Synthesis, Antimicrobial and β-Lactamase Enzyme Inhibition Activity of Some New Tetrazole Containing Maleamic and Phthaleamic Acid Derivatives

2019 ◽  
Vol 4 (3) ◽  
pp. 166-173
Author(s):  
Bhaurao P. Sathe ◽  
Harshal S. Oman ◽  
Naziya N.M.A. Rehman ◽  
Prashant P. Dixit ◽  
Arun S. Kharat ◽  
...  

In the present study, two series of tetrazole containing maleamic (5a-h) and phthaleamic acid (5i-l) derivatives were synthesized and evaluated for their antimicrobial and β-lactamase enzyme inhibition activities. The synthesized compounds were characterized by IR, 1H NMR and 13C NMR spectral techniques. Among the screened compounds, the compound 5c, 5d, 5e, 5f, 5g and 5h have shown good antimicrobial activity. We further performed exploratory β-lactamase enzyme inhibitors studies on β-lactamase.

2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.


2008 ◽  
Vol 73 (7) ◽  
pp. 683-690 ◽  
Author(s):  
Dipti Dodiya ◽  
Amit Trivedi ◽  
Samir Jarsania ◽  
Shailesh Vaghasia ◽  
Viresh Shah

The synthesis of substituted pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidin-8-ones (IIIa-j) from 5-amino-3-methyl-1H-thieno[3,2-c]pyrazole-6-carbonitrile (II) is described. The key compound II was synthesized from (5-methyl- -2,4-dihydro-3H-pyrazol-3-ylidene)malononitrile I via the Gewald reaction. The synthesis of the title compounds IIIa-j was accomplished by condensation of II with different aromatic aldehydes. The newly synthesized heterocyles were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectroscopic investigation. All the newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains. .


2014 ◽  
Vol 10 (7) ◽  
pp. 2937-2943
Author(s):  
Nambinina V. Rakotoarivelo ◽  
Ennaji Najahi ◽  
Pierre Perio

A novel series of isoindolinotriazole derivatives with different substituents in the triazole moiety were synthesized via copper-catalyzed cycloaddition (CuAAC) click chemistry between 2-(meta- or para-ethynylphenyl)-4,6-dimethoxyisoindolin-1-ones and several azides. The synthesized triazoles were characterized by IR, 1H NMR, 13C NMR and mass spectral techniques.


2010 ◽  
Vol 9 (3) ◽  
pp. 487-490
Author(s):  
Weny Musa ◽  
Hersanti Hersanti ◽  
Achmad Zainuddin ◽  
Roekmi-ati Tjokronegoro

The poriferasta-5.22E.25-trien-3β-ol compound of leaves of this plant Clerodendrum paniculatum has activity as an inducer agent of plant systemic resistance of red plant toward Cucumber Mosaic Viruses (CMV), the inhibition activity compound shows 82% inhibition activity at 300 ppm. The structure of these compound were determined on the basis of spectroscopic data including UV, IR, 1H-NMR, 13C-NMR and 2D-NMR   Keywords: Poriferasta-5.22E.25-trien-3β-ol, Clerodendrum paniculatum, induction of systemic resistance, CMV


2021 ◽  
Vol 6 (3) ◽  
pp. 211-216
Author(s):  
Vidhya V. Jadvani ◽  
Yogesh T. Naliapara

A series of novel (E)-4-(4-(3,3-dimethyltriaz-1-en-1-yl)phenyl)-N-phenylpyrimidin-2-amine derivatives have been synthesized from the condensation of (E)-3-(dimethylamino)-1-(4-(E)-3,3-dimethyltriaz- 1-en-1-yl)phenyl)prop-2-en-1-one with several guanidinium hydro-chloride. The newly synthesized compounds were examined for in vitro antimicrobial activity against some antibacterial and fungal strains. The synthesized compounds were characterized by 1H NMR, 13C NMR, IR, mass and elemental analyses.


2011 ◽  
Vol 76 (1) ◽  
pp. 1-11 ◽  
Author(s):  
Surendra Kumar ◽  
A. Idhayadhulla ◽  
Abdul Nasser ◽  
J. Selvin

A series of 1,4-dihydropyridine derivatives (1a-g) were prepared from Hantzsch syntheses. The compounds (1a-g) were reacted with thiosemicarbazide to give the new series of compounds (2a-g). IR, 1H-NMR, 13C-NMR, mass spectral and elemental analysis confirmed the synthesized compounds. The synthesized compounds were also screened for their antimicrobial activity.


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.


Molbank ◽  
10.3390/m1019 ◽  
2018 ◽  
Vol 2018 (3) ◽  
pp. M1019
Author(s):  
Afzal Shaik ◽  
Mahamuda Shaik ◽  
Srinivasa Puttagunta

Thiazole and chalcone motifs are of research interest to medicinal chemists due to their array of synthetic and biological utility. Hence, in the present study we intended to prepare (E)-1-(2′,4′-dimethyl)-(5-acetylthiazole)-(2,4″-difluorophenyl)-prop-2-en-1-one (3c) containing both these scaffolds. The compound 3c was synthesized by the acid-catalyzed condensation of 2,4-dimethyl-5-acetylthiazole with 2,4-difluorobenzaldehyde. Purification and characterization of the compound were carried out by recrystallization and spectral techniques including UV, IR, 1H-NMR, 13C-NMR, Mass spectrometry and X-ray powdered diffractometry. The molecule 3c was successfully synthesized, purified, and characterized.


2020 ◽  
Vol 17 ◽  
Author(s):  
Mehri Abdollahi fard ◽  
Mohammadreza Manafi ◽  
Manijeh Motevalian ◽  
Seyed Saied Homami

Abstract: In this paper, a novel series of 1-(alkyl)-3-(2-oxo-2H-chromenyloxy acetamido) methylpyridinium salts were syn-thesized in a simple and efficient way. The method showed to be facile and the compounds were obtained in high isolated yields. All the synthesized compounds were characterized by 1H NMR, 13C NMR, FT-IR, Mass and elemental analysis. AChE and BuChE inhibition activity of the synthesized compounds were evaluated and the results showed that, all the com-pounds were active in the inhibition of the mentioned enzymes. All the compounds were active in the inhibition of the two studied enzymes. Among all the compounds, the compound 6a (1.85 μM) and 6i (0.106 μM) showed the highest inhibition activity against AChE and BuChE, respectively. The kinetic study was performed to get more insight into the mechanism of action of the synthesized compounds. Docking studies were also performed to obtain the interactions between the synthe-sized compounds and the enzymes.


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