Synthesis and in vitro antimicrobial activity of new 3-(2-morpholinoquinolin-3-yl) substituted acrylonitrile and propanenitrile derivatives

2011 ◽  
Vol 65 (5) ◽  
Author(s):  
Jigar Makawana ◽  
Manish Patel ◽  
Ranjan Patel
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Double Bond ◽  
Fungal Pathogen ◽  
Condensation Reaction ◽  
Clostridium Tetani ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi

AbstractA series of new 3-(2-morpholinoquinolin-3-yl)acrylonitrile derivatives (IVa-IVf) has been synthesised by the base-catalysed condensation reaction of 2-morpholinoqionoline-3-carboxaldehydes (IIa-IIc) and 2-cyanomethylbenzimidazoles (IIIa-IIIb). Subsequent regiospecific reduction of the C—C double bond in acrylonitrile moiety afforded 3-(2-morpholinoquinolin-3-yl)propanenitrile derivatives (Va-Vf). All the compounds synthesised were subjected to in vitro antimicrobial screening against some representatives of bacteria and fungi. The majority of the compounds were found to be active against Gram-positive bacteria Bacillus subtilis and Clostridium tetani as well as against the fungal pathogen Candida albicans.

Antimicrobial Activity of Extracts of the Lichen Xanthoparmelia pokornyi and its Gyrophoric and Stenosporic Acid Constituents

2006 ◽  
Vol 61 (5-6) ◽  
pp. 319-323 ◽  
Author(s):  
Mehmet Candan ◽  
Meral Yılmaz ◽  
Turgay Tay ◽  
Merih Kıvança ◽  
Hayrettin Türk
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Aeromonas Hydrophila ◽  
Candida Glabrata ◽  
Proteus Vulgaris ◽  
Ethanol Extracts ◽  
Bacteria And Fungi ◽  
Gyrophoric Acid

The antimicrobial activity of the diethyl ether, acetone, chloroform, petroleum ether, and ethanol extracts of the lichen Xanthoparmelia pokornyi and its gyrophoric acid and stenosporic acid constituents has been screened against some foodborne bacteria and fungi. Both the extracts and the acids showed antimicrobial activity against Aeromonas hydrophila, Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Proteus vulgaris, Staphylococcus aureus, Streptococcus faecalis, Yersinia enterocolitica, Candida albicans and Candida glabrata. The extracts were inactive against the tested filamentous fungi. The MIC values of the extracts and the acids for the bacteria have also been determined.

scholarly journals Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu
Keyword(s):  
Biological Activities ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
C Nmr

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).

scholarly journals Microwave assisted synthesis of novel 4h-chromene derivatives bearing phenoxypyrazole and their antimicrobial activity assess

2012 ◽  
Vol 77 (9) ◽  
pp. 1165-1174 ◽  
Author(s):  
Chetan Sangani ◽  
Nimesh Shah ◽  
Manish Patel ◽  
Ranjan Patel
Keyword(s):  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Inhibitory Concentration ◽  
Salmonella Typhi ◽  
Microwave Assisted Synthesis ◽  
Gram Negative Bacteria ◽  
Clostridium Tetani ◽  
Gram Positive Bacteria ◽  
Concentration Method ◽  
Mic Minimum Inhibitory Concentration

A new series of 4H-chromene derivatives 4(a-p) bearing 5-phenoxypyrazole nucleus has been synthesized under microwave irradiation by reaction of 5-phenoxypyrazole-4-carbaldehyde 1(a-h), malononitrile 2 and compounds (Cyclohexanedione, Dimedon) 3(a-b) in presence of NaOH as basic catalyst. All the compounds were screened against three Gram positive bacteria (Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis), three Gram negative bacteria (Salmonella typhi, Vibrio cholerae, Escherichia coli) and two fungi (Aspergillus fumigatus, Candida albicans) using broth microdilution MIC (Minimum Inhibitory Concentration) method. Upon study of antimicrobial screening, it has been observed that, majority of the compounds were found to be active against Clostridium tetani and Bacillus subtilis as well as against Candida albicans as compared to standard drugs.

