Synthesis and Biological Evaluation of Various New Substituted 1,3,4-oxadiazole-2-thiols

2008 ◽  
Vol 59 (4) ◽  
Author(s):  
Gabriela Laura Almajan ◽  
Stefania Felicia Barbuceanu ◽  
Ioana Saramet ◽  
Mihaela Dinu ◽  
Cristian Vasile Doicin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Plant Growth ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Biological Evaluation ◽  
Ethyl Chloroacetate ◽  
Low Concentrations ◽  
Synthesis And Biological Evaluation

5-[4-(4X-phenylsulfonyl)phenyl]-1,3,4-oxadiazole-2-thiols, X=H, Cl, Br, reacted with ethyl chloroacetate to give S-alkylated compounds. Aminomethylation of the thione form of oxadiazoles yielded N(3)-derivatives. All the products have been characterized by elemental analysis, IR, 1H-NMR and 13C-NMR. The plant-growth regulating effects of the title compounds were examined. From the biological activity results, we found that most compounds showed weak stimulatory activities at low concentrations.

scholarly journals Characterization and biological evaluation of some novel pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidin-8-ones synthesized via the Gewald reaction

2008 ◽  
Vol 73 (7) ◽  
pp. 683-690 ◽  
Author(s):  
Dipti Dodiya ◽  
Amit Trivedi ◽  
Samir Jarsania ◽  
Shailesh Vaghasia ◽  
Viresh Shah
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Spectroscopic Investigation ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Gewald Reaction ◽  
Compound Ii

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. .

SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME HETEROCYCLES CONTAINING OXADIAZOLE AND PYRAZOLE RING FOR ANTI-BACTERIAL, ANTI-FUNGAL AND ANTI-TUBERCULAR ACTIVITIES

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 18-24
Author(s):  
S. R. Pattan ◽  
◽  
P. A Chavan ◽  
R. A Muluk ◽  
S. S Dengale ◽  
...  
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
Ethyl Acetoacetate ◽  
Pyrazole Ring ◽  
Biological Evaluation ◽  
Secondary Amines ◽  
Anti Fungal ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

1, 3, 4-oxadiazoles were synthesized by treating pyrazine-2-carbohydrazide with CS2 and alc. KOH and their derivatives were prepared by using R-Cl compounds. pyrazolones were synthesized by treatingpyrazine-2-carbohydrazide with ethyl acetoacetate. The derivatives of pyrazolone were prepared by refluxing pyrazolone with formaldehyde and different substituted secondary amines. All the synthesized compounds were characterized by IR, 1H-NMR and elemental analysis and evaluated for antibacterial, antifungal and antitubercular activities.

Design and Synthesis of some novel 3-benzylidene-1H-benzo [4,5]imidazo[2,1-c] [1,4]oxazine-1,4(3H)-dione derivatives and evaluation of their biological activity

2021 ◽  
Vol 25 (11) ◽  
pp. 157-169
Author(s):  
Ch. Sunitha ◽  
G. Brahmeshwari
Keyword(s):  
Mass Spectrometry ◽  
Biological Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
The Other ◽  
Good Activity ◽  
Design And Synthesis ◽  
Anti Oxidant ◽  
Anti Fungal

A novel series of 3-arylbenzylidene-1H-benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dione (4a-l) was synthesized in moderate to good yields. The structures of the newly synthesized compounds were confirmed by 1H NMR, 13C NMR mass spectrometry and elemental analysis. The synthesized compounds were evaluated for their anti-bacterial and anti-oxidant activities. Among all the derivatives tested, the compound 3-(3,5- dimethoxy benzylidene)-1H-benzo [4,5]imidazo[2,1- c][1,4]oxazine-1,4-(3H)-dione showed more potent activity and 3-(4-methoxybenzylidene)-1H benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dion exhibited good activity as compared to standard streptomycin. The anti-fungal activity reveals that the compound 3- (3,5-dimethoxy benzylidene)-1H-benzo[4,5]imidazo [2,1-c][1,4]oxazine-1,4-(3H)-dione showed more promising activity as compared to standard Itrazole. The remaining compounds showed moderate to poor activity. Similarly, the anti-oxidant activity results revealed that the compound 3-(3,5-dimethoxy benzylidene)-1H-benzo [4,5] imidazo[2,1-c][1,4] oxazine-1,4-(3H)-dione exhibited potent activity as compared to the other tested compounds.

