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

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.

Author(s):  
Prakash Mehta ◽  
Prakash Davadra ◽  
Nirav Shah ◽  
Hitendra Joshi

In this study some new o-benzimidazol-2'-yl-benzamido-p'-benzamido-2-phenyl-4-substituted phenyl-5-oxo-Imidazolines 3a-3j were synthesized. To synthesized target molecules we used various substituted oxazolone derivatives, synthesized from substituted benzaldehyde with hippuric acid. Substituted oxazolones 2a-2j were reacted with carbohydrazide derivative of benzimidazole 1 in presence of pyridine as base to obtained substituted imidazolinone derivatives. All synthesized compounds were characterized by IR, 1H NMR, elemental analysis and further supported by mass spectroscopy. All synthesized compounds were screened for their antimicrobial activity against gram positive and gram negative bacteria which showed moderate to good activity. All compounds showing good to moderate active against fungal strain as compare to standard drug.


2015 ◽  
Vol 80 (3) ◽  
pp. 305-313 ◽  
Author(s):  
Dongamanti Ashok ◽  
Bommidi Lakshmi ◽  
Sidda Ravi ◽  
Arram Ganesh

A series of pyrazolines 4a-g have been synthesized by Michael addition of chalcones 3a-g with hydrazine hydrate in presence of sodium acetate under conventional heating and microwave irradiation. Structures of the newly synthesized chalcones 3a-g and pyrazolines 4a-g have been established on the basis of IR, 1H & 13C NMR and mass spectral data. All the synthesized compounds were screened for their antimicrobial activity. Some of the compounds shown very good activity compared to standard drugs against all pathogenic bacteria and fungi.


Author(s):  
Saras Kumar Jain ◽  
Rohit Singhal ◽  
Neetesh K. Jain

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.


2010 ◽  
Vol 7 (4) ◽  
pp. 1320-1325
Author(s):  
A. Jamal Abdul Nasser ◽  
A. Idhayadhulla ◽  
R. Surendra Kumar ◽  
J. Selvin

Series of newly prepared 3-{[2,6-bis(4-substituted phenyl)-1- methylpiperidin-4- ylidene] amino}- 2-thioxo-imidazolidin-4-one derivatives (3a-3f) have been synthesized by the cyclization of compound (2a-2f), ethyl chloro acetate and fused sodium acetate. The chemical structures were confirmed by IR,1H NMR and elemental analysis. The synthesized compounds were screened for their antimicrobial activity against four antibacterial and four antifungal organisms.


2011 ◽  
Vol 396-398 ◽  
pp. 241-245
Author(s):  
Yu Ting Liu ◽  
Ming Tao Zhao ◽  
Da Wei Yin ◽  
Bo Ning Hui

A series of novel Schiff base containing diacetylferrocene and 5-alkyl-2-amino-1,3,4 -thiodizoles were reported in this paper. Diacetylferrocene(Ⅱ) was synthesised with ferrocene(Ⅰ) and acetyl chloride with AlCl3 as catalyst in CH2Cl2. In the presence of diacetylferrocene and 5-alkyl-2-amino-1,3,4-thiodizole reacted under solvent and catalyst condition to furnish Schiff base containing diacetylferrocene and 5-alkyl-2-amino-1,3,4-thiadiazoles(Ⅲ). Chemical structures have been confirmed by elemental annalysis and the spectral techniques of FTIR,1H NMR. Antimicrobial activity (in vitro) was evaluated against the two pathogenic bacterial strains. The compounds have shown better activity.


2010 ◽  
Vol 7 (1) ◽  
pp. 614-620
Author(s):  
Baghdad Science Journal

This search reports the synthesis of some new series of Schiff base compounds for trimetheprim derivatives which known high been known as a medicinal effectiveness. Trimetheprim was condensed with several substituted aldehydes compounds.(4-dimethyl amine benzaldehyde , propanal , salicaldehyde, 2.4 dimethoxy benzaldehyde and 4- methyl benzaldehyde) to obtain Schiff base products(1a-5a) and several substituted ketones compound (4-aminoacetophenone,4-chloroacetophenone, isobutyleketone, acetylacetone and acetophenone) to obtain Schiff base products(6b-10b) in ethanol in the presence of concentrated sulphuric acid as a catalyst to yield the Schiff base. The structure of synthesized compounds has been established on the basis of their Chemical structures of all products were confirmed by spectrophotometric methods such as U.V. visible and FTIR.. All these compounds were evaluated for their antibacterial activity in vitro against Gram + ve bacteria (bacillus) , Gram –ve bacteria (E-Coli).Most Compound under investigation exhibited potent antibacterial activity


1991 ◽  
Vol 56 (11) ◽  
pp. 2362-2372 ◽  
Author(s):  
Rajeshwar Singh ◽  
Maya P. Singh ◽  
Ronald G. Micetich

Various products from the oxidation of 3-heteroarylthiomethyl-ceph-3-ems using m-chloroperbenzoic acid (m-CPBA) and hydrogen peroxide in acetic acid in varying stoichiometric ratios have been isolated, identified and their in vitro antimicrobial activity determined. The oxidized compounds with the 2-aminothiazol-4-yl-(Z)-2-methoxyiminoacetamido side chain showed better antibacterial activity against various Gram negative bacteria compared to the unoxidized compounds.


2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Christiana Nonye Igwe ◽  
Uchechukwu Chris Okoro

The synthesis and biological activity of N-heteroaryl substituted benzene sulphonamides (3a–h) were successful. Simple condensation reaction of benzene sulphonyl chloride (1) with substituted heteroaromatic compounds (2a–h) under dry pyridine and acetone gave the target molecules (3a–h) in good to excellent yield. The compounds were characterized using FTIR, 1HNMR, and 13CNMR. The compounds were screened for antibacterial activity against E. coli, Salmonella typhi, P. aeruginosa, B. cereus, K. pneumonia, and Sarcina  lutea and antifungal activity against C. albicans and A. niger. The results of the antimicrobial activity showed improved biological activity against some tested organisms.


2008 ◽  
Vol 59 (1) ◽  
pp. 41-44
Author(s):  
Maria-Daniela Sofei ◽  
Maria Ilici ◽  
Valentin Badea ◽  
Carol Csunderlik ◽  
Vasile-Nicolae Bercean

The synthesis of 1H-3-aryl-7-ethoxycarbonyl-6-methyl-pyrazolo[5,1-c][1,2,4]triazoles (2) was carried out by cyclization of 1H-5-arylidenehydrazino-4-ethoxycarbonyl-3-methyl-pyrazoles (1) in the presence of bromine using glacial acetic acid as solvent and sodium acetate as base. The new nine obtained compounds were characterized by IR and NMR spectroscopy and mass spectrometry.


2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  

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.


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