Synthesis of novel pyridine-connected piperidine and 2H-thiopyran derivatives and their larvicidal, nematicidal, and antimicrobial activities

A series of novelpyridine-connected piperidine derivatives (2a-g) and pyridine-connected 2H-thiopyran derivatives (4a-g) were synthesized and screened for larvicidal, nematicidal, and antimicrobial activities. Compound 4e exhibited larvicidal activity against second instar larvae with an LD50 value of 0.8μg/mL. In addition, 4e exhibited high nematicidal activity, with an LD50 value of 3.2μg/mL.Compounds 2e (MIC: 4 μg/mL) and 2d (MIC: 4 μg/mL) exhibited high antibacterial activity against Klebsiella pneumoniae and Escherichia coli, respectively. Compounds 4b (MIC: 0.25 μg/mL) and 4f (MIC: 2 μg/mL) showed high antifungal activity against Candida albicans and Microsporum audouinii, respectively. Therefore, it can be suggested that compounds 2e, 2d, 4e, 4b, and 4f may be useful as lead molecules for the development of new classes ofdrugs with larvicidal,nematicidal,and antimicrobial activities.

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Synthesis and Antimicrobial Screening of Some Novel 5-Substituted-1,10b-dihydroimidazole[1,2-c]quinazoline Derivatives

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.2.6 ◽

2021 ◽

Vol 14 (2) ◽

pp. 5406-5411

Author(s):

Haribhai Rabari ◽

Hetal Vankar ◽

Beenkumar Prajapati

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Candida Albicans ◽

Antifungal Activity ◽

Aspergillus Niger ◽

Antifungal Compound ◽

Bacterial Strains ◽

Standard Drug ◽

Quinazoline Derivatives

The emergence of multidrug microbial resistance is the main challenges that the modern scientists have so far been facing in the recent era. In this respect, new series of drug classes having potential to give antimicrobial effect have been synthesized. A new series of 5- substituted-1,10 b-dihydroimidazole[1,2-c]quinazoline derivatives 8a-e have been synthesized and screened for antibacterial activity and antifungal activity. Synthesized derivatives were characterized by IR, MASS and 1H-NMR spectroscopy. Synthesized compounds show good activity, which was comparable to the standard drug and it can be useful for the further clinical study. Antibacterial activity was evaluated against four different pathogenic bacterial strains like Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudo-monas aeruginosa. Among the screened compounds, 8e show good antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC of 50 and 100 μg/ml respectively. Antifungal activity was evaluated against two strains of fungi. Among the synthesized derivates, compound 8c was emerged out as the potent antifungal compound against Candida albicans and Aspergillus niger with MIC of 25 μg/ml and 75μg/ml respectively. Compound 8e also shows good antifungal activity with MIC of 50 μg/ml against both Candida albicans and Aspergillus niger. The overall results of this study indicated that synthesized quinazoline derivatives had the potential to act as an antibacterial and antifungal agent, hence further investigation is warranted.

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In-Vitro Evaluation of Antimicrobial Activities of Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Neisseria gonorrhoeae, and Candida albicans Nosodes

Homeopathy ◽

10.1055/s-0041-1727149 ◽

2021 ◽

Author(s):

Renuka Munshi ◽

Gitanjali Talele ◽

Rajesh Shah

Keyword(s):

