SYNTHESIS AND ANTICONVULSANT ACTIVITY OF NOVEL 1,3,4-OXADIAZOLE DERIVATIVES

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 40-44
Author(s):  
.Aishwarya T.C ◽  
◽  
James Jainey ◽  
Vijay Kumar M. ◽  
B.C. Revanasiddappa

2 Oxo-2h-chromene-3-carbohydrazide (1) reacts with various aromatic aldehydes to give corresponding 2-oxo-2h-chromene-3-carbohydrazide arylidene hydrazides (SB1-8). Oxidative cyclization of (SB1-8) with mercuric oxide and iodine in DMF medium furnishes the title compounds 3-(5-aryl-1,3,4-oxadiazol2-yl)-2h-chromen-2-ones (2a-h). All the synthesized compounds were assigned structures on the basis of IR, 1 H-NMR and Mass spectral data. Some of the selected compounds were evaluated for In vivo anticonvulsant activity by MES and PTZ models.

2008 ◽  
Vol 5 (3) ◽  
pp. 447-452 ◽  
Author(s):  
G. Nagalakshmi

In the present study, 2-(4-halosubstituted phenyl)-4,5-diphenyl-1Himidazoles have been synthesized by refluxing benzil and ammonium acetate with different 4-halosubstituted aromatic aldehydes in glacial acetic acid. The structural assignment of this compound has been made on the basis of elemental analysis, UV, IR,1H NMR and Mass spectral data. Toxicity of the compound has been determined. The synthesized compound was evaluated for antiinflammatory activity against carrageenan induced paw oedema and anticonvulsant activity against maximal electro-shock-induced convulsions in rats.


2007 ◽  
Vol 4 (3) ◽  
pp. 320-342 ◽  
Author(s):  
Vinod Mathew ◽  
J. Keshavayya ◽  
V. P. Vaidya

4-Amino-5-aryl/heteroaryl substituted-3-mercapto-1,2,4-triazoles 3(a-d) were prepared from the corresponding aromatic carboxylic acids through a multi-step sequence. Compounds 3(a-d) were made to react with various aromatic/hetero aromatic acids and hetero aromatic aldehydes to give 3,6-disubstituted-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles and 3,6-disubstituted-5,6-dihydro-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles respectively. Elemental analysis, IR,1H NMR and mass spectral data elucidated the structures of all newly synthesized compounds. Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities.


2015 ◽  
Vol 21 (4) ◽  
pp. 219-224 ◽  
Author(s):  
Hala M. Refat ◽  
Khaled S. Mohamed

AbstractNew 3-aryl-pyrido[2,1-b][1,3]benzothiazole derivatives 2a–e were synthesized in excellent yields via the reaction of benzothiazoleacetonitrile (1) with different aromatic aldehydes. The treatment of 2-(benzo[d]thiazol-2-yl)-3-(pyridin-4-yl)acrylonitrile (6) with malononitrile afforded 1-amino-3-(pyridin-4-yl)-3H-pyrido[2,1-b][1,3]benzothiazole-2,4-dicarbonitrile (7), which was allowed to react with a variety of reagents to provide pyrimido[5′,4′:5,6]pyrido[2,1-b][1,3]benzothiazole 8, 9 and [1,3]benzothiazolo[3,2-a][1,8]naphthyridine 10, 15 derivatives. All synthesized products were confirmed by elemental analysis, IR, 1H-NMR, 13C-NMR, and mass spectral data.


2009 ◽  
Vol 6 (3) ◽  
pp. 775-779 ◽  
Author(s):  
B. Rajeeva ◽  
N. Srinivasulu ◽  
S. M. Shantakumar

Some new 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3- benzothiazole(3a-j)were synthesized by refluxing benzothiazolyl carboxyhydrazide with different aryl acids in phosphoryl chloride. Structures of the synthesized compounds were established on the basis of1H NMR and Mass spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.


