scholarly journals Synthesis and Antibacterial, Antimycobacterial Activity of 7-[4-{5-(2-Oxo-2-p-substituted-phenylethylthio)-1,3,4-thiadiazol-2yl}-3′-methylpiperazinyl] Quinolone Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Kapil M. Agrawal ◽  
Gokul S. Talele
Keyword(s):  
Biological Activities ◽  
Antimycobacterial Activity ◽  
Bacterial Strains ◽  
Mass Spectral ◽  
H Nmr ◽  
Mass Spectral Study ◽  
Weak Activity ◽  
Fluoroquinolone Derivatives ◽  
Quinolone Derivatives ◽  
C Nmr

Currently we screened 9 newer synthesized fluoroquinolone derivatives5(a–i)against two gram positive, two gram negative bacterial strains, and mycobacterium tuberculosis H37Rv. These analogues were confirmed by IR,1H NMR,13C NMR, and elemental analysis. Selected compounds were confirmed by mass spectral study. Compounds5(b–d)showed comparable biological activities and other analogues of the series showed moderate-to-weak activity, as compared to the reference marketed drugs.

scholarly journals Synthesis of (E)-(4-(Aryl)phenyl)(3-(2-(1-phenyl-3-(thiophen-2-yl)-1Hpyrazol-4-yl)vinyl)benzofuran-2-yl)methanones by Claisen Schmidt-Suzuki Cross Coupling and their Antibacterial and Antifungal Activity

2017 ◽  
Vol 61 (3) ◽  
Author(s):  
Ashok Dongamanti ◽  
Mohammad Ziauddin ◽  
Bommidi Vijaya Lakshmi ◽  
Madderla Sarasija
Keyword(s):  
Antifungal Activity ◽  
Coupling Reaction ◽  
Cross Coupling ◽  
Bacterial Strains ◽  
Mass Spectral ◽  
H Nmr ◽  
Cross Coupling Reaction ◽  
Antibacterial And Antifungal ◽  
C Nmr

A series of ten novel (<em>E</em>)-(4-(aryl)phenyl)(3-(2-(1-phenyl-3- (thiophen-2-yl)-1<em>H</em>-pyrazol-4-yl)vinyl)benzofuran-2-yl)methanones (<strong>7a-j</strong>) derivatives were prepared by traditional Claisen-Schmidt and Suzuki cross-coupling reaction under conventional and microwave irradiation conditions. The structures of all the newly synthesized compounds were established on the basis of FTIR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, mass spectral data and elemental analysis. The products were assayed for their <em>in vitro</em> antibacterial activity against different types of bacterial strains. Further the antifungal activity was examined by inhibitory action against three fungal strains such as <em>Aspergillus niger</em>, <em>Aspergillus flavus</em> and <em>Fusarium oxysporum</em>.

scholarly journals Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency

2016 ◽  
Vol 66 ◽  
pp. 1-12 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Tushar J. Karkar
Keyword(s):  
Antimicrobial Activity ◽  
Synthesis And Characterization ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Broth Dilution ◽  
C Nmr

The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR,1H NMR,13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against selected fungal strains.

scholarly journals Synthesis, Antibacterial and Antioxidant Evaluation of Novel 1-(5,7-Dichloro-1,3-benzoxazol-2-yl)-1H-pyrazolo[3,4-b]quinoline Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
N. D. Jayanna ◽  
H. M. Vagdevi ◽  
J. C. Dharshan ◽  
T. R. Prashith Kekuda
Keyword(s):  
Antibacterial Activity ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Spectral Studies ◽  
Quinoline Derivatives ◽  
Mass Spectral ◽  
H Nmr ◽  
Antioxidant Evaluation ◽  
Target Molecules ◽  
C Nmr

Some novel 1-(5,7-dichloro-1,3-benzoxazol-2-yl)-1H-pyrazolo[3,4-b]quinoline derivatives8(a–f) were synthesized by reacting 5,7-dichloro-2-hydrazino-1,3-benzoxazole4and substituted-2-chloro-3-quinoline carbaldehydes usingp-toluenesulfonic acid (PTSA) as a catalyst for the cyclisation. The target molecules have been characterized by IR,1H NMR,13C NMR, and mass spectral studies. The synthesized compounds were screened for biological activities, and some of the compounds have exhibited encouraging antibacterial and antioxidant activities. The compounds8aand8eshowed potent antibacterial activity, whereas the compounds8eand8fact as antioxidants.