Escherichia Coli ◽

Candida Albicans ◽

Klebsiella Pneumoniae ◽

Neisseria Gonorrhoeae ◽

Salmonella Typhi ◽

Antimicrobial Activities ◽

Positive Control ◽

E Coli ◽

Inhibition Of Growth

Abstract Background This study presents the results of the minimum inhibitory concentration (MIC) assay of a series of nosodes: namely Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Neisseria gonorrhoeae, and Candida albicans. Each was tested against its corresponding infection as well as cross infections. Methods In-vitro efficacy of polyvalent nosodes was tested using the MIC assay technique. The nosodes, namely C. albicans polyvalent nosode (35c, 100c), N. gonorrhoeae (35c), K. pneumoniae (35c, 100c), E. coli polyvalent nosode (35c, 100c) and Salmonella typhi polyvalent nosode (30c, 100c), were tested along with positive and negative controls. Nosodes were studied in different potencies and at 1:1 dilution. Results C. albicans polyvalent nosode 35c, 100c, N. gonorrhoeae 35c, and positive control amphotericin B showed inhibition of the growth of C. albicans species. K. pneumoniae 35c, E. coli polyvalent nosode 100c, and meropenem (positive control) showed inhibition of the growth of K. pneumoniae; this effect was not seen with ceftriaxone, ofloxacin and amoxicillin antibiotics. E. coli polyvalent nosode 30c in 10% alcohol (direct and dilution 1:1) and the positive controls ciprofloxacin, ofloxacin, and amoxicillin showed inhibition of the growth of E. coli. The S. typhi polyvalent nosode 30c in 10% alcohol showed inhibition of growth of S. typhi. Conclusion This study reveals that the tested nosodes exhibited antibacterial potential against the corresponding micro-organisms and against other selected organisms studied using this assay.

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The Antimicrobial Activity of Extracts of the Lichen Hypogymnia tubulosa and Its 3-Hydroxyphysodic Acid Constituent

Zeitschrift für Naturforschung C ◽

10.1515/znc-2005-1-207 ◽

2005 ◽

Vol 60 (1-2) ◽

pp. 35-38 ◽

Cited By ~ 16

Author(s):

Meral Yılmaz ◽

Turgay Tay ◽

Merih Kıvanç ◽

Hayrettin Türk ◽

Ayşen Özdemir Türk

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Bacillus Subtilis ◽

Candida Albicans ◽

Antifungal Activity ◽

Klebsiella Pneumoniae ◽

Aeromonas Hydrophila ◽

Proteus Vulgaris ◽

Ethanol Extracts

The antimicrobial activity and the MIC values of the diethyl ether, acetone, chloroform, petroleum ether, and ethanol extracts of the lichen Hypogymnia tubulosa and its 3-hydroxyphysodic acid constituent have been investigated against some microorganisms. At least one of the extracts or 3-hydroxyphysodic acid showed antimicrobial activity against Aeromonas hydrophila, Bacillus cereus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Listeria monocytogenes, Proteus vulgaris, Salmonella typhimurium, Staphylococcus aureus, Streptococcus faecalis, and Candida albicans. No antifungal activity of the extracts has been observed against ten filamentous fungi.

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Antimicrobial Activities of LL-37 Fragment Mutant-Poly (Lactic-Co-Glycolic) Acid Conjugate against Staphylococcus aureus, Escherichia coli, and Candida albicans

International Journal of Molecular Sciences ◽

10.3390/ijms22105097 ◽

2021 ◽

Vol 22 (10) ◽

pp. 5097

Author(s):

Takeshi Mori ◽

Miyako Yoshida ◽

Mai Hazekawa ◽

Daisuke Ishibashi ◽

Yoshiro Hatanaka ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Candida Albicans ◽

