scholarly journals Synthesis and Antimicrobial Activity of 4-Oxo-Thiazolidines and 5-Arylidene Derivatives of 2-Amino-5-Ethyl-1,3,4-Thiadiazole

2018 ◽  
Vol 42 (2) ◽  
pp. 155-170
Author(s):  
Sunil Makwane ◽  
SD Srivastava ◽  
Rajiv Dua ◽  
SK Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Thioglycolic Acid ◽  
Sodium Ethoxide ◽  
Aromatic Aldehydes ◽  
Knoevenagel Reaction ◽  
E Coli ◽  
Bacteria And Fungi ◽  
Academy Of Sciences ◽  
Derivatives Of ◽  
Anhydrous Zncl2

A new series of 5-benzylidene-3-(5-ethyl-[1,3,4]thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones (3a-3m) were synthesized. The reaction of thioglycolic acid with benzylidene-(5-ethyl-[1,3,4] thiadiazol-2-yl)-amine 1a in the presence of anhydrous ZnCl2 afforded the new heterocyclic compounds 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazole-yl)-2-phenyl-thiazolidin-4-one, 2a. The latter product on treatment with several selected substituted aromatic aldehydes in the presence of sodium ethoxide underwent the Knoevenagel reaction to yield 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones, 3a-3m. The structures of the compounds were confirmed by IR, 1H-NMR, 13C-NMR and mass spectroscopy and by chemical analysis. All the above compounds were screened for their antimicrobial activity against some selected bacteria and fungi such as E. coli, B. Subtilis, and S. Typhi bacteria and A.niger, A. Flavus and F. oxisporium Fungi. Journal of Bangladesh Academy of Sciences, Vol. 42, No. 2, 155-170, 2018

scholarly journals Synthesis and biological activity of 4-thiazolidinone derivatives of phenothiazine

2012 ◽  
Vol 77 (1) ◽  
pp. 17-26 ◽  
Author(s):  
Ritu Sharma ◽  
Pushkal Samadhiya ◽  
Savitri Srivastava ◽  
Santosh Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Thioglycolic Acid ◽  
Cycloaddition Reaction ◽  
Aromatic Aldehydes ◽  
Knoevenagel Reaction ◽  
Antituberculosis Activity ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Anhydrous Zncl2

A new series of N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo-5-( substituted benzylidene)-1,3-thiazolidine-carboxamide, 5(as) have been synthesized. The cycloaddition reaction of thioglycolic acid with N-[3-(10H-phenothiazinyl)-propyl]-N?-[(substituted phenyl)-methylidene]- urea, 3(a-s) in the presence of anhydrous ZnCl2 afforded new heterocyclic compounds N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo- 1,3-thiazolidine-carboxamide, 4(a-s). The later product on treatment with several selected substituted aromatic aldehydes in the presence of C2H5ONa undergoes Knoevenagel reaction to yield 5(a-s). The structure of compounds 1, 2, 3(a-s), 4(a-s) and 5(a-s) were confirmed by IR, 1H NMR, 13C NMR, Fmass and chemical analysis. All above compounds were screened for their antimicrobial activity against some selected bacteria and fungi and for antituberculosis activity compounds have been screened against the bacterium M. tuberculosis.

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, Characterization and Antimicrobial Activity of N-2-(4-Chlorophenyl)acetyl Derivatives of (S)-Amino Acids

2019 ◽  
Vol 32 (2) ◽  
pp. 381-384
Author(s):  
G. Venkateshappa ◽  
P. Raghavendra Kumar ◽  
Krishna2
Keyword(s):  
Amino Acids ◽  
Antimicrobial Activity ◽  
Diffusion Method ◽  
Gram Negative ◽  
E Coli ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Ft Ir Spectroscopy ◽  
Agar Well Diffusion Method

This paper reports the synthesis, characterization and antibacterial activity of N-2-(4-chlorophenyl)acetyl derivatives of various (S)-amino acids such as (S)-alanine, (S)-phenylalanine, (S)-leucine, (S)-methionine, (S)-proline and (S)-tryptophane. These compounds have been successfully synthesized and their structures were confirmed by 1H NMR and 13C NMR and FT-IR spectroscopy. The antimicrobial activity of these six (S)-amino acids derivatives have been evaluated by the agar well diffusion method against pathogens both Gram-positive (S. aureus) and Gram-negative (K. aerogenes, E. coli and P. desmolyticumas) bacteria and fungi (A. flavus and C. albicans). All these compounds have shown mild to moderate antimicrobial activity.

