scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIMICROBIAL SCREENING OF SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVES

2010 ◽  
Vol 18 (18) ◽  
pp. 11-18
Author(s):  
Anees A Siddiqui ◽  
Asif Husain ◽  
M Shaharyar ◽  
Mohd Rashid ◽  
Ravinesh Mishra ◽  
...  
Keyword(s):  
Aromatic Acids ◽  
E Coli ◽  
Phosphorous Oxychloride ◽  
Diffusion Technique ◽  
Oxadiazole Derivatives ◽  
Bacteria And Fungi ◽  
Hydroxy Quinoline ◽  
Different Strains ◽  
Antibacterial And Antifungal

1,3,4-oxadiazoles are important because of its versatile biological actions. In the present study, several 2-(quinoline-8-yloxymethyl)-5-aryl-1,3,4-oxadiazole derivates (IIIa-j) have been synthesized by the condensation of 8-hydroxy quinoline acetyl hydrazide (II) with various aromatic acids in presence of phosphorous oxychloride. The structures of the newly synthesized compounds have been established on the basis of elemental analysis, UV, IR, and 1H NMR spectral data. The synthesized compounds were screened for their in vitro growth-inhibiting activity against different strains of bacteria and fungi viz., S aureus, E. Coli, P. aeruginosa, C. Albicans, A. flavus, and A. fumigates, and the results were compared with the standard such as Ampicillin (50µg/ml) using agar diffusion technique. Compounds IIIc and IIIf were found to be equipotent as ampicillin when tested against the strains of E.Coli where as tested compounds IIIc, IIIf and IIIi showed good antibacterial and antifungal activity when tested against the strains of S. aureus, P. aeruginosa, and C. Albicans.

scholarly journals Studies of Biologically Active Heterocycles: Synthesis, Characterization and Antimicrobial Activity of Some 2,5-Disubstituted-1,3,4-Oxadiazoles

1970 ◽  
Vol 6 (2) ◽  
pp. 69-75 ◽  
Author(s):  
G Nagalakshmi
Keyword(s):  
Phosphorus Oxychloride ◽  
Biologically Active ◽  
Shigella Dysenteriae ◽  
Diffusion Method ◽  
Diffusion Technique ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi ◽  
Different Strains ◽  
Agar Well Diffusion Method

1,3,4-oxadiazoles are important because of its versatile biological actions. In the present study, several 2,5-disubstituted-1,3,4-oxadiazoles (3a-o) have been synthesized by the condensation of 4-hydroxybenzohydrazide (1) with various aromatic acids (2a-o) in presence of phosphorus oxychloride. The structures of the newly synthesized compounds have been established on the basis of elemental analysis, UV, IR and 1H NMR spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Staphylococcus aureus, Bacillus subtilis, Bacillus megaterium, Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Candida albicans, Aspergillus niger and Aspergillus flavus and the results were compared with the standard antibiotics such as chloramphenicol (50?g/ml) and Griseofulvin (50?g/ml) using agar diffusion technique. Compounds 3b, 3e, 3g, 3h, 3j, 3m and 3n exhibited strong antibacterial activity and compounds 3a, 3d, 3g, 3h and 3i showed good antifungal activity. Key words: 2,5-disubstituted-1,3,4-oxadiazoles, 4-hydroxybenzohydrazide, phosphorus oxychloride, antimicrobial evaluation, agar well diffusion method. Dhaka Univ. J. Pharm. Sci. 6(2): 69-75, 2007 (December)

scholarly journals Syntheses of 2-(6’-Fluorobenzothiazol-2’-ylamino)-4, 6-(disubstituted thiouriedo)-1,3-pyrimidine Derivatives as Antimicrobial Agents

2011 ◽  
Vol 8 (1) ◽  
pp. 240-244 ◽  
Author(s):  
Anoop K. Pathak ◽  
Viney Chawla ◽  
Shailendra K. Saraf
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Inhibiting Activity ◽  
Pyrimidine Derivatives ◽  
E Coli ◽  
Diffusion Technique ◽  
Nucleophilic Reagents ◽  
Different Strains ◽  
Growth Inhibiting