Synthesis and Structural Elucidation of Aminoacetylenic Derivatives of 7-Methoxy- 2-Naphthole as Antimicrobial Agents

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Abu- Safieh Rana ◽  
Muhi- Eldeen Zuhair ◽  
Alsarahni Aseel ◽  
Al-Kaissi Elham
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Naphthalene Derivatives ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi ◽  
Aminoacetylenic Derivatives ◽  
Derivatives Of ◽  
Mic Value

A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 µg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 µg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125µg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 µg/ml, all compounds have the same MIC value against P. aeruginosa (125 µg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 µg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi.

scholarly journals Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity

2008 ◽  
Vol 58 (1) ◽  
pp. 29-42 ◽  
Author(s):  
Rafat Mohareb ◽  
Hanaa Hana
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Dimethyl Acetal ◽  
Dimethyl Formamide ◽  
Gram Positive Bacteria ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Potential Antimicrobial Activity

Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. Thein vitroantimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.

scholarly journals Synthesis and Preliminary Biological Activity Evaluation of New N- Substituted Phthalimide Derivatives

2020 ◽  
Vol 29 (1) ◽  
pp. 247-252
Author(s):  
Halah A. Sahib ◽  
Mohammed H. Mohammed
Keyword(s):  
Antimicrobial Activity ◽  
Methyl Ester ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Phenylalanine Methyl Ester

A A new series of bases of Schiff (H2-H4) derived from phthalic anhydrideweresynthesized. These Schiff bases were prepared by the reaction of different amines (tyrosine methyl ester, phenylalanine methyl ester, and isoniazid) with the phthalimide derived aldehyde with the aid of glacial acetic acid or triethylamine ascatalysts. All the synthesized compounds were characterized by (FT-IR and 1HNMR) analyses and were in vitro evaluated for their antimicrobial activity against six various kinds of microorganisms. All the synthesized compounds had been screened for their antimicrobial activity against two Gram-positive bacteria “Staph. Aureus, and Bacillus subtilis”, two Gram-negative bacteria “Escherichia coli, and Klebsiella pneumoniae”, and two fungi species “Candida tropicalis and Candida albicans” using concentrations of 62.5, 125 and 250 µg\mLof derivative in dimethyl sulfoxide(DMSO). All the synthesized compounds showed no activity at all against Gram-positive bacteria, for Gram-negative bacteria and fungi they showed moderate or no activity except compound H1revealedhigh antifungal activityagainstCandida tropicalisat concentrations 125 and 250 µg\ mL. Keywords: Schiff base, phthalic anhydride, antimicrobial.  

scholarly journals In vitro antimicrobial activity of Caesalpinia coriaria (Jacq.) Willd extracts on Streptococcus pyogenes and Candida albicans

Revista Vitae ◽  
2021 ◽  
Vol 28 (2) ◽  
Author(s):  
Silvio Alejandro Lopez-Pazos ◽  
Leanis Pitre-Ruiz ◽  
Deycis Galván-Ayala ◽  
Kelly Johanna Ávila Mendez ◽  
Omar Castro-Uriana
Keyword(s):  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Streptococcus Pyogenes ◽  
Ethanolic Extract ◽  
Antimicrobial Effect ◽  
Inhibitory Effect ◽  
Bioactive Metabolites ◽  
Soxhlet Method ◽  
Bacteria And Fungi

