Synthesis, characterization and antimicrobial activities of 1,5-dimethyl-2-phenyl-4-(pyrolidin-2-ylideneamino)-pyrazolidin-3-one and complex with iron(II)

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Condensation Reaction ◽  
Physical Method ◽  
Antimicrobial Activities ◽  
Multifunctional Ligand

A multifunctional ligand derivative of pyrrolidone has been synthesized by condensation reaction between 4-aminoantipyrine and 2-pyrrolidinone. The ligand and its Iron(II) complex were characterized using physical method and UV and IR techniques. The ligand and Fe(II) complex were tested against broad spectrums of bacterial organisms and the results show that both the ligand and complex were active against various organisms tested.

scholarly journals New Urea and Thiourea Derivatives of Piperazine Doped with Febuxostat: Synthesis and Evaluation of Anti-TMV and Antimicrobial Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Reddivari Chenna Krishna Reddy ◽  
Syed Rasheed ◽  
Devineni Subba Rao ◽  
Shaik Adam ◽  
Yellala Venkata Rami Reddy ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Biological Data ◽  
Thiourea Derivatives ◽  
Biological Interest ◽  
Antiviral Activities ◽  
High Yields ◽  
Selective Reagent ◽  
Substituted Urea

A series of new 4-(5-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-2-carbonyl)-N-(substituted phenyl)piperazine-1-carboxamides8(a–e)/carbothioamides8(f–j)were accomplished for biological interest by the simple addition of active functionalized arylisocyanates7(a–e)/arylisothiocyanates7(f–j)with 2-isobutoxy-5-(4-methyl-2-(piperazine-1-carbonyl)thiazol-5-yl)benzonitrile(4). Compound4was synthesized in high yields (94%) by the condensation reaction of febuxostat (1) with piperazine using a selective reagent such as propylphosphonic anhydride (T3P). Antiviral activity againstTobacco mosaic virus(TMV) and antimicrobial activity of the synthesized compounds were evaluated. Biological data revealed that 4-nitrophenyl substituted urea8d, and 3-bromophenyl substituted thiourea8fexhibited promising antiviral activities. Moreover, 4-fluorophenyl substituted urea8a, 4-nitrophenyl substituted urea8d, 3-bromophenyl substituted thiourea8f, and 2,4-dichlorophenyl substituted thiourea8jexhibited potent antimicrobial activity.

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 Cloning and expression of \(\textit{ pigI}\) gene in \(\textit{Escherichia coli}\) BL21 (DE3)

2021 ◽  
Vol 43 (3) ◽  
pp. 59-67
Author(s):  
Do Minh Trung ◽  
Do Hai Quynh ◽  
Nguyen Thuy Duong
Keyword(s):  
Escherichia Coli ◽  
Recombinant Protein ◽  
Biosynthetic Pathway ◽  
Condensation Reaction ◽  
Potential Method ◽  
Antimicrobial Activities ◽  
Cloning And Expression ◽  
E Coli ◽  
Recombinant Vector ◽  
His Tag

Prodigiosin (Pg), a secondary metabolite with anticancer and antimicrobial activities, can be produced in Serratia marcescens bacteria through the condensation reaction of 4-methoxy-2, 2’-bipyrrole-5-carboxyaldehyde (MBC) and 2-methyl-3-amylpyrrole (MAP). Among these, the MBC synthetic pathway is started by the conversion of L-proline to L-proline-AMP before this complex is covalently attached to PigG. This reaction is catalyzed by an L-prolyl-AMP ligase named PigI. Therefore, PigI protein plays an important role in the prodigiosin biosynthetic pathway. However, studies related to PigI protein have not been carried out in Vietnam yet. In this work, the pigI gene was cloned and expressed in Escherichia coli DH10B and BL21 (DE3), respectively. Sequence alignment results revealed that the obtained pigI gene is 99.7% identical to the four strains, CP027798, CP027796, CP021984 and CP003959. This recombinant vector pJET1.2/pigI was used to reamplify pigI, and the acquired amplicon was inserted into pET22b vector at the site of HindIII and XhoI. The clone E. coli BL21 (DE3) containing the recombinant vector pET22b/pigI was expressed in an auto-induced medium. The presence of PigI protein in the lysate was identified due to a 53 kDa band through Western Blot analysis using an anti-his-tag antibody. The results of our study provide a potential method for producing prodigiosin from recombinant protein in Vietnam.

