Molecular Drug Design, Synthesis and Antibacterial study of Novel 4-Oxothiazolidin-3-yl Derivatives

2020 ◽  
pp. 1-10
Keyword(s):  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Docking Simulations ◽  
Chemical Structures ◽  
Molecular Core ◽  
Diffusion Technique

New compounds containing 4-thiazolidinone pharmacophore 5(a) and (5b) have been synthesized. The chemical structures of the intermediate and final compounds were characterized and confirmed by using FT-IR and 1H-NMR spectroscopy. All final compounds were tested against gram-positive and gram-negative bacteria using a well-diffusion technique for their ability as antimicrobial agents. The tested compounds 5a and 5b showed variable and modest antibacterial activity against gram-negative bacteria and gram-positive bacteria. Molecular docking simulations were studied to understand the molecular core. The results were achieved by docking, the most active compounds into the active site of protein of the bacteria which completely accorded with in vitro results.

scholarly journals Design, Synthesis and Evaluation of Schiff’s Bases of 4-Chloro-3-coumarin aldehyde as Antimicrobial Agents

2009 ◽  
Vol 6 (3) ◽  
pp. 759-762 ◽  
Author(s):  
Shriram Bairagi ◽  
Ashok Bhosale ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

4-Chloro-2-oxo-2H-chromene-3-carbaldehyde(2)was reacted with different anilines in rectified spirit as solvent to yield a series of the title compoundsi.e. 4-chloro-3-((substituted-phenylimino) methyl)-2H-chromen-2-one(3a-i). These compounds were charaterised on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive and gram negative bacteria and fungi. Compound3Cwas found to be most active with an MIC of 15 μg /mL against all the tested organisms.

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.

In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives

Chemotherapy ◽  
2017 ◽  
Vol 62 (3) ◽  
pp. 194-198 ◽  
Author(s):  
Socorro Leyva-Ramos ◽  
Denisse de Loera ◽  
Jaime Cardoso-Ortiz
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
New Drugs ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Topoisomerase Iv ◽  
Gram Positive ◽  
Disk Diffusion Method ◽  
Gram Negative

Background: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. Methods: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. Results: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. Conclusion: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound.

scholarly journals In Vitro, Controlling the Establishment of Xanthomonas Campestris with different Bacterial Bioagents

2016 ◽  
Vol 29 (1) ◽  
pp. 37-40
Author(s):  
Amna Ali ◽  
M Saleem Haider ◽  
Sobia Mushtaq ◽  
Ibatsam Khokhar ◽  
Irum Mukhtar ◽  
...  
Keyword(s):  
Xanthomonas Campestris ◽  
Fruits And Vegetables ◽  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Diffusion Technique

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

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 ANTIMICROBIAL ACTIVITY OF A PROTEASE INHIBITOR ISOLATED FROM THE RHIZOME OF CURCUMA AMADA

2017 ◽  
Vol 10 (9) ◽  
pp. 131 ◽  
Author(s):  
Sangeetha R ◽  
Padmini R
Keyword(s):  
Protease Inhibitor ◽  
Antimicrobial Agents ◽  
Gel Permeation Chromatography ◽  
Membrane Disruption ◽  
Minimal Bactericidal Concentration ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Curcuma Amada

  Objective: Protease inhibitors (PIs) are effective antimicrobial agents, and this study was aimed to study the antibacterial efficacy of a PI isolated from the rhizome of Curcuma amada.Methods: A proteinaceous protease inhibitor was isolated from the rhizome of C. amada and purified by Sephadex G-50 gel permeation chromatography. The purified inhibitor was denoted as Curcuma amada protease inhibitor (CAPI). The antibacterial effect of CAPI against Gram-positive and Gram-negative bacteria, the minimal inhibitory concentration (MIC), and minimal bactericidal concentration (MBC) of CAPI was studied in vitro, and the membrane disruption activity of CAPI was also analyzed.Results: CAPI was effective against both Gram-positive and Gram-negative bacteria, with slightly higher concentrations required for Gram-negative bacteria. The MIC ranged from 75 to 100 μg/ml and the MBC ranged from 100 to 125 μg/ml of CAPI. The study of membrane disruption by CAPI revealed the release of cell contents, namely, reducing sugars and proteins from the bacterial cell.Conclusion: A PI was effectively isolated from the rhizome of C. amada, and the isolated inhibitor proved to be a promising antibacterial agent.

