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.

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. .

New Heterocyclic Compounds from 1,2,4-triazoles Class with Potential Cytotoxic Activity

2017 ◽  
Vol 68 (11) ◽  
pp. 2503-2508 ◽  
Author(s):  
Laura Ileana Socea ◽  
Stefania Felicia Barbuceanu ◽  
Bogdan Socea ◽  
Constantin Draghici ◽  
Theodora Venera Apostol ◽  
...  
Keyword(s):  
Nmr Spectroscopy ◽  
Cytotoxic Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Heterocyclic Compounds ◽  
Cytotoxic Effect ◽  
13C Nmr Spectroscopy ◽  
New Compounds

Acylhydrazinecarbothioamides (2a,b) were synthesized by addition of 2-(5H-dibenzo[a,d][7]annulen-5-yl)acetohydrazide to different isothiocyanates. The new 1,2,4-triazol-3-thioles (3a,b) were synthesized by cyclization of new 2- acylhydrazinecarbothioamides (3a,b) in basic media. Alkylation of 1,2,4-triazole-3-thiols (3a-c) with ethyl bromide gave only S-substituted derivatives (4a-c). The structures of the synthesized compounds have been established on spectral data (IR, 1H-NMR and 13C-NMR spectroscopy) and elemental analysis. The cytotoxic effect of new compounds was evaluated using two alternative models on plant and invertebrate organisms.

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.

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 Synthesis and Cytotoxic Activity Study of Novel 2-(Aryldiazenyl)-3-methyl-1H-benzo[g]indole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4240
Author(s):  
Manar M. Arafeh ◽  
Ebrahim Saeedian Moghadam ◽  
Sirin A. I. Adham ◽  
Raphael Stoll ◽  
Raid J. Abdel-Jalil
Keyword(s):  
Melting Point ◽  
Cytotoxic Activity ◽  
Elemental Analysis ◽  
13C Nmr ◽  
National Cancer Institute ◽  
Polyphosphoric Acid ◽  
Human Cancer ◽  
Indole Derivatives ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a–f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a–f) were characterized using 1H NMR, 13C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.

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.

scholarly journals 6-[1-Acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-yl]-2(3H)-benzoxazolone

Molbank ◽  
10.3390/m1021 ◽  
2018 ◽  
Vol 2018 (4) ◽  
pp. M1021
Author(s):  
Yordanka Ivanova ◽  
Antonya Todorova ◽  
Christo Chanev ◽  
Ognyan Petrov
Keyword(s):  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Title Compound ◽  
Target Compound

The title compound, 6-[1-acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl]-2(3H)-benzoxazolone, was synthesized by condensation of 6-[3-(4-methoxyphenyl)-2-propenoyl]-2(3H)-benzoxazolone (1) and hydrazine hydrate in acetic acid in 84% yield. The structure of the target compound was confirmed using 1H-NMR, 13C-NMR, IR, MS, and elemental analysis.

A Novel Synthesis of Acetophenone Benzopyran Derivative

2010 ◽  
Vol 152-153 ◽  
pp. 1483-1486
Author(s):  
Xiao Yan Qi ◽  
Lin Wu ◽  
Jian Guo Wang ◽  
De Lian Yi
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Lewis Acids ◽  
Cyclization Reaction ◽  
Novel Synthesis ◽  
Intermolecular Cyclization

The development of a novel synthesis of acetophenone benzopyran is reported. A acetophenone benzopyran derivative was prepared from 1-(2,4-dihydroxyphenyl)ethanone (3) through O-prenylation and Lewis acids catalyzed intermolecular cyclization reaction. The structure of product 1-(3,4-dihydro-4,4-dimethyl-7-hydroxy-2H-1- benzopyran -6-yl)- ethanone (1) was characterized by UV, IR, 1H-NMR, 13C-NMR and elemental analysis.

Study of Synthesis of Novel ɤ-Valerolactone-Based Polyurethanes

2012 ◽  
Vol 229-231 ◽  
pp. 297-302 ◽  
Author(s):  
Mochamad Chalid ◽  
Hans J. Heeres ◽  
Antonius A. Broekhuis
Keyword(s):  
Molecular Weight ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Experimental Work ◽  
Ring Opening ◽  
Molecular Engineering ◽  
Amine Compounds

The ring opening of -valerolactone (GVL) with amine compounds was reported as a promising molecular engineering tool to synthesize precursors for new bio-based polymers such as polyurethanes (PUs). Experimental work on the synthesis of polymers based on GVL/1,2-ethanolamine and GVL/1,2-diaminoethane adducts, and di-isocyanates (1,4-phenylene-di-isocyanate (PDI) 2,4-toluene-di-isocyanate (TDI) and hexamethylene-di-isocyanate (HDI)) is described. The polymers were characterized by FTIR, 1H-NMR, 13C-NMR, elemental analysis and GPC. The best polymerization results were obtained using TEA as the catalyst, DMA as the solvent and a temperature of 140°C for the reaction of the GVL/1,2-aminoethanol adduct with TDI. A polymer with a molecular weight (Mw) of 156 KDalton was produced in 97% yield.

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