scholarly journals New S-alkylated 1,2,4-triazoles incorporating diphenyl sulfone moieties with potential antibacterial activity

2009 ◽  
Vol 74 (10) ◽  
pp. 1041-1049 ◽  
Author(s):  
Stefania Barbuceanu ◽  
Gabriela Almajan ◽  
Ioana Saramet ◽  
Constantin Draghici ◽  
Radu Socoteanu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Ethyl Bromide ◽  
Phenacyl Bromide ◽  
Antibacterial Effects ◽  
Ethyl Chloroacetate ◽  
Diphenyl Sulfone ◽  
New Compounds

Alkylation of the 5-{4-[(4-bromophenyl)sulfonyl]phenyl}-4-(3/4-methylphenyl)- 2,4-dihydro-3H-1,2,4-triazole-3-thiones 3a,b with various alkylation agents, i.e., ethyl bromide, phenacyl bromide and ethyl chloroacetate, afforded the S-substituted 1,2,4-triazoles 4-6a,b. The structures of these new compounds were elucidated by elemental analysis and IR, UV, 1H-NMR, 13C-NMR and MS spectroscopy. The newly synthesized products were tested for their antibacterial effects.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF NOVEL S-SUBSTITUTED PHENACYL-1, 3, 4-TRIAZOLE-THIOL DERIVATIVES FOR ANTIMICROBIAL STUDIES

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (08) ◽  
pp. 14-20
Author(s):  
S. S Kerur ◽  
◽  
K. R Alagawadi ◽  
H. Zhu ◽  
F. V Manvi
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Biological Evaluation ◽  
Triazole Derivatives ◽  
Antimicrobial Studies

In the present study, synthesis and antimicrobial activity of 2,5-disubstituted triazole derivatives 5a-f are described. The structures of the newly synthesized compounds were confirmed by FTIR, 1H NMR, mass and elemental analysis. All compounds were screened for antitubercular and antibacterial activity. The results revealed that most of the compounds showed high or moderate biological activity against tested microorganisms.

scholarly journals Reactions of MoCl5 and MoO2Cl2 with Succinimide, 1, 4-Diaminobutane, 3-Methylpyridine, 1, 3-Diaminopropane, Pyrazole and 1- Methylpyrrolidine in Tetrahydrofuran

2021 ◽  
Vol 37 (3) ◽  
pp. 634-642
Author(s):  
Rakesh Kumar ◽  
Gursharan Singh
Keyword(s):  
Biological Activity ◽  
Transition Metals ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Inert Atmosphere ◽  
Biologically Active ◽  
Vacuum Line ◽  
Characterization Studies ◽  
Hydrolysis Of

It has been reported that molybdenum may extract oxygen from oxygen containing ligands. Oxo complexes of above bases with transition metals show numerous applications and are biologically active. So to study the biological activity of molybdenum complexes and to study oxo abstraction reactions by molybdenum, reactions of succinimide/1, 4-diaminobutane/3-methylpyridine/1, 3-diaminopropane/pyrazole/1-methylpyrrolidine with MoCl5/MoO2Cl2 have been carried out, in THF medium using equimolar/bimolar quantities of the ligand, at normal temperature. The products thus obtained are: Mo2O3Cl5(C4H5NO2)2(C4H8O)2, [1]; Mo2O2Cl2(C4H5NO2)2(C4H8O)2, [2]; MoO2Cl2(H2NCH2CH2CH2CH2NH2)2, [3]; Mo3Cl8(C6H7N)4(C4H8O)2, [4]; Mo3Cl6(C6H7N)6(C4H8O)6, [5]; MoO2Cl3(H2NCH2CH2CH2NH2)2, [6]; Mo2O4Cl4(C3H4N2)4, [7] and Mo2O6Cl8(C5H11N)4, [8]. There is oxygen abstraction by molybdenum during the reaction from the oxygen containing solvent THF. Formulations of these compounds were made and their properties were studied with FTIR(transmission mode), 1H NMR/13C NMR, microbiological studies, elemental analysis(Mo, Cl, C, H, N) and LC-MS. All preparations, separations and isolations were executed in vacuum line and inert atmosphere (dry nitrogen) to eliminate any oxidation/hydrolysis of products by air/moisture. The formulations proposed have been supported by the above characterization studies.

