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 ◽  

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.

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (06) ◽  
pp. 7-13
Author(s):  
Archana ◽  

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.


Author(s):  
N.Ya. Kuzmenko ◽  
S.N. Kuzmenko ◽  
O.V. Skrinnik ◽  
V.V. Bugrym

Synthesis and properties of products based on tris[[tri(butoxy)titanate]boron with complete or partial substitution of butoxy groups linked with titanium by fluorinated alkoxy group were described. Extracted products were liquid or solid substances which are high soluble in aliphatic-, aromatic- chloraromatic- and chlorinated hydrocarbons, low alcohols, and ketone. Their structure was confirmed by elemental analysis, determination of molecular mass, IR and 1H NMR spectroscopy.


2005 ◽  
Vol 14 (2-3) ◽  
pp. 139-149 ◽  
Author(s):  
C. L. Stabler ◽  
R. C. Long ◽  
I. Constantinidis ◽  
A. Sambanis

Direct, noninvasive monitoring of tissue engineered substitutes containing live, functional cells would provide valuable information on dynamic changes that occur postimplantation. Such changes include remodeling both within the construct and at the interface of the implant with the surrounding host tissue, and may result in changes in the number of viable cells in the construct. This study investigated the use of 1H NMR spectroscopy in noninvasively monitoring the viable cell number within a tissue engineered construct in vivo. The construct consisted of mouse βTC3 insulinomas in a disk-shaped agarose gel, surrounded by a cell-free agarose gel layer. Localized 1H NMR spectra were acquired from within implanted constructs, and the total choline resonance was measured. Critical issues that had to be addressed in accurately quantifying total choline from the implanted cells included avoiding signal from host tissue and correcting for interfering signal from diffusing solutes. In vivo NMR measurements were correlated with MTT assays and NMR measurements performed in vitro on explanted constructs. Total choline measurements accurately and noninvasively quantified viable βTC3 cell numbers in vivo, in the range of 1 × 106 to more than 14 × 106 cells, and monitored changes in viable cell number that occurred in the same construct over time. This is the first study using NMR techniques to monitor viable cell numbers in an implanted tissue substitute. It established architectural characteristics that a construct should have to be amenable to NMR monitoring, and it set the foundation for future in vivo investigations with other tissue engineered implants.


1991 ◽  
Vol 30 (6) ◽  
pp. 579-585 ◽  
Author(s):  
Ronald J T Corbett ◽  
Abbot R Laptook ◽  
Joan I Ruley ◽  
Damian Garcia

2008 ◽  
Vol 194 (2) ◽  
pp. 163-168 ◽  
Author(s):  
Vladimír Mlynárik ◽  
Cristina Cudalbu ◽  
Lijing Xin ◽  
Rolf Gruetter

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