Synthesis, characterization and biological activity of Pyrazoline derivatives

2021 ◽  
pp. 6223-6227
Author(s):  
Saras Kumar Jain ◽  
Rohit Singhal ◽  
Neetesh K. Jain
Keyword(s):  
Crystal Structure ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Biological Activity ◽  
Spectroscopic Data ◽  
Glacial Acetic Acid ◽  
Retardation Factor ◽  
Physical Parameters ◽  
Pyrazoline Derivative

Pyrazoline is dihydropyrazole having only one endocyclic double bond. Synthesis of pyrazoline derivatives from chalcones is an active arena of investigation due to established pharmacological result. In present study, chalcones were prepared by reacting of acetophenone with benzaldehyde. Then prepared chalcones react with isoniazid in the presence of glacial acetic acid results pyrazoline derivative. Physical parameters such as color, crystal structure, solubility, melting point, retardation factor (Rf) and % yield was evaluated. Confirmations of structures of all synthesized derivatives, were done by spectroscopic data of IR, 1HNMR and Mass spectroscopy. Also, all synthesized compounds were evaluated for antibacterial activity against B. subtilis, S. aureus, P.aeruginosa and E.coli, and antifungal activity was accomplished against C. albicans and A. niger at the different conc. and concluded that some compounds have excellent antimicrobial activity and most of the synthesized compounds exhibits moderate antimicrobial activity.

Complexes of Cu (II) with a-Ketoglutaric Acid and 1- (o-tolyl) Biguanide Synthesis, characterization and biological Activity

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Copper Complexes ◽  
Substrate Adhesion ◽  
Inert Substrate

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.

Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity

2020 ◽  
Vol 17 (5) ◽  
pp. 396-403
Author(s):  
Nalla Krishna Rao ◽  
Tentu Nageswara Rao ◽  
Botsa Parvatamma ◽  
Y. Prashanthi ◽  
Ravi Kumar Cheedarala
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Sodium Acetate ◽  
Good Activity ◽  
Activity Profile ◽  
Aryl Aldehydes ◽  
Chemical Structures ◽  
Novel Synthesis ◽  
Target Molecules

Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. Objective: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. Methods: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. Results: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. Conclusion: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.

scholarly journals Synthesis and Prognosis of Anti-inflammatory Activity of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3h)-one

2021 ◽  
Vol 7 (12) ◽  
pp. 25-33
Author(s):  
A. Chiriapkin ◽  
I. Kodonidi ◽  
A. Ivchenko ◽  
L. Smirnova
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Dimethyl Sulfoxide ◽  
In Silico ◽  
Glacial Acetic Acid ◽  
Inflammatory Activity ◽  
Modified Method ◽  
Anti Inflammatory ◽  
Catalytic Addition ◽  
Derivatives Of

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

scholarly journals Synthesis and Antimicrobial Activities of Some New Synthesized Imide and Schiff's Base Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Nermien M. Sabry ◽  
Eman M. Flefel ◽  
Mohamed A. Al-Omar ◽  
Abd El-Galil E. Amr
Keyword(s):  
Acetic Acid ◽  
Fusidic Acid ◽  
Spectroscopic Data ◽  
Glacial Acetic Acid ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Schiff’S Bases ◽  
Schiff’S Base ◽  
Antimicrobial Screening ◽  
Positive Controls

A series of 2,6-bis(substituted thiazolopyrimi-dinyl) pyridine(2a,b)and corresponding Schiff's bases(3a–j)were synthesized from 2,6-bis-(3-amino-2-methyl-4-oxo-9-substituted-3,4-dihydropyrido-[30,20 : 4,5]-thieno[3,2-d]pyrimidin-7-yl)pyridines(1a,b)as starting materials. The compounds1a,bwere reacted with 2,3,4,5-tetrachlorophthalic anhydride in glacial acetic acid to give the corresponding bis-imides(2a,b). But they are treated with aromatic aldehydes in refluxing ethanol to afford the Schiff’s base derivatives(3a–j). The antimicrobial screening showed that many of these newly synthesized compounds had good antimicrobial activities comparable to streptomycin and fusidic acid as positive controls. The detailed synthesis, spectroscopic data, and antimicrobial activities of the synthesized compounds were reported.

scholarly journals Synthesis and Biological Evaluation of Some Novel 1, 3, 5-Trisubstituted Pyrazolines

2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Spectral Data ◽  
Glacial Acetic Acid ◽  
Biological Evaluation ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Synthesis And Biological Evaluation

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.

scholarly journals Synthesis of Bioactive Fluorinated 10H-Phenothiazines and their Sulfone Derivatives

2008 ◽  
Vol 5 (s1) ◽  
pp. 1063-1068 ◽  
Author(s):  
Yogesh Dixit ◽  
Rahul Dixit ◽  
Naveen Gautam ◽  
D. C. Gautam
Keyword(s):  
Hydrogen Peroxide ◽  
Acetic Acid ◽  
Spectroscopic Data ◽  
Halogen Atom ◽  
Glacial Acetic Acid ◽  
Present Communication ◽  
Smiles Rearrangement ◽  
Antimicrobial Studies ◽  
Sulfone Derivatives

The present communication deals with the synthesis of a series of fluorinated 10H-phenothiazines. 10H-phenothiazines is prepared by Smiles rearrangement of substituted 2-foramido-2´-nitrodiphenylsulfide. Substituted 2-foramido-2´-nitrodiphenylsulfide were obtained by the reaction of 2-amino-3-fluorobenzenethiol witho-halonitrobenzenes followed by formylation and 1-nitro/1-halo-10H-phenothiazines have been prepared by the reaction of substituted 2-aminobenzenethiols with reactiveo-halonitrobenzene containing a nitro group or halogen atom ato-position to the reactive halogen atom directly yielded 1-nitro/1-halo-10H-phenothiazines in situ. 10H-phenothiazine sulfone derivatives have been synthesized by the oxidation of 10H-phenothiazines by 30% hydrogen peroxide in glacial acetic acid. The structure of the synthesized compounds has been characterized by spectroscopic data and elemental analysis. Antimicrobial studies of the synthesized compounds have also been included.

scholarly journals Complexes of Cu (II) with a-Ketoglutaric Acid and 1- (o-tolyl) Biguanide Synthesis, characterization and biological Activity

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Copper Complexes ◽  
Substrate Adhesion ◽  
Inert Substrate

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: Cl (C1), •H2O (C2) and (NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications. Keywords: 1-(o-tolyl)biguanide, a-ketoglutaric acid, copper complexes, antibacterial activity, celule HeLa, antifungal activity

scholarly journals Synthesis and Biological Activity of 1,2,4-Triazolo-[3,4-b]Thiadiazole as Antimicrobial Agents

2014 ◽  
Vol 26 ◽  
pp. 45-52
Author(s):  
Piyush B. Vekariya ◽  
Jalpa R. Pandya ◽  
Vaishali Goswami ◽  
Hitendra S. Joshi
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Spectral Analysis ◽  
Biological Activity ◽  
Antimicrobial Agents ◽  
Dilution Method ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
Broth Dilution

Some novel 6-fluoro chroman derivatives having 1,2,4-triazolo-[3,4-b]thiadiazole were synthesized and characterized by IR, NMR and mass spectral analysis. All synthesized compounds were screened for antimicrobial activity using broth dilution method. All the compounds showed good antimicrobial activity and compound 5e showed significant antibacterial activity.

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