scholarly journals The Synthesis and Antimicrobial Activity of Some 4-Hydroxycoumarin Derivatives

2008 ◽  
Vol 8 (3) ◽  
pp. 277-281 ◽  
Author(s):  
Davorka Završnik ◽  
Samija Muratović ◽  
Selma Špirtović ◽  
Dženita Softić ◽  
Marica Medić-Šarić
Keyword(s):  
Antimicrobial Activity ◽  
Growth Inhibition ◽  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Coumarin Derivatives ◽  
Microbiological Activity ◽  
Gram Negative ◽  
Bacteria And Fungi ◽  
Derivatives Of

Due to exceptional reactivity of 4-hydroxycoumarin, the synthesis of new coumarin derivatives of dimer and tetramer type has been carried out. The synthesis was carried out from 4-hydroxycoumarin and various aromatic aldehydes. In this way, compounds of the dimer 3,3’-(benzilidene)bis (4-hydroxycoumarin) type, as well as of the tetramer 3,3,’3’,’3’’’-(1,4-dim- ethylenphenyl)tetra (4-hydroxycoumarin) type were prepared.The newly synthesized derivatives contain different functional groups, and as such they could exhibit microbiological activity. Therefore, we tested the microbiological activity of these derivatives on various species of bacteria and fungi. The tested compounds have shown different activity in terms of growth inhibition of microorganisms. Newly synthesized derivatives exhibit antibacterial activities, manifested as growth inhibition on Grampositive bacteria types (Bacillus, Staphylococcus), while the activity against Candida was much weaker. The same compound did not show any antimicrobial activity against two Gram-negative bacteria types (Escherichia coli, Pseudomonas aeruginosa). The compound 1 showed the best microbiological activity. The obtained results confirmed its good antibacterial and antimycotic activities against different microorganisms.

scholarly journals Antimicrobial Activity of Cationic Poly(3-hexylthiophene) Nanoparticles Coupled with Dual Fluorescent and Electrochemical Sensing: Theragnostic Prospect

Sensors ◽  
2021 ◽  
Vol 21 (5) ◽  
pp. 1715
Author(s):  
Nada Elgiddawy ◽  
Shiwei Ren ◽  
Wadih Ghattas ◽  
Waleed M. A. El Rouby ◽  
Ahmed O. El-Gendy ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fluorescence Spectroscopy ◽  
Bacterial Infections ◽  
Electrochemical Impedance ◽  
Spectroscopic Properties ◽  
Electrochemical Sensing ◽  
E Coli ◽  
Normal Human ◽  
Dual Detection ◽  
Bacteria And Fungi

Designing therapeutic and sensor materials to diagnose and eliminate bacterial infections remains a significant challenge for active theragnostic nanoprobes. In the present work, fluorescent/electroactive poly(3-hexylthiophene) P3HT nanoparticles (NPs) stabilized with quaternary ammonium salts using cetyltrimethylammonium bromide (CTAB), (CTAB-P3HT NPs) were prepared using a simple mini-emulsion method. The morphology, spectroscopic properties and electronic properties of CTAB-P3HT NPs were characterized by DLS, zeta potential, SEM, TEM, UV-vis spectrophotometry, fluorescence spectroscopy and electrochemical impedance spectroscopy (EIS). In an aqueous solution, CTAB-P3HT NPs were revealed to be uniformly sized, highly fluorescent and present a highly positively charged NP surface with good electroactivity. Dual detection was demonstrated as the binding of the bacteria to NPs could be observed by fluorescence quenching as well as by the changes in EIS. Binding of E. coli to CTAB-P3HT NPs was demonstrated and LODs of 5 CFU/mL and 250 CFU/mL were obtained by relying on the fluorescence spectroscopy and EIS, respectively. The antimicrobial activity of CTAB-P3HT NPs on bacteria and fungi was also studied under dark and nutritive conditions. An MIC and an MBC of 2.5 µg/mL were obtained with E. coli and with S. aureus, and of 0.312 µg/mL with C. albicans. Additionally a good biocompatibility toward normal human cells (WI38) was observed, which opens the way to their possible use as a therapeutic agent.

