Synthesis of Nitro-Substituted 4-Oxo-4H-pyrimido[2,1-b]benzothiazole-3-carboxylic Acids and Their Spectral Characteristics

1995 ◽  
Vol 60 (4) ◽  
pp. 583-593 ◽  
Author(s):  
Alexander Bartovič ◽  
Dušan Ilavský ◽  
Ondrej Šimo ◽  
Lubomír Zalibera ◽  
Anna Belicová ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acids ◽  
Elemental Analysis ◽  
Nmr Spectra ◽  
Spectral Characteristics ◽  
C Nmr

The Gould-Jacobs reaction of all position isomeric 2-aminonitrobenzothiazoles II with diethyl ethoxy- methylenemalonate has been studied. The structure of substitution (IV) and cyclization (VI) products and of the corresponding acids (VIII) was confirmed by elemental analysis, IR, UV, 1H and 13C NMR spectra. Analogous derivatives III, V and VII, derived from the unsubstituted 2-aminobenzothiazole I, were used as standards in interpretation of the spectra. The synthesized derivatives I - VIII were tested for antimicrobial 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>

Pteridines, XCVI. Synthesis and Reactions of 6-(1,2,3-Trihydroxypropyl)pteridines

Pteridines ◽  
1990 ◽  
Vol 2 (2) ◽  
pp. 63-74 ◽  
Author(s):  
Rainer Soyka ◽  
Wolfgang Pfleiderer
Keyword(s):  
Folic Acid ◽  
Carboxylic Acids ◽  
Elemental Analysis ◽  
Nmr Spectra ◽  
Periodate Oxidation ◽  
Pteridine Derivatives

Summary Various hydropyrano [3.2-g] pteridines (7, 10, 12, 21 , 33) were oxidized to the corresponding 6-(1,2,3- trihydroxypropyl)pteridine derivatives (8,9, 11, 13,32, 34), which are valuable intermediates for the synthesis of new 6-substituted pteridines (15 - 46). Periodate oxidation led to pteridine-6-carboxaldehydes (15, 16, 17, 38), which easily formed oximes (19 - 22, 39, 40). The aldehydes were further oxidized to 6-carboxylic acids (25,26,42) or reduced to 6-hydroxymethyl derivatives (27, 28, 43). Reductive condensations of the aldehydes (15, 16, 38) with p-aminobenzoylglutamic acid afforded folic acid analogues (29, 30, 44). Dehydration of the oximes (19, 20, 39) resulted in the formation of 6-carbonitriles (23, 24, 41, 46). The newly synthesized compounds were characterized by elemental analysis and by UV and NMR spectra.

Bicyclo[2.2.2]octane-2-spirocyclohexanes, Part 4. Birch Reduction of Spirodiisophor-6-ones

1992 ◽  
Vol 47 (4) ◽  
pp. 579-588 ◽  
Author(s):  
Frederick Kurzer ◽  
Zakir Kapadia
Keyword(s):  
Nmr Spectra ◽  
Liquid Ammonia ◽  
Spectral Characteristics ◽  
Keto Group ◽  
Secondary Alcohols ◽  
Hydroxy Compound ◽  
Sodium Bisulphite ◽  
Birch Reduction ◽  
C Nmr

Birch reduction of spirodiisophorones by sodium in liquid ammonia - t-butanol reduces their normally inert 6-keto-group, producing the corresponding secondary alcohols, the 6-hydroxygroup of which assumes the endo- or exo-configuration. 3´-Oximinospirodiisophor-6-one is converted predominantly into the 6-endo-hydroxy-compound , from which the 3´,6-endo-ketol is obtainable by the action of sodium bisulphite. 3´-eq(and ax)-Hydroxyspirodiisophor-6-one each yield a pair of stereoisomeric 3´,6-diols, distinguished by their spectral characteristics and derivatives. Spirodiisophora-3´,6-dione yields a mixture of the same four diols, three of which are isolable in low yield. The structure of selected compounds is correlated with their assigned 13C NMR spectra.

scholarly journals Nanoparticles of novel organotin(IV) complexes bearing phosphoric triamide ligands

2013 ◽  
Vol 4 ◽  
pp. 94-102 ◽  
Author(s):  
Zahra Shariatinia ◽  
Ebadullah Asadi ◽  
Vahid Tavasolinasab ◽  
Khodayar Gholivand
Keyword(s):  
Fluorescence Spectroscopy ◽  
Elemental Analysis ◽  
Nmr Spectra ◽  
Fluorescence Spectra ◽  
Sem Micrographs ◽  
H Nmr ◽  
Phosphoric Triamide ◽  
C Nmr