2005 ◽  
Vol 09 (07) ◽  
pp. 509-518 ◽  
Author(s):  
Rajendra Prasad ◽  
Ajay Kumar

The ( bpy )2 Ru II and ( phen )2 Ru II moieties were linked to [ Ni ( OBTTAP )]1, periphery through coordinate bonds in order to synthesize cationic di- and pentanuclear complexes 2-5 that were obtained as PF 6− salts. They were characterized by IR, 1 H NMR, UV-vis, and mass spectral data. The electronic absorption, emission and redox data of these bichromophoric systems indicate the presence of a high degree of intercomponent electronic interaction. The position and relative intensities of the Soret and Q bands in these complexes is altered due to peripheral binding of the metal units. The compounds were non-emissive for the Q band excitation but, Soret excitation led to a strong S 2 emission, observed between 400-450 nm. In cyclic voltammetry, the compounds exhibited one Ru centered oxidation together with one or two OBTTAP centered oxidations. The Ru II/ Ru III oxidations were observed at significantly lower potentials as compared to the corresponding simple maleonitrile-benzylthioether complexes and has been interpretted in terms of weaker d π( S )– d π( Ru ) interactions.


Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit

2- Methoxy – 6 - {4' - [(4'''- Chlorophenyl) (phenyl) methyl amino] phenyl} - 4 - aryl nicotinonitrile (3a-3l) and 2-Amino-6-{4'-[(4'''-Chlorophenyl)(phenyl)methyl amino]phenyl}-4-aryl nicotinonitrile (4a-4l) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve, Gram -ve bacteria and fungi. The structure of the products has been elucidated by IR, 1H-NMR, mass spectral data, elemental analysis and thin layer chromatography.


1979 ◽  
Vol 44 (2) ◽  
pp. 420-423 ◽  
Author(s):  
Josef Prousek ◽  
Adolf Jurášek ◽  
Miloslava Dandárová ◽  
Jaroslav Kováč

5-Nitrofurfuryl trichloromethyl sulphone (I) was reacted with paraformaldehyde in methanol in the presence of piperidine as catalyst to give 1-(5-nitro-2-furyl)-1-trichloromethylsulphonyl-2-(5-nitro-2-furyl)cyclopropane. This substance was also obtained from 1-(5-nitro-2-furyl)-1-trichloromethylsulphonyl-2-(5-nitro-2-furyl)ethylene and diazomethane. The reaction products were characterized by IR, UV, 1H NMR and mass spectral data.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (05) ◽  
pp. 21-29
Author(s):  
Natasha N. Aggarwal ◽  
B. C. Revanasiddappa ◽  
Banylla Felicity ◽  
Vijay Kumar ◽  
Hemanth Kumar ◽  
...  

In this present study, a novel series of chalcones (C1-10) were synthesized by reacting 4-nitro acetophenone and various substituted aromatic aldehydes in an alcohol medium. The title compounds, pyrimidine derivatives (PD1-10), were obtained by the cyclization of chalcones (C1-10) with guanidine carbonate in an alcoholic medium. Each of the newly synthesized compounds was structurally assigned in accordance with FT-IR, 1 H-NMR and mass spectral data. All the synthesized compounds were subjected to in silico analysis among which, some of the synthesized compounds were chosen and evaluated for in vivo anticonvulsant study by employing PTZ-induced seizure and MES seizure models. Compounds PD2 and PD7 demonstrated significant anticonvulsant activity when compared to the standard.


2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.


2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Seranthimata Samshuddin ◽  
Badiadka Narayana ◽  
Balladka Kunhanna Sarojini ◽  
Divya N. Shetty ◽  
Nalilu Suchetha Kumari

New functionalized terphenyl derivatives incorporating various heterocyclic rings are prepared by using 4,4′′-difluoro-5′-hydroxy-1,1′:3′,1′′-terphenyl-4′-carbohydrazide as a key intermediate derived from 4,4′-difluoro chalcone, a versatile synthone. All the derivatives are characterized by 1H NMR, IR, and mass spectral data. All the synthesized products are screened for their in vitro antimicrobial and antioxidant properties. The majority of the tested compounds exhibited significant antioxidant activity and some of them showed good antimicrobial activity.


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