Triazolopyridine nucleosides. II. Glycosylations of 3-oxo-s-triazolo[4,3-a]pyridines with accompanying conversions into 2-oxo-s-triazolo[1,5-a]pyridine nucleosides

1977 ◽  
Vol 55 (5) ◽  
pp. 831-840 ◽  
Author(s):  
Brian Maurice Lynch ◽  
Suresh Chandra Sharma
Keyword(s):  
General Structure ◽  
Spectroscopic Properties ◽  
Mass Spectral Fragmentation ◽  
Mass Spectral ◽  
H Nmr ◽  
Pyridine Nitrogen ◽  
Methyl Derivatives ◽  
Fragmentation Patterns ◽  
Ribose Moiety ◽  
C Nmr

3-Oxo-s-triazolo[4,3-a]pyridine and various C-methyl derivatives (general structure 1) have been converted into the 2-β-D-ribofuranosyl species 2 and thence 4 via Friedel–Crafts catalyzed reaction with tetra-O-acetyl-β-D-ribofuranose, followed by deblocking. During the course of these reactions, rearrangements into the isomeric 3-β-D-ribofuranosyl-2-oxo-s-triazolo[1,5-a]-pyridines occur through ring-opening of the pyridine rings yielding species 3 and 5. The proportion of rearrangement products is dependent upon the position and number of the C-methyl substituents.Structural assignments for these compounds are based upon comparisons of spectroscopic properties (1H nmr, 13C nmr, uv) with model compounds from each isomeric series; structural assignments for these models are based on unequivocal mass-spectral fragmentation patterns. Unlike related triazolopyridine nucleosides with the ribose moiety attached to a pyridine nitrogen (Lynch and Sharma (1976)), there are no unusual aspects in the conformations of the nueleosides of types 4 and 5.

scholarly journals Synthesis, Characterization, and Agricultural Biological Activities of 5-Fluoro-2-hydroxy Butyrophenone

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Fengli Xin ◽  
Chunhua Du ◽  
Gongjia Lan ◽  
Zhuanping Wu
Keyword(s):  
Lactuca Sativa ◽  
Biological Activities ◽  
Raw Material ◽  
Synthetic Approach ◽  
Target Compound ◽  
Echinochloa Crusgalli ◽  
Agricultural Plant ◽  
H Nmr ◽  
Valsa Mali ◽  
C Nmr

A novel synthetic approach towards 5-fluoro-2-hydroxy butyrophenone is reported. Using 4-fluorophenol as a raw material, the processes of etherification protection, Friedel-Crafts acylation and demethylation provide the target compound under mild conditions. The structure was characterized by the melting point and IR, MS,1H-NMR, and13C-NMR spectroscopy. The bioassay results indicate that the target compound exhibits potent antifungal activities againstValsa mali,Coniella dipodiella, and other agricultural plant fungi. The target compound also shows potent herbicidal activities forLactuca sativa, a dicotyledon, andEchinochloa crus-galli, a monocotyledon. The toxicity regression C50values of the compound againstValsa mali,Coniothyrium diplodiella,Lactuca sativaseedling, andEchinochloa crusgalliseedling were calculated by SPSS. The Hormesis effect for roots ofEchinochloa crusgalliwas confirmed.

Synthesis and Pharmacological Activities of Some New 2-[1-Heptyl-3-(4- methoxybenzyl)-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]acetohydrazide Derivatives

2014 ◽  
Vol 69 (9-10) ◽  
pp. 969-981 ◽  
Author(s):  
Olcay Bekircan ◽  
Emre Mentese ◽  
Serdar Ulker
Keyword(s):  
Nmr Spectroscopy ◽  
Elemental Analysis ◽  
Lipase Activity ◽  
Spectral Studies ◽  
Antituberculosis Activity ◽  
Pharmacological Activities ◽  
Mass Spectral ◽  
H Nmr ◽  
Acetohydrazide Derivative ◽  
C Nmr

Abstract In the present investigation, the key intermediate acetohydrazide derivative 5 was synthesized starting from 3-(4-methoxybenzyl)-4-amino-4,5-dihydro-1,2,4-triazol-5-one (1) by a four-step reaction. Thiosemicarbazides 6a-f and arylidenehydrazide derivatives 8a-d were obtained from compound 5. The cyclization of compounds 6a-f in the presence of NaOH resulted in the formation of compounds 7a-f. The compounds were characterized by IR, 1H NMR, 13C NMR spectroscopy, elemental analysis and mass spectral studies. The compounds were tested for their anti-lipase, anti-α-glucosidase and anti-mycobacterial activities. Compounds 6b and 8c exhibited excellent anti-lipase activity, and compound 8d showed excellent anti-a-glucosidase activity. Compounds 3 and 4 exhibited good antituberculosis activity

