scholarly journals Synthesis, spectral studies and in vitro antimicrobial activity of some new di/tri-organotin (IV) complexes of Schiff bases derived from 2-benzoylpyridine

2017 ◽  
Vol 82 (1) ◽  
pp. 13-23 ◽  
Author(s):  
Priyanka Khatkar ◽  
Sonika Asija ◽  
Namita Singh
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Lipid Membrane ◽  
Antimicrobial Activities ◽  
Molar Ratio ◽  
Spectral Studies ◽  
Dilution Method ◽  
Gram Positive ◽  
Gram Negative

In the present work, a series of twenty-four organotin (IV) complexes of the type [R2SnLCl, R3SnL] have been synthesized by the condensation of 2-benzoylpyridine Schiff bases with R2SnCl2, R3SnCl (R= Me, n-Bu, Ph) in 1:1 molar ratio. These complexes were well characterized by IR, 1H, and 13C, 119Sn NMR, XRD and mass spectral techniques. In the search for biologically more effective antimicrobial agents, all the synthesized ligands and organotin complexes were evaluated for their in vitro antimicrobial activities against two Gram positive and two Gram negative bacteria, and two fungal strains by serial dilution method. The results of spectral data revealed that the complexes formed were hexacoordinated with tridentate ligands which coordinated through azomethine N, pyridine N and carboxylate O ligation sites. The ligands on co-ordination with tin metal showed a discernible augmentation in biocidal activity, however, the Ph and Bu complexes were found to be more intoxicating. The results revealed that the synthesized complexes were more noxious towards Gram positive strains as compared to Gram negative strains which may be attributed to the presence of an outer lipid membrane of lipopolysaccharides.

scholarly journals DESIGN, SYNTHESIS, DOCKING STUDIES AND BIOLOGICAL EVALUATION OF 2-PHENYL-3-(SUBSTITUTED BENZO[d] THIAZOL-2-YLAMINO)-QUINAZOLINE-4(3H)-ONE DERIVATIVES AS ANTIMICROBIAL AGENTS

2018 ◽  
Vol 10 (10) ◽  
pp. 57
Author(s):  
Pooja Pisal ◽  
Meenakshi Deodhar ◽  
Amol Kale ◽  
Ganesh Nigade ◽  
Smita Pawar
Keyword(s):  
Antimicrobial Agents ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Fusion Reactions ◽  
Gram Positive ◽  
Gram Negative

Objective: A new series 2-phenyl-3-(substituted benzo[d] thiazol-2-ylamino)-quinazoline-4(3H)-one was prepared by the fusion method by reacting 2-phenyl benzoxazine with 2-hydrazino benzothiazole and it was evaluated for their antimicrobial activity against gram positive, gram negative bacteria and fungi.Methods: Titled compounds were synthesized by fusion reactions. These compounds were evaluated by in vitro antibacterial and antifungal activity using the minimum inhibitory concentration and zone of inhibition methods. The synthesized compounds were characterized with the help of infrared, NMR and mass spectral studies. The benzothiazole moiety and the quinazoline ring have previously shown DNA gyrase inhibition and target related antibacterial activity. Thus, molecular docking studies of synthesized compounds were carried out (PDB: 3G75) to study the possible interaction of compounds with the target. The batch grid docking was performed to determine the probable.Results: These compounds showed significant activity against gram positive and gram negative bacteria as well against the fungi. The compound A5 was found to be active against B. subtilis, P aeruginosa and C. albican at 12.5 µg/ml MIC. The compound A3 was found to be active against all microbial strains selected at 25 and 12.5 µg/ml MIC.Conclusion: Though the relationship between the activities shown by these compounds in, the antimicrobial study is still to be established, the docking studies conducted found to be consistent with antimicrobial results. Thus the results indicate that the designed structure can be a potential lead as an antimicrobial agent.

scholarly journals Design, Synthesis, and Evaluation of Novel 3-, 4-substituted, and 3,4-di Substituted Quinazoline Derivatives as Antimicrobial Agents

2020 ◽  
Vol 71 (2) ◽  
pp. 422-435
Author(s):  
Farag A. El-Essawy ◽  
Abdulrahman I. Alharthi ◽  
Mshari A. Alotaibi ◽  
Nancy E. Wahba ◽  
Nader M. Boshta
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Spectroscopic Analyses ◽  
Quinazoline Derivatives