scholarly journals Synthesis and Biological evaluation of some new 2-thioxoimidazolidin-4-one derivatives (part II)

2018 ◽  
Vol 29 (1) ◽  
pp. 79 ◽  
Author(s):  
Amjad Gali
Keyword(s):  
Antibacterial Activity ◽  
1H Nmr ◽  
Heterocyclic Compounds ◽  
Biological Evaluation ◽  
Ethyl Chloroacetate ◽  
In Series ◽  
Cyclic Compounds ◽  
Synthesis And Biological Evaluation

In the present work adifferent of new heterocyclic  compounds were synthesized by reaction of thiosemicarbazide with tow aldehydes (4-bromo benzaldehyde,2-chloro benzaldehyde). the reacting `of compounds(1,2)  with ethyl chloroacetate to give 3-[(arylidene)amino]-2-sulfanyl-3,5-dihydro-4H-imidazol-4-one (3,4) which treating with defferent aldehydes togive chalcones  . the compound (3) reacted with ethyl aceto acetate to give ethyl 4-aryl-1-[(4-bromo benzylidene)amino]-6-oxo-2-sulfanyl-3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-5-carboxylate,and in series of reaction converted into a variety of derivatives. The prepared compounds were characterized by 1H NMR and FTIR spectroscopy.further more antibacterial activity of some the prepared  new cyclic compounds were evaluated against three types of bacteria

Synthesis and Spectral Characterization of New S-Alkylated 1,2,4-Triazoles as Potential Biological Agents

2017 ◽  
Vol 68 (10) ◽  
pp. 2436-2439
Author(s):  
Stefania Felicia Barbuceanu ◽  
Laura Ileana Socea ◽  
Constantin Draghici ◽  
Elena Mihaela Pahontu ◽  
Theodora Venera Apostol ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Ethyl Bromide ◽  
Spectral Characterization ◽  
Basic Medium ◽  
Phenacyl Bromide

In the work we presented the behavior of 5-(4-(4-X-phenylsulfonyl)phenyl)-4-(n-propyl)-2H-1,2,4-triazole-3(4H)-thiones (X= Cl or Br) with some alkylation agents. Thus, new S-alkylated 1,2,4-triazole derivatives were synthesized by reaction of the corresponding 1,2,4-triazole-3-thione derivatives with different �-halogenated compounds (ethyl bromide, ethyl chloroacetate or phenacyl bromide), in basic medium. The structures of synthesized compounds were elucidated by spectral data (1H-NMR, 13C-NMR, mass spectrometry) and elemental analysis.

Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives

2018 ◽  
Vol 17 (6) ◽  
pp. 448-457 ◽  
Author(s):  
Xia Huang ◽  
Tie Chen ◽  
Rong-Bi Han ◽  
Feng-Yu Piao
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Anticonvulsant Activity ◽  
Mass Spectra ◽  
Maximal Electroshock ◽  
Test Compound ◽  
Maximal Electroshock Test ◽  
Mes Test ◽  
Structure Activity

Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1). Conclusion: Possible structure-activity relationship was discussed.

scholarly journals N-Benzo[c][1,2,5]thiazol-4-yl-3-trifluoromethylbenzamide

Molbank ◽  
10.3390/m1075 ◽  
2019 ◽  
Vol 2019 (3) ◽  
pp. M1075 ◽  
Author(s):  
Hamad H. Al Mamari ◽  
Nasser Al Awaimri ◽  
Yousuf Al Lawati
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Title Compound ◽  
Structural Motif ◽  
Spectroscopic Methods ◽  
Bond Functionalization ◽  
Directing Group ◽  
Metal Catalyzed

The title compound, N-benzo[c][1,2,5]thiazol-4-yl-3-trifluoromethylbenzamide (1) was synthesized by reacting 3-trifluoromethylbenzoyl chloride (4) and 4-aminobenzo[c][1,2,5]thiadiazole (5). The compound was characterized by various spectroscopic methods (1H NMR, 13C NMR, IR, GC-MS) and its composition confirmed by elemental analysis. The importance of this compound lies in its possession of an N,N-bidentate directing group. Such a structural motif is potentially suitable for metal-catalyzed C-H bond functionalization reactions.

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