scholarly journals Ultrasonication-Induced Synthesis and Antimicrobial Evaluation of Some Multifluorinated Pyrazolone Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Anil Gadhave ◽  
Shashikant Kuchekar ◽  
Bhausaheb Karale
Keyword(s):  
Fungal Pathogens ◽  
Condensation Reaction ◽  
Ultrasound Irradiation ◽  
Conventional Heating ◽  
Aspergillus Clavatus ◽  
H Nmr ◽  
Pyrazolone Derivatives ◽  
Knoevenagel Condensation Reaction ◽  
Antimicrobial Evaluation

A series of novel fluorine containing pyrazole-pyrazolone (4a–j) and chromone-pyrazolone (5a–i) was synthesized from multifluorinated pyrazolone by the Knoevenagel condensation reaction. All compounds were synthesized by conventional heating as well as ultrasound irradiation technique. It was found that ultrasonication method was more efficient than conventional heating method. The newly synthesized compounds were subjected forin vitroantimicrobial screening against four bacterial pathogens, namely,Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli,andPseudomonas aeruginosaand three fungal pathogensCandida albicans, Aspergillus niger,andAspergillus clavatus, using broth microdilution (MIC) method (CLSI guidelines). Among them, some compounds exhibited promising antibacterial activity against the tested strains. All synthesized compounds were characterized by IR,1H-NMR, mass, and elemental analysis.

scholarly journals Synthesis and In Vitro Antimicrobial Evaluation of Amine Substituted s-Triazine Based Thiazolidinone/Chalcone Hybrids

2014 ◽  
Vol 36 ◽  
pp. 207-219
Author(s):  
Dhruvin R. Shah ◽  
Harshad P. Lakum ◽  
Kishor H. Chikhalia
Keyword(s):  
Multidrug Resistant ◽  
Drug Candidate ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Potent Drug ◽  
Broth Dilution ◽  
Mic Value

In an attempt to control multidrug resistant dilemma, a library of s-triazine based on two novel series of thiazolidinone (4a-e) and chalcone (7a-e) derivatives were designed and synthesized with simple and efficient etiquette. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus Aureus, Bacillus Cereus, Pseudomonas Aeruginosa, Klebsiella Pneumoniae,) and fungi (Candida Albicans, Aspergillus Clavatus) using the broth dilution technique. Compound 7d was the best bioactive desired antibacterial analogue with less MIC value against different tested strains. Results of bioassay study revealed the future hope of the potent drug-candidate based on s-triazine scaffold. All the final synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass and elemental analysis.

scholarly journals Synthesis and Characterization of New Amino Acid-Schiff Bases and Studies their Effects on the Activity of ACP, PAP and NPA Enzymes (In Vitro)

2012 ◽  
Vol 9 (2) ◽  
pp. 962-969 ◽  
Author(s):  
Zahraa Salim M. Al-Garawi ◽  
Ivan Hameed R. Tomi ◽  
Ali Hussein R. Al-Daraji
Keyword(s):  
Schiff Base ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Activation Effect ◽  
Inhibition Effect ◽  
H Nmr ◽  
Ft Ir ◽  
High Concentrations

In this study, two new Schiff base compounds derived from the condensation reaction ofL-glycine andL-tryptophan with 4-methylbenzal-dehyde have been synthesized. The Schiff base compounds were characterized by FT-IR, UV and1H NMR spectroscopy. Their effects on the activity of total (ACP), prostatic (PAP) and non prostatic (NPA) acid phosphatase enzymes were studied. The Schiff base derived fromL-glycine (A) demonstrated inhibition effect on the ACP and NPA activities and activation effect on PAP activity. The Schiff base derived fromL-tryptophan (B) demonstrated semi fixed inhibition effects on the ACP and NPA activities at high concentrations (5.5×10-2, 5.5×10-3and 5.5×10-4M) and activator effect at low concentration (5.5×10-5M) while it was exhibits as activator on PAP activity.

scholarly journals Synthesis and In Vitro Antibacterial and Antifungal Evaluation of Quinoline Analogue Azetidin and Thiazolidin Derivatives

2014 ◽  
Vol 39 ◽  
pp. 195-210 ◽  
Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  
Keyword(s):  
Gram Negative Bacteria ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal ◽  
Broth Dilution

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.

