SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL BENZODIAZEPINE CONTAINING BENZOTHIAZEPINE/BENZOXAZEPINE DERIVATIVES AS POTENT ANTICONVULSANT AGENTS

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (06) ◽  
pp. 7-13
Author(s):  
Archana ◽  
Keyword(s):  
Nmr Spectroscopy ◽  
Acute Toxicity ◽  
Elemental Analysis ◽  
Anticonvulsant Activity ◽  
1H Nmr Spectroscopy ◽  
Biological Evaluation ◽  
Standard Drug ◽  
Phenytoin Sodium ◽  
Synthesis And Biological Evaluation

A new series of 4-benzodiazepinyl-2-( substituted phenyl)-1,5-benzothiazepines (3a-3f) and 4-benzodiazepinyl-2-(substituted phenyl)-1,5-benzoxazepines (4a-4f) were synthesised and evaluated for their anticonvulsant activity. All these compounds were screened in vivo, for their anticonvulsant activity and acute toxicity. Compound 4-benzodiazepinyl-2-(p-methoxy phenyl)-1,5-benzothiazepine 4b, was found to be most potent compoundof this series, more potent than standard drug phenytoin sodium. The homogeneity of all the compounds was checked by TLC. The structures of these compounds have been established by elemental analysis, IR and 1H NMR spectroscopy.

SYNTHESIS AND EVALUATION OF SOME NEWER QUINAZOLINONYL SUBSTITUTED BENZOXAZEPINYL / BENZOTHIAZEPINYL INDOLES AS POTENT ANTICONVULSANT AGENTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 18-24
Author(s):  
Archana ◽  
Keyword(s):  
Nmr Spectroscopy ◽  
Acute Toxicity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Anticonvulsant Activity ◽  
1H Nmr Spectroscopy ◽  
Standard Drug ◽  
Anticonvulsant Agents ◽  
Phenytoin Sodium

new series of 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H)-onyl chalconyl)-2-substituted indoles (3-8), 3-[3-Amino-2-methyl-6- substituted quinazolin-4(3H) -onyl-benzoxazepin/benzo -thiazepin- 2-yl] -2-substituted indoles (9-20) and 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H) -onyl-3- (sub-stituted phenylaminomethylene) -benzoxazepin/benzothizepin-2-yl] -2-substitutedindoles (21-44) were synthesised and evaluated for anticonvulsant activity. All these compounds were screened in vivo, for their anticonvulsant activity and acute toxicity. Coumpund 44 , 3-[3-amino-2-methyl-6-bromoquinazolin- 4(3H)-onyl-3- (chlorophenylaminomethylene)-benzothiazepine-2-yl]-2-chloroindole, was found to be most potent compound of this series , more potent than standard drug phenytoin sodium. The homogeneity of all the compounds have been established by elemental analysis, IR and 1H-NMR spectroscopy.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

Synthesis and biological evaluation of mixed-ligands cyclometalated iridium(III)-quinoline complexes

2021 ◽  
Author(s):  
Yan Yang ◽  
Cheng-Ming Wang ◽  
Feng-Hua Pan ◽  
Qi-Pin Qin ◽  
Qiu-Ji Xie ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
In Vivo Efficacy ◽  
Mixed Ligands ◽  
Synthesis And Biological Evaluation ◽  
Insight Into

With the aim of gaining new insight into the underlying apoptosis mechanisms and in vivo efficacy of cyclometalated Ir(III) complexes as metalodrugs, six new cyclometalated Ir(III)-quinoline complexes, [Ir(1a)(2pq)2] (2a), [Ir(1b)(2pq)2]...

scholarly journals Nickel(II) cyclohexylethyl-dithiocarbamate P-donor ligands in the coordination sphere

2004 ◽  
Vol 69 (12) ◽  
pp. 1053-1061 ◽  
Author(s):  
Josef Husárek ◽  
Richard Pstorek ◽  
Michal Malon ◽  
Zedenek Sindalar ◽  
Marek Pavlícek
Keyword(s):  
Thermal Analysis ◽  
Nmr Spectroscopy ◽  
Elemental Analysis ◽  
1H Nmr Spectroscopy ◽  
Chemical Study ◽  
Donor Ligands ◽  
Conductivity Measurements ◽  
Physico Chemical ◽  
Square Planar ◽  
Vis Spectroscopy

A series of new Ni(II) dithiocarbamate compounds of the composition [NiX(cetdtc)(PR3)](X = Cl, Br, I, NCS; cetdtc = cyclohexylethyldithiocarbamate; R = phenyl, n-butyl) has been synthesized. All the isolated complexes have been characterized by elemental analysis, IR and UV/VIS spectroscopy, 31P{1H}-NMR spectroscopy, thermal analysis magnetochemical and conductivity measurements. On the basis of the results of the physico-chemical study, all complexes are diamagnetic, non-electrolytes with a square-planar NiS2PX chromophore.

scholarly journals Synthesis, characterization and acute toxicity of new Schiff base derived from phenylethyl amine and 2-hydroxy naphthaldehyde

2019 ◽  
Vol 10 (1) ◽  
pp. 26-29
Author(s):  
Ibtihal Hassan Hatim ◽  
Wasfi Aboud Al-Masoudi ◽  
Rashad Fadhil Ghadhban
Keyword(s):  
Body Weight ◽  
Schiff Base ◽  
Nmr Spectroscopy ◽  
Acute Toxicity ◽  
Elemental Analysis ◽  
Good Yield ◽  
Mice Model ◽  
Base Derivative ◽  
New Compounds

There is an urgent need for the design and development of new and safer drugs, this has attracted organic chemists to synthesize new compounds with potential of biological and chemotherapeutic activities. Here we report, the condensation of phenylethylamine with 2-hydroxy naphthaldehyde yielded Schiff base derivative in good yield. Characterization of synthesized compound was carried by elemental analysis, IR, 1H-, 13C- and HSQC-NMR spectroscopy. The toxicity of the synthesized compound was determined using Balb/c mice model. Dixon’s up and down method was found to have an LD50 of 827.2 mg/kg of body weight, moderate toxicity.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

scholarly journals Synthesis and characterization of new Oxazine , Thiazine and Pyrazol derived from chalcones

2014 ◽  
Vol 11 (2) ◽  
pp. 477-485 ◽  
Author(s):  
Baghdad Science Journal
Keyword(s):  
Nmr Spectroscopy ◽  
Hydrazine Hydrate ◽  
Elemental Analysis ◽  
Potassium Hydroxide ◽  
1H Nmr Spectroscopy ◽  
Room Temperature ◽  
Potassium Hydroxide Solution ◽  
Synthesis And Characterization ◽  
Heterocyclic Derivatives

In this study, chalcones were synthesis by condensing 2-acetylpyridine with aromatic aldehyde derivatives in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. After that, new heterocyclic derivatives such as Oxazine, Thiazine and Pyrazol were synthesis by reaction between chalcones with urea, thiourea and hydrazine hydrate respectively scheme 1. All these compounds wrer characterization by FTIR, 1H-NMR spectroscopy and elemental analysis.

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