Antifungal Activity ◽

Glycolic Acid ◽

Critical Micellar Concentration ◽

Antibacterial Activities ◽

Antimicrobial Activities ◽

Transmission Electron ◽

Acid Conjugate

Various peptides and their derivatives have been reported to exhibit antimicrobial activities. Although these activities have been examined against microorganisms, novel methods have recently emerged for conjugation of the biomaterials to improve their activities. Here, we prepared CKR12-PLGA, in which CKR12 (a mutated fragment of human cathelicidin peptide, LL-37) was conjugated with poly (lactic-co-glycolic) acid (PLGA), and compared the antimicrobial and antifungal activities of the conjugated peptide with those of FK13 (a small fragment of LL-37) and CKR12 alone. The prepared CKR12-PLGA was characterized by dynamic light scattering and measurement of the zeta potential, critical micellar concentration, and antimicrobial activities of the fragments and conjugate. Although CKR12 showed higher antibacterial activities than FK13 against Staphylococcus aureus and Escherichia coli, the antifungal activity of CKR12 was lower than that of FK13. CKR12-PLGA showed higher antibacterial activities against S. aureus and E. coli and higher antifungal activity against Candida albicans compared to those of FK13. Additionally, CKR12-PLGA showed no hemolytic activity in erythrocytes, and scanning and transmission electron microscopy suggested that CKR12-PLGA killed and disrupted the surface structure of microbial cells. Conjugation of antimicrobial peptide fragment analogues was a successful approach for obtaining increased microbial activity with minimized cytotoxicity.

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Evaluation of Antibacterial and Antifungal Activity of Herbs Used in Treatment of Diabetes, Malaria and Pneumonia in Kisii and Nyamira Counties Region, Kenya

Journal Of Tropical Pharmacy And Chemistry ◽

10.25026/jtpc.v5i4.314 ◽

2021 ◽

Vol 5 (4) ◽

pp. 330-337

Author(s):

Moses A. Guto Maobe ◽

Leonard Gitu ◽

Erastus Gatebe

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Candida Albicans ◽

Antifungal Activity ◽

Diffusion Method ◽

Root Extract ◽

Plant Parts ◽

Toddalia Asiatica ◽

Antibacterial And Antifungal

The herbs Carissa spinarum, Physalis minima and Toddalia asiatica have traditionally been used in healing diabetes, malaria and pneumonia by the communities around the Kisii region, Kenya. However in the available literature, there is scanty information on effectiveness of different plant parts of the herbs in healing the ailments. The objective of this study was to investigate the potential antimicrobial and antifungal activity of methanolic extract of whole plant Physalis minima, leaf and root of Carissa spinarum and Toddalia asiatica against gram positive bacteria Staphylococcus aureus (ATCC 25923), gram negative bacteria Escherichia coli (ATCC 25922) and fungus Candida albicans (ATCC14053). Antibiotic disc methicillin, cotrimoxazole, chloramphenicol, gentamicin, ampicillin, nalidixic and nitrofurantoin were used in the study. In each herb, plant part was extracted by soaking in methanol/dichloromethane in ratio 1:1 for a week, filtered, concentrated by rotary vapor and cooled. The same process was repeated three times for all samples. The study was conducted by agar well diffusion method. Methanolic root extract of Toddalia asiatica showed highest antibacterial activity against Staphylococcus aureus (ATCC 25923), root extract of Carissa spinarum had highest antibacterial activity against Escherichia coli (ATCC 25922) while root extract of Toddalia asiatica showed highest antifungal activity. It was concluded that root extract of Toddalia asiatica showed highest antibacterial activity 16.7mm against Staphylococcus aureus(ATCC 25923), root extract of Carissa spinarum had highest antibacterial activity 10 mm against Escherichia coli (ATCC 25922) while root extract of Toddalia asiatica had highest antifungal activity 18 mm against Candida albicans.

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Comparison of Antimicrobial Activity ofAllium sativumCloves from China and Taşköprü, Turkey

Advances in Pharmacological Sciences ◽

10.1155/2018/9302840 ◽

2018 ◽

Vol 2018 ◽

pp. 1-5 ◽

Cited By ~ 4

Author(s):

Ali Yetgin ◽

Kerem Canlı ◽

Ergin Murat Altuner

Keyword(s):

Antimicrobial Activity ◽

Antibacterial Activity ◽

Candida Albicans ◽

Antifungal Activity ◽

Allium Sativum ◽

Antimicrobial Activities ◽

Diffusion Method ◽

Disk Diffusion Method ◽

Gram Negative ◽

Gram Positive Bacteria

In this study, antimicrobial activities of two different samples ofAllium sativumL. from Turkey (TR) (Taşköprü, Kastamonu, Turkey) and China (CN) were determined. A broad spectrum of Gram-negative and Gram-positive bacteria (17 bacteria) including species ofBacillus,Enterobacter,Enterococcus,Escherichia,Klebsiella,Listeria,Pseudomonas,Salmonella, andStaphylococcuswere used for testing antibacterial activity. In addition, antifungal activity againstCandida albicanswas also investigated. Antimicrobial activity was tested by using 3 different processes (chopping, freezing, and slicing by the disk diffusion method). The results showed that TR garlic presented more antimicrobial activity than CN garlic. Mechanism of activity of CN garlic could be proposed to be different from that of TR garlic.