An Efficient Synthesis and Antimicrobial Evaluation of some New Pyrazoline, Pyrimidine and Benzodiazepine Derivatives Bearing 1,3,5-Triazine Core

2015 ◽  
Vol 57 ◽  
pp. 13-24 ◽  
Author(s):  
Anjani Solankee ◽  
Riki Tailor
Keyword(s):  
Guanidine Hydrochloride ◽  
Antibacterial Activities ◽  
Dilution Method ◽  
Mass Spectral ◽  
E Coli ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Benzodiazepine Derivatives ◽  
Amino Pyrimidine

In our present investigation a new class of diverse sets of acetyl pyrazolines (6a-e), amino pyrimidines (7a-e) and 1,5-benzodiazepines (8a-e) bearing 1,3,5-triazine core were synthesised from chalcones (5a-e). Treatment of chalcone with hydrazine hydrate, guanidine hydrochloride and o-phenylenediamine afforded the corresponding acetyl pyrazoline, amino pyrimidine and 1,5-benzodiazepine derivatives respectively. The structures of all the newly synthesised compounds were assigned on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data as well as elemental analysis. In vitro antimicrobial proficiency of the title compounds were assessed against selected pathogens S. aureus MTCC 96, S. pyogeneus MTCC 442, E. coli MTCC 443 and P. aeruginosa MTCC 1688 bacteria for antibacterial activities as well as antifungal activities against C. albicans MTCC 227, A. niger MTCC 282 and A. clavatus MTCC 1323 were used. The minimum inhibitory concentration (MIC) was determined by broth dilution method and recorded at the lowest concentration inhibiting growth of the organism. Among the synthesised compounds 6b, 6c, 7b, 8b, 8d and 8e exhibited excellent antimicrobial activity and said to be the most proficient members of the series.

Synthesis and Antimicrobial Evaluation of 1,3,4-Oxadiazole bearing Schiff Base Moiety

2020 ◽  
Vol 5 (1) ◽  
pp. 1-5
Author(s):  
K. Kapadiya ◽  
G. Dubal ◽  
Y. Bhola ◽  
P. Dholaria
Keyword(s):  
Streptococcus Pyogenes ◽  
Nmr Spectra ◽  
Gram Negative Bacteria ◽  
13C Nmr Spectra ◽  
Aspergillus Clavatus ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
In Vitro Antibacterial Activity ◽  
Antimicrobial Evaluation

A new series of 4-((5-(2-chlorophenyl)-1,3,4-oxadiazol-2-yl)methoxy)-N-(benzylidene derivatives)benzenamine (5a-k) have been synthesized and were screened for their in vitro antibacterial activity against Gram-positive bacteria (Pseudomonas aeruginosa, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Staphylococcus aureus) and antifungal activity (Candida albicans, Aspergillus niger, Aspergillus clavatus). Synthesized compounds were characterized by IR, mass (MS), 1H NMR and 13C NMR spectra. The synthesized compounds 5b, 5c, 5g and 5i showed potency in terms of antimicrobial activity against tested microorganisms.

scholarly journals Microwave-Assisted Synthesis of Arylidene Acetophenones

2013 ◽  
Vol 2013 ◽  
pp. 1-5
Author(s):  
Sheauly Khatun ◽  
M. Z. H. Khan ◽  
Khodeza Khatun ◽  
M. A. Sattar
Keyword(s):  
Microwave Irradiation ◽  
Microwave Heating ◽  
Spectral Data ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Conventional Heating ◽  
Microwave Assisted Synthesis ◽  
Efficient Synthesis ◽  
H Nmr ◽  
Microwave Assisted

An efficient synthesis of arylidene acetophenones have been achieved by using the microwave heating in comparison to the conventional heating. In this work compound 1-phenyle-3-(4-droxyphenyle)-2-propen-1-one, 1-(4-chlorophenyle)-3-phenyle-2-propen-1-one, and 1-(4-chlorophenyle)-3-(4-hydroxyphenyle)-2-propen-1-one have been synthesized by the condensation reaction between aromatic aldehydes and substituted acetophenones under microwave irradiation. The compounds of aldehydes and acetophenones were used as benzaldehyde, parahydroxybenzaldehyde, acetophenone, and parachloroacetophenone. The result shows that the time taken for the reaction was reduced from the conventional 1-2 hours to 60–120 seconds. The yield of the compounds in the conventional heating was moderate while the highest yield of 90–98% was observed in MWI method. The structure of the compounds was characterized by their IR,1H-NMR spectral data.

scholarly journals In vitro antimicrobial evaluation of pyrazolone derivatives

2015 ◽  
Vol 10 (1) ◽  
Author(s):  
Leile Rahimi Ahar ◽  
Moayad Hossaini Sadr ◽  
Karim Zare ◽  
Samad Motameni Tabatabaei
Keyword(s):  
Pyrazolone Derivatives ◽  
Antimicrobial Evaluation

scholarly journals PYRIMIDINE INCORPORATED SCHIFF BASE OF ISONIAZID WITH THEIR SYNTHESIS, CHARACTERIZATION AND IN VITRO BIOLOGICAL EVALUATION