Synthesis of isothiocyanates from non-aromatic nitrogen-containing heterocycles

1986 ◽  
Vol 51 (1) ◽  
pp. 112-117 ◽  
Author(s):  
Jozef Gonda ◽  
Pavol Kristian ◽  
Ľubomír Mikler
Keyword(s):  
Spectral Methods ◽  
Mass Spectral ◽  
H Nmr ◽  
C Nmr

Investigation of the reaction of thiophosgene with Δ2-oxazolines I, Δ3-thiazolines II, 4H-benzo[d][1,3]thiazines III, 2-methoxypentahydro-Δ1-azepine IV, theophylline and caffeine showed that only compounds I and IV reacted to give 2-acyloxyethyl isothiocyanates and methyl 6-isothiocyanatohexanoate. The structure of these products was corroborated by IR, 1H NMR, 13C NMR and mass spectral methods. The suitability of the above-mentioned compounds to react is discussed.

Synthesis and Characterization of a New Coumarin-1,2,3-Triazole Diad

2014 ◽  
Vol 618 ◽  
pp. 170-174
Author(s):  
Hong Qi Li ◽  
Xiu Juan Tian ◽  
Zhen Chen ◽  
Ding Xiao ◽  
Ning Fang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Biological Activities ◽  
Antitubercular Activity ◽  
Synthesis And Characterization ◽  
Target Compound ◽  
H Nmr ◽  
Mild Conditions ◽  
Ideal Approach ◽  
C Nmr

A new coumarin-1,2,3-triazole diad was designed and synthesized by Pechmann-Duisberg reaction and click chemistry. The three-step synthetic route to the target compound afforded an overall yield of 56%. The structures of the synthesized compounds were characterized by 1H NMR, 13C NMR, IR and mass spectrum. The click chemistry provided an ideal approach for synthesis under mild conditions of coumarin-1,2,3-triazole diads which may exhibit excellent biological activities such as antitubercular activity.

scholarly journals Synthesis Antimicrobial and Anticancer Evaluation of 1-Aryl-5-(o-methoxyphenyl)-2-S-benzyl Isothiobiurets

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Mohammed M. Ansari ◽  
Shirish P. Deshmukh ◽  
Rizwan Khan ◽  
Mohammed Musaddiq
Keyword(s):  
Biological Activities ◽  
Phenyl Isocyanate ◽  
Spectral Studies ◽  
Mass Spectral ◽  
H Nmr

A series of S-benzyl aryl thiourea were condensed with o-Methoxy phenyl isocyanate to yield respective isothiobiuret derivatives. The newly synthesized compounds were characterized by 1H-NMR, IR, and Mass Spectral studies and tested for biological activities.

scholarly journals Synthesis and Spectroscopic Characterization of Some New Axially Ligated Indium(III) Macrocyclic Complexes and Their Biological Activities

2014 ◽  
Vol 2014 ◽  
pp. 1-7
Author(s):  
Gauri D. Bajju ◽  
Altaf Ahmed ◽  
Deepmala Gupta ◽  
Ashu Kapahi ◽  
Gita Devi
Keyword(s):  
Biological Activities ◽  
Spectroscopic Characterization ◽  
Axial Ligand ◽  
Free Base ◽  
H Nmr ◽  
Pyramidal Geometry ◽  
The Stability ◽  
Square Pyramidal Geometry ◽  
C Nmr

The synthesis and spectroscopic characterization of new axially ligated indium(III) porphyrin complexes were reported. Chloroindium(III) porphyrin (TPPIn-Cl) was obtained in good yield by treating the corresponding free base with indium trichloride. The action of the different phenols on chloroderivatives (TPPIn-Cl) led to the corresponding phenolato complexes (TPPIn-X). These derivatives were characterized on the basis of mass spectrometry,1H-NMR, IR, and UV-visible data. The separation and isolation of these derivatives have been achieved through chromatography. The spectral properties of free base porphyrin and its corresponding metallated and axially ligated indium(III) porphyrin compounds were compared with each other. A detailed analysis of UV-Vis,1H-NMR, and IR suggested the transformation from free base porphyrin to indium(III) porphyrin. Besides,13C-NMR and fluorescence spectra were also reported and interpreted. The stability of these derivatives has also been studied through thermogravimetry. The complexes were also screened for anticancerous activities. Among all the complexes, 4-MePhO-InTPP shows highest anticancerous activity. The title complexe, TPPIn-X (where X = different phenolates), represents a five-coordinate indium(III) porphyrin complex in a square-pyramidal geometry with the phenolate anion as the axial ligand.

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