A new series of 1,3-pyrimidine derivatives (3a-f) have been synthesized by reacting 2,4,6-Trichloropyrimidine with nucleophilic reagents 2-amino-6-fluorobenzothiazole (1) in the presence of acetone. The (4,6- dichloro-pyrimidin-2-yl)-amine (2) so produced was then reacted to two moles of phenylthiourea derivatives to yield title compounds (3a-f). The structural assessment of the compounds (3a-f) was made on the basis of spectral data. The synthesized compounds were screened for theirin vitrogrowth inhibiting activity against different strains of bacteriaviz.,B. subtilis, E. coli, P. aeruginosaandS. aureususing agar diffusion technique. Compounds3cand3fexhibited highest antibacterial activity.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

scholarly journals Biosurfactants Induce Antimicrobial Peptide Production through the Activation of TmSpatzles in Tenebrio molitor

2020 ◽  
Vol 21 (17) ◽  
pp. 6090
Author(s):  
Tariku Tesfaye Edosa ◽  
Yong Hun Jo ◽  
Maryam Keshavarz ◽  
In Seon Kim ◽  
Yeon Soo Han
Keyword(s):  
Antimicrobial Peptide ◽  
Immune Activation ◽  
Tenebrio Molitor ◽  
Antimicrobial Activities ◽  
Iturin A ◽  
E Coli ◽  
Fat Bodies ◽  
Escherichia Coli Bacteria ◽  
Bacteria And Fungi

Biosurfactant immunomodulatory activities in mammals, nematodes, and plants have been investigated. However, the immune activation property of biosurfactants in insects has not been reported. Therefore, here, we studied the defense response triggered by lipopeptides (fengycin and iturin A), glycolipids (rhamnolipid), and cyclic polypeptides (bacitracin) in the coleopteran insect, mealworm Tenebrio molitor. The in vitro antimicrobial activities against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria and fungi (Candida albicans) were assessed by mixing these pathogens with the hemolymph of biosurfactant-immune-activated larvae. E. coli growth was remarkably inhibited by this hemolymph. The antimicrobial peptide (AMP) induction results also revealed that all biosurfactants tested induced several AMPs, exclusively in hemocytes. The survivability analysis of T. molitor larvae challenged by E. coli (106 CFU/µL) at 24 h post biosurfactant-immune activation showed that fengycin, iturin A, and rhamnopid significantly increased survivability against E. coli. Biosurfactant-induced TmSpatzles activation was also monitored, and the results showed that TmSpz3 and TmSpz-like were upregulated in the hemocytes of iturin A-injected larvae, while TmSpz4 and TmSpz6 were upregulated in the fat bodies of the fengycin-, iturin A-, and rhamnolipid-injected larvae. Overall, these results suggest that lipopeptide and glycolipid biosurfactants induce the expression of AMPs in T. molitor via the activation of spätzle genes, thereby increasing the survivability of T. molitor against E. coli.

scholarly journals Phytochemical characterization, anti-cancer and antimicrobial activity of isolated fractions of Alysicarpus vaginalis

2017 ◽  
Vol 12 (1) ◽  
pp. 77 ◽  
Author(s):  
Ganesh Tapadiya ◽  
Mayura A. Kale ◽  
Shweta Saboo
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Methanolic Extract ◽  
Hep G2 ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Anti Cancer ◽  
Proliferative Assay ◽  
Bacteria And Fungi

<p class="Abstract">The methanolic extract of <em>Alysicarpus </em>vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for<em> in vitro</em> antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC<sub>50 </sub>values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and<em> E. coli</em> whereas chloroform and n-butanol fractions were more effective against <em>S. aureus</em> and <em>B. </em>subtilis. The phytochemical characterization by HPLC analysis indicated the presence of important polyphenolic and steroidal compounds.</p>

Synthesis and Evaluation of Novel Fluorobenzimidazole Derivatives as Antibacterial and Antifungal Agents

2019 ◽  
Vol 4 (4) ◽  
pp. 209-215
Author(s):  
D. Joshi ◽  
R. Narigara ◽  
G. Jani ◽  
K. Parikh
Keyword(s):  
Bacterial Strains ◽  
Compound I ◽  
Substituted Anilines ◽  
Gram Negative ◽  
E Coli ◽  
New Class ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Multiple Step