A novel series of 3-, 4-substituted, and 3,4-di substituted quinazoline derivatives were prepared via various cyclized regents and most of the newly prepared compounds evaluated for their antimicrobial activities in vitro against Gram-positive, Gram-negative bacterial strains and fungi strains. The structures of the quinazoline derivatives have been confirmed using spectroscopic analyses (IR, NMR, and EI-MS). Some of the synthesized derivatives displayed a moderate antimicrobial activity in comparison with reference drugs, for example compounds 13d, 15a, 17b, 18b, 18d, 25, and 29a-c. Among the synthesized compounds, the pyrimidoqunazoline derivative 6c elicited the highest activity.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

3,4-Dihydropyrimidin-2(1H)-One Analogues: Microwave irradiated Synthesis with Antimicrobial and Antituberculosis Study

2019 ◽  
Vol 6 (1) ◽  
pp. 61-70
Author(s):  
Navin Patel ◽  
Sabir Pathan ◽  
Hetal I. Soni
Keyword(s):  
Microwave Irradiation ◽  
Biginelli Reaction ◽  
Antitubercular Activity ◽  
Antimicrobial Activities ◽  
Chemical Diversity ◽  
Spectral Studies ◽  
Dilution Method ◽  
Bacterial Strains ◽  
Microwave Irradiation Method

Background: For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation. Objective: The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds. Methods:: Microwave irradiation was used for the synthesis of 2-((3-cyano-4-(3,4-dichloro phenyl)- 6-(4-hydroxy-3-methoxyphenyl) pyridin-2-yl) amino)-N-(5-(substituted) -(6-methyl-2-oxo -1,2,3,4- tetrahydro pyrimidin-5-yl)-1,3,4-oxadiazol-2-yl)acetamide by using Biginelli reaction. New structural analogues were confirmed by spectral studies followed by their screening for in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus Pyogenus, Escherichia coli and Pseudomonas aeruginosa bacterial strains and for antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity determined out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium. Results: As compared to the conventional method, microwave irradiation method is advantageous for the synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antitubercular activity were found for some of the compounds. Conclusion: Microwave irradiation method provided an effective way to discover a novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.

scholarly journals Bacterial Cellulose Containing Combinations of Antimicrobial Peptides with Various QQ Enzymes as a Prototype of an “Enhanced Antibacterial” Dressing: In Silico and In Vitro Data

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1155
Author(s):  
Aysel Aslanli ◽  
Ilya Lyagin ◽  
Nikolay Stepanov ◽  
Denis Presnov ◽  
Elena Efremenko
Keyword(s):  
Antimicrobial Peptides ◽  
Bacterial Cellulose ◽  
In Silico ◽  
Antimicrobial Agents ◽  
Penicillin Acylase ◽  
Signal Molecules ◽  
Bacterial Cells ◽  
Gram Positive ◽  
Gram Negative

To improve the action of already in use antibiotics or new antimicrobial agents against different bacteria, the development of effective combinations of antimicrobial peptides (AMPs) with enzymes that can quench the quorum (QQ) sensing of bacterial cells was undertaken. Enzymes hydrolyzing N-acyl homoserine lactones (AHLs) and peptides that are signal molecules of Gram-negative and Gram-positive bacterial cells, respectively, were estimated as “partners” for antibiotics and antimicrobial peptides in newly designed antimicrobial–enzymatic combinations. The molecular docking of six antimicrobial agents to the surface of 10 different QQ enzyme molecules was simulated in silico. This made it possible to choose the best variants among the target combinations. Further, bacterial cellulose (BC) was applied as a carrier for uploading such combinations to generally compose prototypes of effective dressing materials with morphology, providing good absorbance. The in vitro analysis of antibacterial activity of prepared BC samples confirmed the significantly enhanced efficiency of the action of AMPs (including polymyxin B and colistin, which are antibiotics of last resort) in combination with AHL-hydrolyzing enzymes (penicillin acylase and His6-tagged organophosphorus hydrolase) against both Gram-negative and Gram-positive cells.

scholarly journals Synthesis, Characterization, and Thermal and Antimicrobial Activities of Some Novel Organotin(IV): Purine Base Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik
Keyword(s):  
Antimicrobial Agents ◽  
Rhizopus Oryzae ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Purine Base ◽  
Mass Spectral ◽  
E Coli ◽  
Kinetic And Thermodynamic Parameters ◽  
C Nmr

