitosterol-3-O-glucoside. The β-sitosterol-3-O-glucoside (200μg/ml) was active against S. aureus, Methicillin Resistant Staphylococcus aureus, P. mirabilis, S. typhi, K. pneumoniae, E. coli, B. subtilis with zone of inhibition ranging from 24mm to 34mm and inactive against P. aeroginosa and Proteus vulgaris. It was also active against the fungi C. albicans and C. tropicalis but inactive against C. krusei. The MIC ranged from 25 to 50 μg/ml while the MBC/MFC ranged from 50 to 200 μg/ml. These results show the wide spectrum antimicrobial activity of β-sitosterol-3-O-glucoside.

scholarly journals Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

2016 ◽  
Vol 69 ◽  
pp. 42-48
Author(s):  
Pineshkumar N. Patel ◽  
Denish C. Karia
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Glacial Acetic Acid ◽  
Mixed Solvent ◽  
Dilution Method ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Broth Dilution ◽  
C Nmr

Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin.

scholarly journals Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency

2016 ◽  
Vol 66 ◽  
pp. 1-12 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Tushar J. Karkar
Keyword(s):  
Antimicrobial Activity ◽  
Synthesis And Characterization ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Broth Dilution ◽  
C Nmr

The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR,1H NMR,13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against selected fungal strains.

Synthesis and antimicrobial activity of novel thienopyrimidine linked rhodanine derivatives

2019 ◽  
Vol 97 (2) ◽  
pp. 94-99 ◽  
Author(s):  
Nagaraju Kerru ◽  
Surya Narayana Maddila ◽  
Suresh Maddila ◽  
Sreedhar Sobhanapuram ◽  
Sreekantha B. Jonnalagadda
Keyword(s):  
Antimicrobial Activity ◽  
Condensation Reaction ◽  
Dilution Method ◽  
The Novel ◽  
E Coli ◽  
H Nmr ◽  
Target Molecules ◽  
Novel Target ◽  
C Nmr

This work presents the preparation of a new series of N-(substituted phenyl)-2-(4-oxo-5-(4-(thieno[2,3-d]-pyrimidin-4-yloxy)benzylidene)-2-thioxothiazolidin-3-yl)acetamide derivatives (8a–8l). A condensation reaction of thienopyrimidin-2-thioxothiazolidin-4-one derivative (5) with various 2-chloro-N-phenylacetamides (7a–7l) was employed to afford the new thienopyrimidine tagged rhodanine derivatives under acetone solvent in the presence of potassium carbonate (K2CO3). All of the novel target molecules were characterized by IR, 1H NMR, 13C NMR, and LC–MS spectral analyses and were screened for their in vitro antimicrobial activity by using the broth dilution method. Compounds 8c, 8g, and 8h found to have antibacterial potency against E. coli, B. subtilis, B. cereus, and K. pneumonia with minimum inhibitory concentrations (MICs) of 3.25–6.25 μg/mL compared with the standard Gentamicin. Compounds 8c and 8f demonstrated better antifungal potency (MIC = 3.25–6.25 μg/mL) against A. flavus, A. niger, P. marneffei, and C. albicans when compared with Fluconazole.

scholarly journals Synthesis and In Vitro Antimicrobial Evaluation of Amine Substituted s-Triazine Based Thiazolidinone/Chalcone Hybrids

2014 ◽  
Vol 36 ◽  
pp. 207-219
Author(s):  
Dhruvin R. Shah ◽  
Harshad P. Lakum ◽  
Kishor H. Chikhalia
Keyword(s):  
Multidrug Resistant ◽  
Drug Candidate ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Potent Drug ◽  
Broth Dilution ◽  
Mic Value

In an attempt to control multidrug resistant dilemma, a library of s-triazine based on two novel series of thiazolidinone (4a-e) and chalcone (7a-e) derivatives were designed and synthesized with simple and efficient etiquette. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus Aureus, Bacillus Cereus, Pseudomonas Aeruginosa, Klebsiella Pneumoniae,) and fungi (Candida Albicans, Aspergillus Clavatus) using the broth dilution technique. Compound 7d was the best bioactive desired antibacterial analogue with less MIC value against different tested strains. Results of bioassay study revealed the future hope of the potent drug-candidate based on s-triazine scaffold. All the final synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass and elemental analysis.

scholarly journals A Convergent Approach for the Synthesis of New Pyrazolyl Bipyridinyl Substituted Coumarin Derivatives as Antimicrobials

2014 ◽  
Vol 40 ◽  
pp. 1-16 ◽  
Author(s):  
Varun G. Bhila ◽  
Yogita L. Chovatiya ◽  
Chirag V. Patel ◽  
Rakesh R. Giri ◽  
Dinkar I. Brahmbhatt
Keyword(s):  
Antimicrobial Activity ◽  
Coumarin Derivatives ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
H Nmr ◽  
Convergent Approach ◽  
C Nmr ◽  
Substituted Coumarins

Some new 3-[3-(1-phenyl-3-aryl-1H-pyrazol-4-yl) acryloyl] coumarins 3a-f were synthesized (coumarin chalcones) by the condensation of various 3-acetyl coumarins 1 and appropriate 1-phenyl-3-aryl-1H-pyrazole-4-carbaldehyde 2. These coumarin chalcones 3a-f were then employed for the synthesis of pyrazolyl bipyridinyl substituted coumarins 7a-f, 8a-f, and 9a-f under Krohnke’s reaction condition. The characterization of all the synthesized compounds was carried out by elemental analysis, IR, 1H-NMR, 13C-NMR, DEPT-135 and mass spectral analysis. In addition to that, in vitro antimicrobial competency of the title compounds was assessed against selected pathogens. Compounds 3b, 3e, 7b, 8b, 8c and 9b exhibited excellent antimicrobial activity and said to be the most proficient members of the series.

scholarly journals Synthesis and Antimicrobial Activity of Coumarinyl Schiff Base Derivatives

2014 ◽  
Vol 30 ◽  
pp. 193-201 ◽  
Author(s):  
Arun Mishra ◽  
Jaynt Rathod ◽  
Dipti Namera ◽  
Shailesh Thakrar ◽  
Anamik Shah
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Gram Negative ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Test Organisms ◽  
Ft Ir ◽  
C Nmr

We have reported some novel N’-[(1)-ethylidene]-2-(6-methyl-2-oxo-2H-chromen-4-yl) acetohydrazide synthesized by conventional method. The reaction of 2-(6-methyl-2-oxo-2H-chromen-4-yl)acetohydrazide with substituted benzaldehyde in methanol as a solvent yielded a series of (7a-l). The structures of all synthesized compounds are well characterized by Mass, FT-IR, 1H NMR, 13C NMR and elemental analysis. Moreover, all synthesized compounds were screened for In Vitro antimicrobial activity against the gram positive (Staphylococcus aureus, Bacilluas subtilis) and gram negative (Escherichia coli, P. aeruginosa, K. pneunonae, Enterobacter) bacterial strain. In which some the compounds show potential inhibition against the test organisms.

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