scholarly journals Eco-friendly and simple synthesis of some non-natural flavones through chalcones

2018 ◽  
Vol 9 (3) ◽  
pp. 236-240
Author(s):  
Mohammad Saidur Rahman ◽  
Sayeda Shakila Alam ◽  
Kamrunnahar Happy ◽  
Mohammad Mamun Hossain ◽  
Mohammad Khademul Islam ◽  
...  
Keyword(s):  
Sulfuric Acid ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Simple Synthesis ◽  
Minimal Amount ◽  
Important Class ◽  
High Yields ◽  
Antioxidant And Antimicrobial Activities

A distinctive feature of polyphenolics is the possession of biological properties such as antioxidant and antimicrobial activities. Simple synthesis and study about such important class of compounds and their analogs are very important to enhance the understanding of their role in human health and diseases. Accordingly, a series of chalcones (2a-f) have been synthesized by Claisen-Schmidt condensation reaction with required acetophenones and aromatic aldehydes in high yields. The conversion of chalcones to the corresponding flavones (1a-g) taking minimal amount of dimethyl sulfoxide with iodine in presence of sulfuric acid was carried out under microwave conditions in high yields.

Synthesis, Characterization and evaluation of Anti-inflammatory and Antimicrobial Properties of some Cinnamic Acid Derivatives

2020 ◽  
Vol 16 (1) ◽  
pp. 1-8
Author(s):  
B.B Jacob ◽  
H. Baba ◽  
J.O. Oluwadiya
Keyword(s):  
Dose Level ◽  
Cinnamic Acid ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
High Yield ◽  
Cinnamic Acid Derivatives ◽  
13C Nuclear Magnetic Resonance ◽  
Vis Spectroscopy ◽  
Anti Inflammatory

Background: Cinnamic acid and derivatives are widely spread in plants. They are important intermediates in the synthesis of many aromatic compounds and are known to have diverse biological activities.Objectives: To synthesize, characterize and evaluate some cinnamic acid derivatives, for possible antimicrobial and anti-inflammatory activities.Material and methods: Different cinnamic acid derivatives were synthesized by Knoevenagel condensation reaction between malonic acid and various derivatives of benzaldehydes in the presence of pyridine and hydrochloric acid. The cinnamic acid epoxide was formed in the presence of hydrogen peroxide and KOH, while dihydro-cinnamic acid and paramethoxy-dihydro-cinnamic acids were formed by reducing cinnamic acid and paramthoxy-cinnamic acid respectively with raney nickel in the presence of 10% KOH. The final products were purified on column chromatography (CC), eluting with petroleum spirit/ethyl acetate. All the synthesized compounds were unequivocally characterized using the combination of UV-Vis Spectroscopy, infra-red (FTIR), 1H and 13C Nuclear Magnetic Resonance (NMR) spectroscopy. In-vivo anti-inflammatory activities of the synthesized compounds was investigated using egg albumin-induced paw oedema in rat; while antimicrobial activity was evaluated by agar diffusion method.Results: The compounds were obtained in high yield (30 – 97 %) and purity. 3,4-dioxomethylene cinnamic acid produced the highest (60.8%) and significant (p < 0.05) anti-inflammatory effect at the 2nd hour of the highest dose. Dihydro-cinnamic acid and cinnamic acid epoxide with 4mg/kg dose produced 55.5% and 54.9% inhibition of inflammation respectively at the second hour, while para-methoxy-cinnamic acid at the second hour with 2 mg/kg dose level produced 54.0% inhibition. The reference compound; diclofenac produced no significant inhibition of inflammation at 4mg/kg dose level. All the compounds showed mild antimicrobial activities against the tested organisms.Conclusion: The findings from the study indicate that the synthesized compounds possess mild anti-inflammatory, with weak antibacterial and antifungal activities. Keywords: anti-inflammatory, antimicrobial, cinnamic acid derivatives, Knoevenagel

scholarly journals Synthesis, Spectral Correlations and Antimicrobial Activities of 2-Pyrimidine Schiff’s Bases