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SYNTHESIS AND ANTIMICROBIAL ACTIVITIES OF SOME NEW 1, 3, 4-OXADIAZOLES

INDIAN DRUGS ◽

10.53879/id.49.08.p0038 ◽

2012 ◽

Vol 49 (08) ◽

pp. 38-44

Author(s):

S Desai ◽

◽

U. Laddi

Keyword(s):

Escherichia Coli ◽

Antibacterial Activity ◽

Antifungal Activity ◽

Aspergillus Niger ◽

Spectral Data ◽

Elemental Analysis ◽

Antimicrobial Activities ◽

Side Chain ◽

Moderate Activity ◽

Colletotrichum Capsici

Various 5-β-[(N-Benzenesulphonyl/tosyl)-4-(un) substituted anilino] ethyl-2-H/CH3/C6H5/-CH2C6H5/p-NO2C6H4-1,3,4-oxadiazoles (5a-d), 5--β-[(N-Benzenesulphonyl/tosyl)-4-(un)-substituted anilino] ethyl-2-(N,N-diethylamino/anilino/morpholino)-1, 3, 4-oxadiazoles (6a-r), 3--β-[(N-Benzenesulphonyl/tosyl)-4-(un) substituted anilino] ethyl-4-amino-5-mercapto-4(H)-1, 2, 4-triazoles (7a-f) and 5--β-[(N-Benzenesulphonyl/tosyl)-4-(un)substituted anilino] ethyl-3-(p-toluidino) methyl-1, 3, 4-oxadiazole-2-thiones (8a-f) with sulphonamide moiety at the side chain were synthesised. The structures of the newly synthesised compounds were established on the basis of their spectral data and elemental analysis. All the compounds were screened for antimicrobial activities against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger, Colletotrichum capsici. Most of the compounds have exhibited significant antifungal activity against Colletotrichum capsici, moderate activity against Aspergillus niger and minimum antibacterial activity against both the strains.

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ANTIBACTERIAL ACTIVITY OF DIFFERENT EXTRACTS OF BLACK MUSSEL (MYTILUS GALLOPROVINCIALIS) FROM THE BLACK SEA, BULGARIA

Journal of IMAB - Annual Proceeding (Scientific Papers) ◽

10.5272/jimab.2021271.3506 ◽

2021 ◽

Vol 27 (1) ◽

pp. 3506-3509

Author(s):

Gabriela Tsankova ◽

◽

Tatina Todorova ◽

Neli Ermenlieva ◽

Albena Merdzhanova ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Klebsiella Pneumoniae ◽

