scholarly journals Synthesis, Antimicrobial, and Anti-HIV1 Activity of Quinazoline-4(3H)-one Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
K. Vijayakumar ◽  
A. Jafar Ahamed ◽  
G. Thiruneelakandan
Keyword(s):  
Elemental Analysis ◽  
Mass Spectra ◽  
Product Yields ◽  
H Nmr ◽  
Wide Range ◽  
Quinazolinone Derivatives ◽  
C Nmr

The present investigation aims to synthesize 11 compounds of quinazoline-1 derivatives and to test their antimicrobial and anti-HIV1 activities. A quick-witted method was developed for the synthesis of novel substituted quinazolinone derivatives by summarizing diverse diamines with benzoxazine reactions, and it demonstrated the benefits of typical reactions, handy operation, and outstanding product yields. These compounds were confirmed by elemental analysis, I R, 1H NMR, 13C NMR, and mass spectra. Then antimicrobial and anti-HIV1 activities of the compounds were tested in-vitro. It was found that compounds 7–11 possessed a wide range of anti microbial and anti-HIV1 activity.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

The Synthesis and Anticancer Activities of Peptide 5-fluorouracil Derivatives

2009 ◽  
Vol 2009 (4) ◽  
pp. 261-264 ◽  
Author(s):  
Xiaowei Yan ◽  
Maolin Hu ◽  
Qian Miao ◽  
Shun Wang ◽  
Kejian Zhao
Keyword(s):  
Cell Lines ◽  
Mass Spectra ◽  
Anticancer Activities ◽  
H Nmr ◽  
Elemental Analyses ◽  
C Nmr

A new series of peptide 5-fluorouracil derivatives was designed and synthesised in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses.

scholarly journals Synthesis and Biological Activity of Some Novel 4-(5-Mercapto-1,3,4-thiadiazol-2-yl)-2-phenyl-5-[2-phenylvinyl]-2,4-dihydro-3H-1,2,4-triazol-3-one

2010 ◽  
Vol 7 (2) ◽  
pp. 545-550
Author(s):  
Kumar Sanjeev S. Lamani ◽  
Oblennavar Kortesh
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
Mass Spectra ◽  
Antimicrobial Properties ◽  
H Nmr ◽  
Efficient Route ◽  
C Nmr

A novel and efficient route have been designed for the synthesis of 4-(5-mercapto-1,3,4-thiadiazol-2-yl)-2-phenyl-5-[2-phenylvinyl]-2,4-dihydro-3H-1,2,4-triazol-3-one. All the synthesized compound were characterized by elemental analysis, IR,1H NMR,13C NMR and mass spectra. All the synthesized products were evaluated for their antibacterial activity againstB. SubtilisandE.Coliand antifungal activity againstA. nigerandC.Albicanrespectively. The results indicate that the present compounds may serve as better fungicides when compared to bactericides. The synthesized compounds have turned to be wonder by possessing antimicrobial properties.

scholarly journals Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Oluwole B. Familoni ◽  
Feipeng Wu ◽  
Johnbull O. Echeme ◽  
Zheng Sujiang
Keyword(s):  
Antibacterial Activity ◽  
Mass Spectra ◽  
Room Temperature ◽  
Biological Activities ◽  
Chemical Structures ◽  
Wide Range ◽  
Synthetic Routes ◽  
Mic Value ◽  
C Nmr

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

Synthesis, Characterization and Photophysicochemical Properties of Zinc(Ii) Phthalocyanine With New Benzenesulfonamide Derivative Substituents

2021 ◽  
Author(s):  
Gülen Atiye Öncül ◽  
Ömer Faruk Öztürk ◽  
Mehmet Pişkin
Keyword(s):  
Elemental Analysis ◽  
Mass Spectra ◽  
Spectroscopic Methods ◽  
H Nmr ◽  
Maldi Tof Mass Spectra ◽  
New Type ◽  
Ft Ir ◽  
Photochemical Properties ◽  
Photocatalytic Applications ◽  
C Nmr

Abstract Novel (E)-4-((5-bromo-2-hydroxy-3-methoxybenzylidene)amino)-N-(pyridin-2-yl)benzenesulfonamide 1, (E)-4-((5-bromo-2-(3,4-dicyanophenoxy)-3-methoxybenzylidene)amino)-N-(pyridin-2-yl)benzene sulfonamide 2 and 2(3),9(10),16(17),23(24)-tetra-[(E)-4-((5-bromo-3-methoxy-2-(λ1-oxidanyl)benzyl idene)amino)-N-(pyridine-2-yl)benzenesulfonamide]phthalocyaninato zinc(II) phthalocyanine 3 were synthesized. Their (1-3) structures were illuminated with spectroscopic methods such as FT-IR, 1H NMR,13C NMR, UV–vis, MALDI-TOF mass spectra and also elemental analysis. The spectroscopic, photophysical and photochemical properties of the zinc(II) phthalocyanine 3 were investigated in dimethyl sulfoxide and its effects on the above mentioned properties were reported as a result of containing new type benzenesulfonamide derivatives as substituents. In addition, its above-mentioned properties were reported by comparing different species with those of their substituted and/or unsubstituted counterparts. The zinc(II) phthalocyanine 3 has photosensitizing abilities suitable and sufficient especially for photocatalytic applications.