2015 ◽  
Vol 53 ◽  
pp. 154-164 ◽  
Author(s):  
R. Senbagam ◽  
M. Rajarajan ◽  
R. Vijayakumar ◽  
V. Manikandan ◽  
S. Balaji ◽  
...  
Keyword(s):  
Spectral Data ◽  
Chemical Shifts ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Disc Diffusion Method ◽  
Schiff’S Base ◽  
Ir Frequencies ◽  
Substituent Constants ◽  
Multi Linear Regression

In the present study, a series of substituted (E)-N-benzylidene-2-aminopyrimidine compounds have been synthesized by condensation reaction with 2-aminopyrimidine and meta- and para- substituted benzaldehydes. These synthesized Schiff’s base compounds are confirmed by their physical constants, UV, IR and NMR spectral data. All the observed UV absorption maximum λmax(nm), IR frequencies νC=N(cm-1), NMR δ(ppm) of C-H & C=N chemical shifts have been correlated with Hammett substituent constants and F and R parameters using single and multi-linear regression analyses in order to study the effect of substituents on these spectral data has been studied. The antimicrobial activities of all the synthesized Schiff’s base compounds have been studied using Bauer-Kirby disc diffusion method

TiCl2·2H2O catalyzed one-pot synthesis of highly functionalized tetrahydropiperidines and evaluation of their antimicrobial activities

2016 ◽  
Vol 22 (3) ◽  
Author(s):  
Mohsen Abbasi ◽  
Seyed Mohammad Seyedi ◽  
Hamid Sadeghian ◽  
Maryam Akhbari ◽  
Mohammadreza Enayaty ◽  
...  
Keyword(s):  
Ethyl Acetoacetate ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
One Pot ◽  
One Pot Synthesis ◽  
One Pot Condensation ◽  
Substituted Benzaldehydes

AbstractOne-pot condensation reaction of ethyl acetoacetate, various substituted benzaldehydes and anilines in the presence of TiCl

scholarly journals Synthesis, Hammett Spectral Correlations and Antimicrobial Activities of (E)-1-Benzylidene-2-(4-Chlorophenyl)Hydrazines

2015 ◽  
Vol 59 ◽  
pp. 147-159
Author(s):  
M. Rajarajan ◽  
R. Vijayakumar ◽  
R. Senbagam ◽  
S. Balaji ◽  
V. Manikandan ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Regression Analysis ◽  
Spectral Data ◽  
Condensation Reaction ◽  
Linear Regression Analysis ◽  
Acid Catalyst ◽  
Antimicrobial Activities ◽  
Infra Red ◽  
Substituent Constants ◽  
Multi Linear Regression

In the present study, a series of nine number of (E)-1-benzylidene-2-(4-chlorophenyl) hydrazine compounds have been synthesized by condensation reaction of meta and para substituted benzaldehydes with 4-chlorophenylhydrazine using acetic acid catalyst. They are characterized by their physical constants, UV (200-450 nm), Infra-Red (KBr, 4000-400 cm−1) and NMR (1H and 13C) spectral data. The observed UV, IR and NMR spectral data have been correlated with Hammett substituent constants and Swain-Lupton’s F and R parameters using single and multi-linear regression analysis. From the results of statistical analysis the effects of substituents on the spectral data have been discussed. The antimicrobial activities of all the synthesized (E)-1-benzylidene-2-(4-chlorophenyl) hydrazine compounds have been studied using Bauer–Kirby method.