Background: “Dividivi” Caesalpinia coriaria (Jacq.) Willd fruits are traditionally used by the Wayuú community in La Guajira (Colombia) to treat oral and skin cavity diseases caused by bacteria and fungi. Streptococcus pyogenes is a gram-positive cocci of group A (beta-hemolytic) that is the cause of pharyngeal disease, scarlet fever, cellulitis, erysipelas, or toxic shock-like syndrome. Alternatively, Candida albicans is a yeast-like fungus that is a normal flora of the digestive tract, vagina, or skin folds; it has been known to be the root cause of opportunistic diseases such as diaper rash, oral and esophagus thrush, or vulvovaginitis. Objective: This study evaluated the antimicrobial activity of methanolic and ethanolic extracts of C. coriaria (Jacq.) Willd dry fruits on S. pyogenes ATCC 12384 and C. albicans ATTC 14053. Method: C. coriaria extracts were obtained from the Soxhlet method using two solvents (methanol and ethanol 98%) prepared from pulverized fruits. A phytochemical test and an antimicrobial activity assay were performed using the obtained extracts and tested using S. pyogenes ATCC 12384 and C. albicans ATTC 14053 strains. Results: A phytochemical profile was performed, examining the presence of bioactive metabolites (tannins, alkaloids, glycosides, saponins, and anthraquinones) from each extract. Antimicrobial susceptibility tests showed that the ethanolic extract inhibited S. pyogenes ATCC 12384, causing inhibition halos of 14.1 ± 0.1 mm and a Minimum Inhibitory Concentration (MIC) of 172 mg/ml, and C. albicans test shows inhibition halos of 16.1 ± 0.2 mm and MIC of 212 mg/ml. Additionally, the methanolic extract inhibited S. pyogenes with inhibition halos of 15.2 ± 0.2 mm and MIC of 152 mg/ml; no inhibitory effect was observed on C. albicans. Conclusion: This study revealed that C. coriaria has an antimicrobial effect on the tested species opening the field of its possible use as a therapeutic agent.

SYNTHESIS OF NOVEL BENZOTRIAZOLYL FORMAZANS AND THEIR ANTIMICROBIAL AND ANTIOXIDANT ACTIVITY

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (11) ◽  
pp. 29-33
Author(s):  
S George ◽  
◽  
R. Chakraborty ◽  
F. Saleshier ◽  
T.K. Ravi
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Diazonium Salt ◽  
Aromatic Aldehydes ◽  
Bacterial Strains ◽  
Mass Spectral ◽  
Antimicrobial And Antioxidant Activity

Benzotriazolyl hydrazide (2) has been obtained from the ester ethyl benzotriazolyl acetate (1). The hydrazide with various aromatic aldehydes in presence of glacial acetic acid gave corresponding arylidenes 3(a-h). The arylidenes were made to react with fluoro substituted diazonium salt whereby, benzotriazolyl formazans 4(a-h) were obtained. The structures of the compounds were confirmed by FTIR, 1 H-NMR, mass spectral data and elemental analysis. All the synthesized compounds were screened for their in-vitro antimicrobial activity against the bacterial strains Bacillus subtilis and Escherichia coli and the fungal strains Asperigillus niger and Candida albicans by two fold serial dilution technique and also for their antioxidant activity. Among the compounds tested, compound 4b (fluoro substituted derivative) showed MIC as low as 15.6 µg/mL against Bacillus subtilis and Candida albicans. Other derivatives also showed moderate antimicrobial activity. Also, compound 4e (methoxy substituted derivative) showed significant antioxidant activity when compared to the standard, ascorbic acid.

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.

Synthesis and Biological Activities of Chalcones Derived from Nitroacetophenone

2012 ◽  
Vol 518-523 ◽  
pp. 255-260 ◽  
Author(s):  
Xiao Yang Qiu ◽  
Su Zhi Li ◽  
An Ran Shi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Trichophyton Rubrum ◽  
Biological Activities ◽  
Tumor Cell Line ◽  
And Staphylococcus Aureus

A series of nitrochalcones (compounds 1-10) were synthesized by reacting appropriate nitroacetophenones and suitable benzaldehydes. The synthesized products were evaluated for their cytotoxic, antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus) and antifungal (Aspergillus niger, Candida albicans and Trichophyton rubrum) activities in vitro. Among the compounds tested, (E)-3-(4-fluorophenyl)-1-(3-nitrophenyl)- prop-2-en-1-one (10) showed the favorable in vitro cytotoxic activity against human nasopharyngeal epidermoid tumor cell line KB, and (E)-3-(2-methoxyphenyl)-1-(3-nitrophenyl)prop-2-en-1-one (8) showed the strongest antimicrobial activity with MIC of 20 μg/mL against P. fluorescence.

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