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.

scholarly journals In Vitro Activities of a New Des-Fluoro(6) Quinolone, Garenoxacin, against Clinical Anaerobic Bacteria

2003 ◽  
Vol 47 (11) ◽  
pp. 3667-3671 ◽  
Author(s):  
A. Liebetrau ◽  
A. C. Rodloff ◽  
J. Behra-Miellet ◽  
L. Dubreuil
Keyword(s):  
Clostridium Difficile ◽  
Anaerobic Bacteria ◽  
Bacteroides Fragilis ◽  
Antimicrobial Activities ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Gram Positive ◽  
Agar Dilution ◽  
Gram Positive Cocci

ABSTRACT The antimicrobial activities of garenoxacin and eight other antibiotics against 641 anaerobic isolates were evaluated with the NCCLS agar dilution method. Overall, the MICs of garenoxacin for 50 and 90% of the strains tested (in micrograms per milliliter) were as follows: Bacteroides fragilis group, 0.5 and 2; Prevotella spp., 0.25 and 2; Fusobacterium spp., 0.25 and 0.5; Porphyromonas spp., 0.125 and 0.25; Bilophila wadsworthia, 0.5 and 1; Veillonella spp., 0.25 and 0.5; Clostridium spp., 0.25 and 1; Clostridium difficile, 2 and >64; Bifidobacterium spp., 1 and 2; Eggerthella lenta, 0.25 and 1; Propionibacterium spp., 0.5 and 0.5; gram-positive cocci, 0.125 and 0.25.

scholarly journals New oxadiazole derivatives of isonicotinohydrazide in the search for antimicrobial agents: Synthesis and in vitro evaluation

2012 ◽  
Vol 77 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Manav Malhotra ◽  
Mohit Sanduja ◽  
Abdul Samad ◽  
Aakash Deep
Keyword(s):  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Spectral Studies ◽  
Dilution Method ◽  
Mass Spectral ◽  
Oxadiazole Derivatives ◽  
Derivatives Of ◽  
And Staphylococcus Aureus

Structural modification of the front line antitubercular drug isoniazid provide a lipophilic adaptations of the drug in which hydrazide moiety of isoniazid is replaced by 1,3,4-oxadiazole heterocycles to eliminate in-vivo acetylation by arylamine N-acetyltransferase which results to form inactive acetylated drug. In the present study a series of sixteen oxadiazole derivatives were synthesized and characterized by (IR, 1H NMR, 13C NMR and Mass spectral) studies. All the synthesized compounds were evaluated for their antimicrobial activity by broth dilution method against two Gram positive strains (Bacillus subtilis and Staphylococcus aureus), two Gram negative strains (Pseudomonas aeruginosa and Escherichia coli) and fungal strain (Candida albicans and Aspergillus niger). The minimum inhibitory concentration of the compounds was in the range of 1.56-50 ?g ml-1 against bacterial and fungal strain. The results revealed that all synthesized compounds have a significant biological activity against the tested microorganisms. Among the synthesized derivatives 4g, 4h, 4m and 4p were found to be most effective antimicrobial compounds.

scholarly journals Synthesis and Antimicrobial Evaluations of Sulfur Inserted Fluoro-Benzimidazoles

2021 ◽  
Vol 33 (7) ◽  
pp. 1525-1529
Author(s):  
Parmesh Kumar Dwivedi ◽  
Devdutt Chaturvedi
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Strains ◽  
Substituted Anilines ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
New Compounds ◽  
Derivatives Of ◽  
Multiple Step

A new series of fluorinated sulfur inserted benzimidazole analogues Za-i were synthesized and characterized. The new compounds were screened for their antimicrobial and antioxidant potential. The synthesized compounds were obtained by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol X. The compounds Ya-i prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF. Finally, the compound X was reacted with different derivatives of 2-chloro-N-phenylacetamide resulting in formation of titled compounds Za-i. The synthesized compounds (Za-Zi) were characterized by spectral analysis viz.1H & 13C NMR, mass spectra, elemental analysis and IR. The in vitro antimicrobial potential against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans) was recorded for the obtained compounds. Some of the compounds exhibited encouraging results (in MIC) against Gram-positive and Gram-negative bacterial strains. These studies thus suggest that the designed sulfur inserted fluoro-benzimidazoles scaffold may serve as new promising template for further amplification as antimicrobial agents.

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