2017 ◽  
Vol 10 (10) ◽  
pp. 209 ◽  
Author(s):  
Hetal I Soni ◽  
Navin B Patel
Keyword(s):  
Pyridine Ring ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Biological Evaluation ◽  
Resonance Spectroscopy ◽  
Antituberculosis Activity ◽  
Aspergillus Clavatus ◽  
Pyrimidine Derivatives ◽  
In Vitro Antibacterial Activity

  Objective: Versatile biological activities of nitrogen containing heterocycles in medicinal chemistry, mainly pyrimidine and pyridine ring based heterocyclic moieties are very important. Pharmaceutical important of pyrimidine and isoniazid moiety prompted us to synthesize isoniazid clubbed pyrimidine derivatives and evaluated for antimicrobial and antituberculosis activity.Method: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) have been synthesized by condensation reaction of 2-chloro-N-[4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl] acetamide and N’-[(E)- (3-bromophenyl) methylidene]pyridine-4-carbohydrazide. All newly synthesized compounds were screened for in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus pyogenes, antifungal against Candida albicans, Aspergillus niger, and Aspergillus clavatus, and antituberculosis activity against Mycobacterium tuberculosis H37RV.Results: Majority of the compounds exhibited good antibacterial, antifungal, and antituberculosis activity. All titled compounds were characterized by spectral analyses (infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectroscopy).Conclusion: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) showed good antimicrobial activity and comparatively good antituberculosis activity. Hence, all the compounds of this series considered for future investigation mainly in area of antibacterial, antifungal study.

scholarly journals Facile synthesis of some 5-(3-substituted-thiophene)-pyrimidine derivatives and their pharmacological and computational studies

2021 ◽  
Vol 8 (4) ◽  
pp. 20218401
Author(s):  
S. H. Sukanya ◽  
Talavara Venkatesh ◽  
S.J. Aditya Rao ◽  
N. Shivakumara ◽  
Muthipeedika Nibin Joy
Keyword(s):  
In Silico ◽  
Energy Gap ◽  
Condensation Reaction ◽  
In Vitro Cytotoxicity ◽  
Bacterial Strains ◽  
Pyrimidine Derivatives ◽  
E Coli ◽  
Knoevenagel Condensation Reaction ◽  
In Silico Molecular Docking

A series of 5-(3-substituted-thiophene)-pyrimidine derivatives (3a-d) were synthesized via Knoevenagel condensation reaction in aq. ethanol using H2O2:HCl as a catalyst. Their pharmacological effects were evaluated. Analytical and spectroscopic methods confirmed the structures of the target molecules. The antibacterial activity studies revealed that compounds 3b and 3d exhibited the most effective zone of inhibition against bacterial strains E. coli and S. aureus, respectively. The in vitro cytotoxicity was carried out by MTT assay against MCF-7 cell line. The results showed excellent selectivity for all four compounds, among which the compound 3a exhibited remarkable cytotoxicity with a minimum cell viability range of 23.68 to 44.16%. The interaction of compounds with calf thymus DNA was determined using UV-absorption spectroscopy. The results confirmed that all the synthesized compounds interacted strongly with CT DNA through electrostatic or groove binding. In silico ADME-toxicology studies indicated that all the molecules under investigation are non-toxic with good oral bioavailability. The drug-likeness score indicated that they are suitable as drug-leads. In silico molecular docking the specified compound 3b bound with GlcN-6-P and P38 MAPk with a minimum binding energy of –7.9 and –6.4 kcal/mol, respectively. DFT study demonstrated that compound 3d was chemically and biologically more reactive due to less energy gap.

scholarly journals Facile synthesis, characterization, and cytotoxicity study of new 3-(indol-2-yl)bicyclotetrazatridecahexaens

2017 ◽  
Vol 95 (8) ◽  
pp. 858-862 ◽  
Author(s):  
Kamal Sweidan ◽  
Dima A. Sabbah ◽  
Sanaa Bardaweel ◽  
Ghassan Abu Sheikha ◽  
Tariq Al-Qirim ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Hct116 Cell ◽  
Chloroacetic Acid ◽  
Human Colon ◽  
Cytotoxic Activities ◽  
Human Skin Fibroblast ◽  
Normal Human Skin ◽  
H Nmr ◽  
Elemental Analyses

A new series of thiosemicarbazone-based indole derivatives 12–15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8–11 with thiosemicarbazide. The former compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16–19. These newly synthesized compounds have been characterized by means of FTIR, 1H NMR, 13C NMR, and HRMS and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibroblast, human colon carcinoma (HCT116), and leukemia (K562) cell lines; results revealed that the series inhibits only HCT116 cell line. In addition, results showed that compound 18 exerts moderate potency in HCT116 with an IC50 value of 54 μmol/L and significantly induces apoptosis.

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