A new class of fluorobenzimidazole derivatives (IIIa-j)was synthesized to investigate their antimicrobial potential. All the compounds were prepared by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol (I). The compound I was further reacted with different derivatives of 2-chloro-N-phenylacetamide (IIa-j) prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF (solvent); resulting in formation of fluorobenzimidazoles IIIa-j. The compounds IIIa-j were characterized by spectral analysis viz. 1H NMR, 13C NMR, mass spectra, elemental analysis and IR. All these compounds were screened in vitro for their antimicrobial activity 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). Some of the compounds exhibited promising results (in MIC) against Gram-negative bacterial strains.

scholarly journals Synthesis and Biological Activity Evaluation of Some Azetidinone and Thiazolidinone Derivatives of Coumarins

1970 ◽  
Vol 4 (2) ◽  
Author(s):  
BB Subudhi ◽  
PK Panda ◽  
BK Tosh ◽  
S Sahu ◽  
P Majhi
Keyword(s):  
Aromatic Aldehydes ◽  
Aluminium Chloride ◽  
Standard Drug ◽  
E Coli ◽  
Triethyl Amine ◽  
Hydroxy Coumarin ◽  
Pharmacological Potential ◽  
Different Strains ◽  
Coumarin 1

Keeping in view the pharmacological potential of azetidinones, thiazolidinones and coumarins, the title compounds containing these nuclei were synthesized. The 4-methyl -7-hydroxy coumarin (1) on treatment with hydrazine hydrate affords 2-hydrazo- 4-methyl -7-hydroxy coumarin (2). The N- (2’-imino-4’-methyl-7’-hydroxy coummarinyl)-imino substituted benzene (3) was synthesized by reaction of compound 2 with various aromatic aldehydes. Condensation of compound 3 with chloroacetyl chloride in presence of 1,4-dioxan and triethyl amine yields the 3-chloro-4- (substituted)-1-(2’-imino-4’-methyl-7’-hydroxy coumarinyl) azetidin-2-one (4a-d). Further more condensation of 3 with thioglycollic acid in presence of 1,4-dioxan and anhydrous aluminium chloride gives 2-(substituted phenyl)-3-(2’-imino-4’-methyl-7’-hydroxy coumarinyl)-1,3-thiazolidinone (4’a-d). Elemental and spectral characterization established the identity of these compounds. All the products were screened in vitro for their anti microbial activity against different strains of urinary tract pathogens. All compounds exhibited significant antimicrobial activity compared to the standard drug nitrofurantoin. Key words: Azetidinones, thiazolidinone, coumarin, nitrofurantoin, E. coli, P. auregenosa, K. pneumoniae, P. mirabilis E. faecalis, and S.aureus. Dhaka Univ. J. Pharm. Sci. Vol.4(2) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals In vitro Effects of Muscodor albus and Three Volatile Components on Growth of Selected Postharvest Microorganisms

HortScience ◽  
2005 ◽  
Vol 40 (7) ◽  
pp. 2109-2114 ◽  
Author(s):  
Ali A. Ramin ◽  
P. Gordon Braun ◽  
Robert K. Prange ◽  
John M. DeLong
Keyword(s):  
Erwinia Carotovora ◽  
Isobutyric Acid ◽  
Penicillium Expansum ◽  
Volatile Components ◽  
E Coli ◽  
In Vitro Effects ◽  
Bacteria And Fungi ◽  
Air Circulation ◽  
Muscodor Albus