scholarly journals Cloning and expression of pigC gene in Escherichia coli

2020 ◽  
Vol 16 (4) ◽  
pp. 757-765
Author(s):  
Do Minh Trung ◽  
Do Hai Quynh ◽  
Tran Viet Tien ◽  
Nguyen Duy Bac ◽  
Do Thi Tuyen ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Condensation Reaction ◽  
Pcr Amplification ◽  
Antimicrobial Activities ◽  
Cloning And Expression ◽  
Universal Primers ◽  
Coding Region ◽  
Colony Pcr ◽  
E Coli ◽  
Recombinant Vector

Prodigiosin (Pg), which is particularly of interest because of anticancer and antimicrobial activities, can be produced through the PigC-catalyzed condensation reaction of 4-methoxy-2, 2’-bipyrrole-5-carboxyaldehyde (MBC) and 2-methyl-3-amylpyrrole (MAP). Therefore, the PigC protein plays an important role in prodigiosin biosynthetic pathway. However, studies related to PigC protein have not been carried out in Vietnam yet. In this work, the pigC gene was cloned and expressed in Escherichia coli DH10B and BL21 (DE3), respectively. Using PCR and universal primers, we amplified a fragment of 3 kb covering entire coding region of the pigC gene from Serratia sp. strain M5. The pigC gene was inserted into pJET1.2 vector, and then transformed into E. coli DH10B. The sequence of a recombinant vector pJET1.2/pigC was evaluated by using whole colony PCR amplification. Sequence alignment results revealed that the obtained pigC gene possesses 71.5% and 75.4% of nucleotide identity in comparison with two strains, Serratia 39006 and Serratia sp. AS9 published in GenBank with their respective accession numbers of AJ833001 and CP002773. The recombinant vector pJET1.2/pigC was used to reamplify pigC, and the acquired amplicon was inserted into pET22b vector at the site of HindIII and XhoI. The clone E. coli BL21 (DE3) containing recombinant vector pET22b/pigC was expressed in the auto-induced medium. The presence of PigC protein in the lysate was identified as a 100 kDa band through Western Blot analysis using anti his-tag antibody. Afterward, the PigC protein was purified by Ni-NTA column, and its expression level was quantified through SDS-PAGE analysis. The results of our study provide a potential material for producing prodigiosin from recombinant protein in Vietnam.

scholarly journals Synthesis, characterization and antimicrobial activities of schiff base derived from thiourea and anisaldehyde and its Mn(II), Fe (II) and Co(II) complexes

2018 ◽  
Vol 11 (1) ◽  
pp. 20-24
Author(s):  
I.T. Siraj ◽  
B.U. Sambo
Keyword(s):  
Escherichia Coli ◽  
Schiff Base ◽  
Metal Ion ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Tetradentate Ligand ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Metal Ligand

Complexes of Mn(II), Fe(II) and Co(II) with a Schiff base derived from condensation reaction of thiourea and o-anisaldehyde has been synthesized and characterized analytically and spectroscopically. Melting point of the Schiff base was found to be 160°C and the complexes decomposed within a temperature range of 215 to 275°C. Molarconductances of the complexes were found to be within 1.1 to 3.5W–1 cm2 mol–1 range. Magnetic moment indicated the complexes to be paramagnetic (4.03 to 5.71BM). Infrared spectrum of the Schiff base showed the azomethine peak at 1601cm–1 which shifted up to1687cm–1 in the complexes. The analytical and spectral studies revealed that all the metal(II) complexes are in 1:3 metal ligand ratio, with the Schiff base acting as tetradentate ligand towards the metal ion via azomethine – N, and methoxy –O and two chlorine atoms were further coordinated to the metal(II) ion. The synthesized ligand and its respective metal (II) complexes were screened for their antibacterial activity against Staphylococcus aureus and Escherichia coli strains and antifungal activity against Aspergillus flavus and Mucorindicus. The results revealed that, the Schiff base and the metal (II) complexes showed significant antibacterial and antifungal activities at high concentration.Keywords: Metal complexes, thiourea, anisaldehyde, characterization, antimicrobial

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