Four novel organotin(IV) complexes containing phosphoric triamide ligands were synthesized and characterized by multinuclear (1H, 31P, 13C) NMR, infrared, ultraviolet and fluorescence spectroscopy as well as elemental analysis. The 1H NMR spectra of complexes 1–4 proved that the Sn atoms adopt octahedral configurations. The nanoparticles of the complexes were also prepared by ultrasonication, and their SEM micrographs indicated identical spherical morphologies with particles sizes about 20–25 nm. The fluorescence spectra exhibited blue shifts for the maximum wavelength of emission upon complexation.

scholarly journals Synthesis, antimicrobial activity, urease inhibition and molecular docking studies of new proline linked thiourea derivatives

2020 ◽  
Vol 65 (9) ◽  
pp. 783-788
Author(s):  
Ahmad RAHEEL ◽  
◽  
Imtiaz-Ud DIN ◽  
Syed Hassan IFTIKHAR ◽  
Muhammad Babar TAJ ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Carboxylic Acids ◽  
Elemental Analysis ◽  
Binding Mode ◽  
Docking Studies ◽  
Urease Inhibition ◽  
Thiourea Derivatives ◽  
Molecular Docking Studies ◽  
Docking Simulations

A series of new thiourea based carboxylic acids (Ia-Ie) were synthesized and characterized by elemental analysis, FTIR and NMR (1 H and 13C) spectroscopy. They were preliminary bioassayed for their antibacterial, anifungal and urease inhibition activities. Molecular docking simulations were carried out to determine the probable binding mode of the synthesized compounds. The bioassay results showed that some of titled compounds exhibited encouraging results.

Preparation and properties of 2-(dialkylaminomethyl)cyclohexyl and 2-(dialkylaminomethyl)phenyl carbanilates

1990 ◽  
Vol 55 (7) ◽  
pp. 1854-1865 ◽  
Author(s):  
Alena Brádlerová ◽  
Nadežda Prónayová ◽  
Eva Mišíková ◽  
Ján Ďurinda
Keyword(s):  
Acute Toxicity ◽  
Elemental Analysis ◽  
Local Anaesthetic ◽  
Nmr Spectra ◽  
Analysis And Evaluation ◽  
C Nmr

A series of 2-(dialkylaminomethyl)cyclohexyl and 2-(dialkylaminomethyl)phenyl esters of substituted carbanilic acid have been prepared and their identity verified by elemental analysis and evaluation of IR and 13C NMR spectra. The spectral results have been used also for determination of isomerism of the starting 2-dialkylaminomethylcyclohexanols and final carbanilates. Local anaesthetic activity and acute toxicity have been tested with some of the substances.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity Studies of Ni(II) Complex with Pyridine as a Ligand

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Faridul Islam ◽  
Md. Amran Hossain ◽  
Nur Mostaq Shah ◽  
Hridika Talukder Barua ◽  
Md. Alamgir Kabir ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Nmr Spectra ◽  
Conductivity Measurement ◽  
Molar Conductivity ◽  
Molecular Formula ◽  
H Nmr ◽  
Square Planar ◽  
Elemental Analyses ◽  
Prepared Complex ◽  
C Nmr

We represent a metal complex which has been synthesized by the simple reaction with Ni(II) chloride and pyridine (as a lignd) affording a complex having the molecular formula [NiC5H5N2Cl2], characterized on the basis of elemental analyses, electronic, infrared,1H NMR,13C NMR spectra, magnetic susceptibility, and also aid of molar conductivity measurement. Conductivity measurement reveals nonelectrolytic nature of the complex. IR and13C NMR spectra reveal the presence ofcis- andtrans-structure. On the basis of above analyses the square planarcis- andtrans-structures are proposed for the prepared complex.

scholarly journals Synthesis and Evaluation of Some Novel Chromone Based Dithiazoles as Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naureen Aggarwal ◽  
Vishal Sharma ◽  
Harpreet Kaur ◽  
Mohan Paul Singh Ishar
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Fungal Strains ◽  
Inhibitory Potential ◽  
C Nmr

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

scholarly journals Synthesis and Antimicrobal Activities of some Novel Triazolo[1,5-a]Pyrimidine Derivatives

2014 ◽  
Vol 30 ◽  
pp. 127-134 ◽  
Author(s):  
Sagar P. Gami ◽  
Kalpesh V. Vilapara ◽  
Hasmukh R. Khunt ◽  
Jayesh S. Babariya ◽  
Yogesh T. Naliapara
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Sodium Methoxide ◽  
Pyrimidine Derivatives ◽  
Ketene Dithioacetals ◽  
Convenient Synthesis ◽  
Bacteria And Fungi ◽  
C Nmr

A convenient synthesis of substituted 1,2,4-triazolo[1,5-a]pyrimidine was carried out by the reaction of various ketene dithioacetals with 5-amino 1,2,4-triazole in methanol in presence of sodium methoxide. The newly synthesized compound were characterized by 1H NMR, 13C NMR, IR, MS, elemental analysis and screened for their antimicrobial activity against various strains of bacteria and fungi.

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.

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