Biofumigation by volatiles of Muscodor albus Worapong, Strobel & W.M. Hess, an endophytic fungus, was investigated for the biological control of three postharvest fungi, Botrytis cinerea Pers., Penicillium expansum Link, and Sclerotinia sclerotiorum (Lib) de Bary, and three bacteria, Erwinia carotovora pv. carotovora (Jones) Bergey et al., Pseudomonas fluorescens Migula (isolate A7B), and Escherichia coli (strain K12). Bacteria and fungi on artificial media in petri dishes were exposed to volatiles produced by M. albus mycelium growing on rye seeds in sealed glass 4-L jars with or without air circulation for up to 48 hours. The amount of dry M. albus–rye seed culture varied from 0.25 to 1.25 g·L–1 of jar volume. Fan circulation of volatiles in jars increased efficacy and 0.25 g·L–1 with fan circulation was sufficient to kill or suppress all fungi and bacteria after 24 and 48 hours, respectively. Two major volatiles of M. albus, isobutyric acid (IBA) and 2-methyl-1-butanol (MB), and one minor one, ethyl butyrate (EB), varied in their control of the same postharvest fungi and bacteria. Among the three fungi, IBA killed or suppressed S. sclerotiorum, B. cinerea, and P. expansum at 40, 25, and 45 μL·L –1, respectively. MB killed or suppressed S. sclerotiorum, B. cinerea, and P. expansum at 75, 100, and 100 μL·L –1, respectively. EB was only able to kill S. sclerotiorum at 100 μL·L –1. Among the three bacteria, IBA killed or suppressed E. coli (K12), E. carotovora pv. carotovora, and P. fluorescens at 5, 12.5, and 12.5 μL·L–1, respectively. MB killed or suppressed E. coli (K12), E. carotovora pv. carotovora, and P. fluorescens at 100, 75, and 100 μL·L–1, respectively. EB did not control growth of the three bacteria. This study demonstrates the need for air circulation in M. albus, MB, and IBA treatments to optimize the efficacy of these potential postharvest agents of disease control.

scholarly journals Synthesis of some new 6-aryl-3-(4-isopropylphenyl)[1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles and its anti-microbial study

2021 ◽  
Vol 10 (4) ◽  
pp. 479-488 ◽  
Author(s):  
K. A. Joshi ◽  
J. M. Dhalani ◽  
H. B. Bhatt ◽  
K. M. Kapadiya
Keyword(s):  
Antifungal Activity ◽  
Spectroscopic Techniques ◽  
Aromatic Acids ◽  
Reference Standard ◽  
Antibacterial And Antifungal Activity ◽  
Essential Step ◽  
Step Procedure ◽  
Antibacterial And Antifungal ◽  
Microbial Study

New series of fused 1,2,4-triazoles, i.e., 3-(4-isopropylphenyl)-6-substituted phenyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-5j) have been synthesized via a four-step procedure and using eco-friendly reaction condition at some steps of the synthesis. It was adopted by the formation of hydrazide of methyl 4-isopropylbenzoate (1) followed by reaction with CS2 in basic media to afford potassium salt, which on cyclized to our essential step, 4-amino-5-(4-isopropylphenyl)-4H-1,2,4-triazole-3-thiol (4). The desired adducts (5a-5j) were formed by (4) on reaction with various aromatic acids in POCl3 media. The newly synthesized triazolo- thiadiazoles have been characterized by different spectroscopic techniques and investigated for their in vitro antibacterial and antifungal activity. It was revealed that the compounds 5a, 5c, 5h, and 5i showed interesting antibacterial and antifungal activity compared to the used reference standard.

In vitro effectiveness of antimicrobial properties of propolis and chlorhexidine on oral pathogens: A comparative study

2020 ◽  
Vol 1 (3) ◽  
pp. 116-125
Author(s):  
Hadis Tavafi ◽  
Maryam- sadat Sadrzadeh-Afshar ◽  
Soroush Niroomand
Keyword(s):  
Periodontal Disease ◽  
Antimicrobial Properties ◽  
Bacterial Strains ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Microbial Strains ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
Oral Conditions

Periodontal disease is one of the most prevalent infectious oral conditions in the present century, and it is necessary to conduct research to find a solution to overcome these diseases. A variety of microbial strains of bacteria and fungi are involved in the pathogenesis of periodontal disease. The use of chemical agents such as mouthwashes is one of the strategies to control these diseases. The purpose of the present study was to compare the antimicrobial effects of propolis and chlorhexidine gluconate (CHX) on the bacterial strains of Streptococcus mutans, Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, Pseudomonas aeruginosa, and the yeast strain of Candida albicans using the broth microdilution method. The results showed the inhibitory and microbicidal activities of the two substances against the tested microbial strains. The antibacterial and antifungal effects of CHX were more effective reported in this study than that of propolis against the studied pathogens. The results of this study also indicated that the propolis was less effective in inhibiting bacterial growth than the CHX. In addition, the combination of these two solutions had a synergistic effect on inhibition of other studied strains, with the exception of C. albicans and S. aureus. There is a need for further research on strains isolated from oral biofilm to achieve complementary results.

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