scholarly journals Synthesis and Evaluation of Some Coumarin Containing Potential Antimicrobial Agents

2012 ◽  
Vol 9 (4) ◽  
pp. 2493-2500
Author(s):  
Sayali D. Kudale ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Schiff’S Bases ◽  
Gram Positive ◽  
Gram Negative ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the Schiff’s bases incorporating coumarin and chalcone moeities, 3-(4-(4-(substituted phenyl)prop-1-ene-3-one) phenylimino) methyl)-4-chloro-2h-chromen-2-one 4(a-g) were synthesized as potential antimicrobial agents. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activity in vitro against gram positive and gram negative bacteria and fungi. Compound 4b was found to be most active with an MIC of 20 µg/mL against all the tested organisms.

scholarly journals Synthesis, Characterisation and Biological Evaluation of Substituted 4- ((1H-Benzo[d]Imidazol-2-YL) Methoxy) Coumarin Derivatives as Antimicrobial Agents

2019 ◽  
Vol 7 (02) ◽  
pp. 01-08
Author(s):  
Harpreet Kaur ◽  
Baljeet Singh
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
Gram Negative Bacteria ◽  
Coumarin Derivatives ◽  
Gram Positive ◽  
Standard Drug ◽  
Gram Negative

A series of coumarin-benzimidazole derivatives i.e. 4-((1H-Benzo[d]imidazol-2- yl)methoxy)coumarin derivatives (7a-j) was synthesized by reacting appropriate starting materials and evaluated for its in vitro antimicrobial activity. The newly synthesized compounds have been characterized on the basis of elemental analyses, spectroscopic techniques (FT-IR). Antimicrobial studies of these compounds were performed against the both the Gram positive, MRSA (Staphylococcus aureus, Bacillus subtilis) as well as Gram negative (Escherichia coli) bacteria. The activity was investigated by using both Agar well diffusion as well as MIC assay. All the compounds were show significant bactericidal activity against all the pathogenic strains in comparison to Ciprofloxacin, a broad spectrum antibiotic against Gram positive and Gram negative bacteria. Most of the synthesized derivatives appeared as excellent antimicrobial agents as compared to standard drug Ciprofloxacin. Compound 7b was found to be the most active antibacterial agent against Gram positive as well as Gram negative bacteria.

Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

2015 ◽  
Vol 69 (8) ◽  
Author(s):  
Martin Krátký ◽  
Jana Mandíková ◽  
František Trejtnar ◽  
Vladimír Buchta ◽  
Jiřina Stolaříková ◽  
...  
Keyword(s):  
Fungal Pathogens ◽  
Antimicrobial Agents ◽  
Oxalyl Chloride ◽  
Atypical Mycobacteria ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Urea Derivatives ◽  
Gram Negative ◽  
Gram Positive Bacteria

AbstractProgression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine- 2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 μM and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)- N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 μM, and with acceptable toxicity (selectivity indices for M. avium and M. kansasii higher than 16 and 62.5, respectively). Gram-positive bacteria, including methicillinresistant Staphylococcus aureus, were inhibited at concentrations starting from 125 μM, whereas the investigated derivatives exhibited almost no antifungal potency and activity against gram-negative species.

scholarly journals Synthesis and Evaluation of Some Coumarin Based Schiff's Bases as Potential Antimicrobial Agents'

2012 ◽  
Vol 9 (4) ◽  
pp. 2079-2088 ◽  
Author(s):  
Vishakha Bansode ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the title compounds 3-(4-(4, 5-dihydro-5-(substituted phenyl)-1H-3-pyrazolyl) phenylimino) methyl)-4-chloro-2H-chromen-2-one 5(a-g) have been synthesized. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive bacteria, gram negative bacteria and fungi. The compound (5b) was found to be the most active with MIC of 20 µg/ml against all the tested organisms.

Sign in / Sign up

Export Citation Format

Share Document