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 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 Synthesis and Antimicrobial Assessment of Some New 2-(Thiazol-5-yl)-1,3,4-oxadiazoles

2019 ◽  
Vol 70 (6) ◽  
pp. 1996-1999
Author(s):  
Catalin Araniciu ◽  
Smaranda Dafina Oniga ◽  
Cristina Ioana Stoica ◽  
Mariana Carmen Chifiriuc ◽  
Marcela Popa ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Physicochemical Characterization ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Fungal Strains ◽  
New Compounds

Considering the promising antimicrobial activity of compounds bearing the thiazole or the oxadiazole rings in their structures, we set out to obtain new antimicrobial molecules bearing the 2-(thiazol-5-yl)-1,3,4-oxadiazole schaffold. The structures of the 8 new compounds obtained was confirmed by physicochemical characterization including: 1H-NMR, MS and elemental analysis. Antimicrobial activity was investigated against 5 Gram-positive bacterial strains, 2 Gram-negative bacterial strains and 2 fungal strains. The newly synthesized compounds showed modest antimicrobial activity.

scholarly journals New N-acylhydrazones with Potential Cytotoxic Activity

2019 ◽  
Vol 69 (12) ◽  
pp. 3341-3344
Author(s):  
Laura Ileana Socea ◽  
Stefania Felicia Barbuceanu ◽  
Lucian Iscrulescu ◽  
Bogdan Socea ◽  
Madalina Hrubaru ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Daphnia Magna ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Aromatic Aldehydes ◽  
Toxicological Profile

Some new N-acylhydrazones 7a-c having dibenzo[a,d][7]annulene moiety were synthesized by condensation of corresponding hydrazide 5 with aromatic aldehydes. The structures of these newly compounds were elucidated by IR, 1H-NMR, 13C-NMR, and elemental analysis. In the view of the therapeutical potential of the newly compounds, we evaluated their toxicological profile using Daphnia magna bioassay.

Synthesis and Biological Evaluation of a New Schiff Base and its Cu(II) Complex

2017 ◽  
Vol 68 (3) ◽  
pp. 586-588
Author(s):  
Gladiola Tantaru ◽  
Antonia Poiata ◽  
Nela Bibire ◽  
Alina Diana Panainte ◽  
Mihai Apostu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Elemental Analysis ◽  
Schiff Base Ligand ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

A new Schiff base ligand, N-hydroxy-N�-salicylidene-urea was synthesized through the condensation of salicylaldehyde with hydroxyurea. The copper(II) complex of the Schiff base has been also obtained. Their structure has been proven using spectral methods such as UV-Vis, FT-IR, 1H-NMR and elemental analysis. The antimicrobial activity of the copper(II) complex was evaluated through comparison to the activity of the Schiff base on various bacterial strains. All tested compounds were very active against both gram-positive and gram-negative bacteria.

scholarly journals Synthesis and antimicrobial activity of a new series 1,4-dihydropyridine derivatives

2011 ◽  
Vol 76 (1) ◽  
pp. 1-11 ◽  
Author(s):  
Surendra Kumar ◽  
A. Idhayadhulla ◽  
Abdul Nasser ◽  
J. Selvin
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Mass Spectral ◽  
Dihydropyridine Derivatives

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.

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 Synthesis, Characterisation and Biological Screening of s-Triazine Based Chalcones and its Derivatization into Phenyl Pyrazolines, Isoxazoles

2015 ◽  
Vol 47 ◽  
pp. 109-119 ◽  
Author(s):  
Anjani Solankee ◽  
Riki Tailor
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Hydroxylamine Hydrochloride ◽  
Aromatic Aldehydes ◽  
Phenyl Hydrazine ◽  
Biological Screening ◽  
Gram Negative ◽  
E Coli ◽  
Heterocyclic Derivatives

Heterocyclic derivatives such as phenyl pyrazolines and isoxaxoles were prepared from s - triazine based chalcones. Chalcones (A1 - A5) are synthesised by the reaction of compound (V) with various aromatic aldehydes. Moreover, further reaction of chalcones with phenyl hydrazine hydrochloride and hydroxylamine hydrochloride in the presence of alkali gives phenyl pyrazolines (A6 - A10) and isoxazoles (A11 - A15) derivatives respectively. The structures of the newly synthesised compounds were confiremed by spectroscopic (IR, 1H NMR, 13C NMR) and elemental analysis. All the newly synthesised compounds have been screened for their antimicrobial activity against selected Gram - positive (S. aureus and S. pyogenus), Gram - negative (E. coli and P. aeruginosa) bacterial and fungal strains (C. albicans, A. niger and A. clavatus).

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

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.

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