Black Sea ◽

Mytilus Galloprovincialis ◽

Antimicrobial Activities ◽

Diffusion Method ◽

The Black Sea ◽

Glycerol Water

Background: Over the past decade, there has been a growing interest in sea bivalves, which are an inexpensive and easily accessible source of high-quality proteins, lipids and secondary metabolites with antimicrobial and anti-fungal potential. Farmed Black Sea mussel (M. galloprovincialis) are promising objects for the study of their antimicrobial potential. Purpose: The aim of this work is to determine the antibacterial activity of different extracts from the Black Sea mussel Mytilus galloprovincialis tissues by using the disc diffusion method with cultures of Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae. Material/Methods: Extraction of mussel tissues was done with different solvents: ethyl acetate (100%), methanol (100%), glycerol:water (50%, 1:1 v/v), ethanol (50%), acetone (70%), hot water. Antimicrobial activities of these extracts from Mytilus galloprovincialis was assessed by the disc-diffusion method. Results: Testing antibacterial activity of black mussels revealed that ethyl acetate extract showed the highest activity against Еscherichia coli (13 mm) and Klebsiella pneumoniae (11 mm) and no activity against Staphilococcus aureus. The glycerol: water extract showed growth inhibition effect against Staphylococcus aureus (11 mm) and Escherichia coli (10 mm), but no effect against Klebsiella pneumoniae. Conclusions: The preliminary information presented in this study showed that the Black Sea farmed mussel could be an interesting source of antibacterial compounds. The glycerol-water extracts of Mytilus galloprovincialis had low antimicrobial activities against Staphylococcus aureus and more important against Escherichia coli.

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Antimicrobial Activity of Copper(II) and Cobalt(II) Complexes of Citral-Valine Derived Schiff Base

Asian Journal of Chemistry ◽

10.14233/ajchem.2020.21801 ◽

2019 ◽

Vol 32 (1) ◽

pp. 192-194

Author(s):

S. Sudha Kumari

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Schiff Base ◽

Candida Albicans ◽

Schiff Base Ligand ◽

Antimicrobial Activities ◽

Bacterial Strains ◽

Gram Negative

In present work, the screening of antimicrobial activities of copper(II) and cobalt(II) complexes with Schiff base ligand derived from the condensation of citral with valine (amino acid) was carried out on agar plates are reported. The antibacterial activity of Schiff base and its copper(II) and cobalt(II) complexes were evaluated against two bacterial strains Staphylococcus aureus (Gram-positive), Escherichia coli (Gram-negative) and fungus Candida albicans. The results revealed that the Schiff base ligand exhibited the poor antimicrobial activity against Escherichia coli and Candida albicans except for Staphylococcus aureus. Generally, Gram-negative bacteria shows rigid outer membrane, well enough to defend against the drug but Schiff base (citral with valine derived) impregnated cobalt(II) complex seem to be more active against Escherichia coli organisms in comparison to copper(II) complex, which exhibits higher activity than uncomplexed ligand. The antimicrobial results revealed that cobalt(II) and copper(II) complexes have a considerable antibacterial activity than antifungal activity and suggest their potential application as antibacterial agents.

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Novel Substituted Thiophenes and Sulf-Polyacetylene Ester from Echinops ritro L.

Molecules ◽

10.3390/molecules24040805 ◽

2019 ◽

Vol 24 (4) ◽

pp. 805 ◽

Cited By ~ 1

Author(s):

Liang-Bo Li ◽

Guang-Da Xiao ◽

Wei Xiang ◽

Xing Yang ◽

Ke-Xin Cao ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Candida Albicans ◽

Spectroscopic Analysis ◽

Inhibitory Concentration ◽

2D Nmr ◽

Antibacterial Activities ◽

Antimicrobial Activities ◽

Whole Plant

Three new substituted bithiophenes (1–3), and one new sulf-polyacetylene ester, ritroyne A (16) were isolated from the whole plant of Echinops ritro together with twelve known substituted thiophenes. The structures were elucidated on the basis of extensive spectroscopic analysis including 1D and 2D NMR as well as MS. Furthermore, the absolute configuration of ritroyne A (16) was established by computational methods. In bioscreening experiments, four compounds (2, 4, 12, 14) showed similar antibacterial activity against Staphylococcus aureus ATCC 2592 with levofloxacin (8 µg/mL). Five compounds (2, 4, 9, 12, 14) exhibited antibacterial activities against Escherichia coli ATCC 25922, with minimum inhibitory concentration (MIC) values of 32–64 µg/mL. Three compounds (2, 4, 12) exhibited antifungal activities against Candida albicans ATCC 2002 with MIC values of 32–64 µg/mL. However, compound 16 did not exhibit antimicrobial activities against three microorganisms.

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