scholarly journals Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Property ◽  
Docking Study ◽  
Gram Negative Bacteria ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Comparable Activity ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

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>

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

scholarly journals Synthesis, Characterisation and Antimicrobial Potential of Novel N-Alkylated Pyrrole Derivatives of Chitosan

2021 ◽  
Vol 14 (4) ◽  
pp. 1730-1736
Author(s):  
Kalpana. P. R
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Effect ◽  
Maximum Activity ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Pyrrole Derivatives ◽  
Structural Modifications ◽  
E Coli ◽  
Antimicrobial Potential ◽  
Derivatives Of

Chitosan, a cationic biopolymer is a major derivative of chitin. It is biocompatible, non-toxic and environ-friendly material and has broad spectrum antimicrobial activity. However, it is less effective in neutral or basic conditions due to its solubility only in acidic medium. Therefore, chemical modification with suitable groups is necessary to enhance the potency of chitosan. The present study was mainly conducted to explore the effect of structural modifications on antimicrobial potential of chitosan. N-Methyl, N-Ethyl and N-Propyl pyrrole were reacted with N-chloroacyl-6-O-triphenylmethylchitosan prepared by stepwise modification of chitosan to form N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives of chitosan. Structural characterization of these pyrrole derivatives was done by IR, NMR, XRD, DSC and Elemental Analysis. The gram-negative bacterium Escherichia coli, gram-positive bacterium Staphylococcus aureus were selected for antibacterial activity and the fungus C. albicans was selected for antifungal activity by agar diffusion method and MIC method. Antimicrobial activity of the N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives on E. coli, S. aureus and C. albicans showed an inhibitory effect on all the organisms. The potency of inhibition was found to be varied with the substitutions. The maximum activity was shown by N-pyrrolylpropylchitosan against E. coli (zone of inhibition 1.2±0.05cm, MIC 0.15±0.03mg/ml), S. aureus (zone of inhibition 1.4±0.03cm, MIC 0.15±0.01mg/ml), C. albicans (zone of inhibition 0.8±0.03cm, MIC 0.2±0.03mg/ml). The study also confirmed that all the three derivatives exhibited higher inhibition than that of chitosan against E. coli (zone of inhibition 0.7±0.03cm, MIC 0.09±0.02mg/ml), S. aureus (zone of inhibition 0.8±0.03cm, MIC 0.09±0.02mg/ml), C. albicans (zone of inhibition 0.6±0.03cm, MIC 0.09±0.03mg/ml). Results demonstrated that these three N-alkylpyrrole chitosan derivatives exhibited improved potency and hence can have the more applicability as antimicrobials.

scholarly journals Antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata

2020 ◽  
Vol 4 (1) ◽  
pp. 49
Author(s):  
Gracielle Oliveira Sabbag Cunha ◽  
Ana Paula Terezan ◽  
Andreia Pereira Matos ◽  
Marcela Carmen De Melo Burger ◽  
Paulo Cezar Vieira ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Methyl Esters ◽  
Carboxyl Group ◽  
Isomeric Mixture ◽  
E Coli ◽  
Bacillus Subtilis Atcc ◽  
Derivatives Of

This study evaluated the antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata (Melastomataceae) against five microorganisms: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6623), Pseudomonas aeruginosa (ATCC 15442), and Candida albicans (ATCC 10231). The isomeric mixture of ursolic and oleanolic acids was active against S. aureus (MIC = 250 μg mL-1) and against E. coli, B. subtilis, and P. aeruginosa (MIC = 500 μg mL-1). The flavone 5,6,7-trihydroxy-4’-methoxyflavone and the methyl esters, semisynthetic derivatives of a mixture of ursolic and oleanolic acids, showed no activity against the tested microorganisms. These results suggest that the carboxyl group present in the triterpenes may contribute to antimicrobial activity.

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