scholarly journals Synthesis, biological evaluation, and molecular docking of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5]tetrazin-6-yl) piperazin-1-yl)methyl) benzohydrazide derivatives

2020 ◽  
Vol 44 (9-10) ◽  
pp. 543-550
Author(s):  
Xiaoyu Wu ◽  
Feng Xu ◽  
Zhenzhen Yang ◽  
Zhonglu Ke ◽  
Lei Shi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antitumor Activity ◽  
Tumor Cells ◽  
Elemental Analysis ◽  
Biological Evaluation ◽  
Significant Inhibition ◽  
Antitumor Activities ◽  
H Nmr ◽  
C Nmr

A series of ((4-([1,2,4]triazolo[4,3- b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by 1H NMR, 13C NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC50 values of 5f (12 μM), 5h (7.1 μM), 6a (8.4 μM), and 6d (9.2 μM) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 μM), and the IC50 value of 6a (5.2 μM) exhibited better antitumor activity against Bewo than cisplatin (7.7 μM).

scholarly journals Synthesis, Characterization and Antibacterial Activity of Schiff Bases and their Metal Complexes Derived from 4-Acyl-1-phenyl-3-methyl-2-pyrazolin-5-ones and 2-Amino-4(4'-methylphenyl)-thiazole

2010 ◽  
Vol 7 (4) ◽  
pp. 1396-1406 ◽  
Author(s):  
A. S. Thakar ◽  
K. K. Singh ◽  
K. T. Joshi ◽  
A. M. Pancholi ◽  
K. S. Pandya
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Elemental Analysis ◽  
Mass Spectra ◽  
Nmr Spectra ◽  
Electrical Conductance ◽  
H Nmr ◽  
Infrared Spectral ◽  
Ft Ir ◽  
C Nmr

4-Acyl-1-phenyl-3-methyl-2-pyrazolin-5-ones condensed with 2-amino-4(4'-methylphenyl)-thiazole to form Schiff base. These Schiff bases from complexes of type ML22H2O (M=Mn, Fe, Co, Ni and Cu). Elemental analysis, magnetic susceptibility, electrical conductance, electronic and Infrared spectral data suggested octahedral structure for the complexes. All the compounds were tested for their antibacterial activity. The result indicates that the growth of the tested organism was inhibited by most of the compounds. These Schiff bases are characterized by elemental analysis, mass spectra,1H-NMR spectra,13C NMR spectra and FT IR spectra.

scholarly journals Synthesis and Anticancer Activity of 1-(1H-Indol-3-yl)-2-(4-diarylmethylpiperazine-1-yl)ethane-1,2-dione Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Jun-Rong Jiang ◽  
Feng Xu ◽  
Han-Gui Wu
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Elemental Analysis ◽  
Mass Spectra ◽  
Cancer Cell Lines ◽  
H Nmr ◽  
Antiproliferative Activities

Several new 1-(4-diarylmethylpiperazine-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione derivatives were synthesized by acylation of 1-diarylmethylpiperazine with 2-(1H-indol-3-yl)-2-oxoacetyl chloride. Their structures were confirmed by1H NMR, IR, mass spectra, and elemental analysis. These compounds were further evaluated for their anticancer activity, and most of them were found to have moderate-to-potent antiproliferative activities against Hela, A-549, and ECA-109 cancer cell linesin vitro.

scholarly journals Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

2016 ◽  
Vol 66 ◽  
pp. 109-118 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Malay J. Bhatt
Keyword(s):  
Mass Spectra ◽  
Solid Base ◽  
Base Catalyst ◽  
Solid Base Catalyst ◽  
Thiazole Derivatives ◽  
Spectra Analysis ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
C Nmr

A series of nitro pyrazole based thiazole derivatives compounds were synthesized by using solid base catalyst. The process was further optimized by setting up the solvent and catalyst ratio. The structures of these compounds were elucidated by spectral (IR, 1H NMR, 13C NMR, mass spectra) analysis. Synthesized compounds were screened for their in vitro antibacterial activity against the representative panel of Gram-positive (Staphylococcus aureus, Streptococcus pyogenes) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria. These compounds were tested for their inhibitory action against strains of fungi (Candida albicans, Aspergillusniger, Aspergillusclavatus).

Synthesis of 2-amino-5,7-dimethyl-4-oxopyrido[3,4-e]-1,3-thiazines

1983 ◽  
Vol 48 (12) ◽  
pp. 3426-3432 ◽  
Author(s):  
Dušan Koščík ◽  
Pavol Kristian ◽  
Ondrej Forgáč
Keyword(s):  
Spectral Data ◽  
Chlorine Atom ◽  
Mass Spectra ◽  
High Reactivity ◽  
Secondary Amines ◽  
Dimroth Rearrangement ◽  
H Nmr ◽  
New Synthesis ◽  
C Nmr

New synthesis of pyrido[3,4-e]-1,3-thiazines consisting in reaction of 2,6-dimethyl-4-chloronicotinoyl isothiocyanate with primary or secondary amines, or with benzaldehyde phenylhydrazone, is described. High reactivity of the chlorine atom does not allow isolation of the corresponding thioureas, arising as intermediates, except in the case of the benzylamino derivative. Structure of the products was unequivocally confirmed by their spectral data (IR, UV, 1H NMR, 13C NMR and mass spectra). The synthesized derivatives do not undergo the Dimroth rearrangement.

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