scholarly journals Theophylline Derivatives' In-vivo Analgesic and Anti-Inflammatory Activities

Author(s):  
Faruk Alam ◽  
Ruhul Amin ◽  
Biplab Kumar Dey ◽  
Josef Yakin ◽  
Smriti Rekha Chanda Das ◽  
...  

The reaction of theophylline and chloro-acetyl chloride produced an exceptional series of substituted theophylline derivatives (3A-3D), followed by ammonium thiocyanate and substituted aromatic aldehyde, and these synthesized derivatives were screened to study their analgesic and anti-inflammatory activities. UV, IR, H-1 NMR, mass spectral data, and CHN activities were used to describe the compounds, which were shown to be considerably efficacious at 100 mg/kg p.o., as well as experimental results that were statistically significant at the p <0.01 and p <0.05 levels.

Author(s):  
Garima Shrivastava ◽  
Manjul Shrivastava

New Schiff base (2-[(1H-benzimidazol-2-ylimino) methyl]-4,6- diiodophenol) was synthesized by the condensation of aryl/hetero aromatic aldehyde (3,5diiodosalicylaldehyde) with 2- amino benzimidazole under conventional and microwave conditions and characterized through IR, HNMR and Mass spectral data and CHN analysis


2021 ◽  
Vol 68 (2) ◽  
pp. 395-403
Author(s):  
Nataliia Krasovska ◽  
Viktor Stavytskyi ◽  
Inna Nosulenko ◽  
Oleksandr Karpenko ◽  
Oleksii Voskoboinik ◽  
...  

The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-с]quinazolines that were used as initial compounds for chemical modification aimed to the introduction of amide fragment to the molecule. The IR, 1H NMR and chromato-mass spectral data of obtained compounds were studied and discussed. Obtained substances were studied for anti-inflammatory activity using carrageenan-induced paw inflammation model. Amides of ([1,2,4]triazolo[1,5-с]quinazoline-2-yl)alkyl carboxylic acids were detected as promising class of anti-inflammatory agents for further purposeful synthesis and profound study of anti-inflammatory activity.


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.


2009 ◽  
Vol 6 (4) ◽  
pp. 1055-1062 ◽  
Author(s):  
Manish Srivastav ◽  
MD. Salahuddin ◽  
S. M. Shantakumar

A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with various substituted amine. The compounds (IIa-d) prepared by treating 2-[(chloroacetyl) amino] benzoic acid with different 2-amino-6-substituted benzothiazole. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolines-4-one derivative were investigated for their anti-inflammatory and antibacterial activity.


2002 ◽  
Vol 70 (3) ◽  
pp. 277-286 ◽  
Author(s):  
Khan M.S.Y. ◽  
Husain A. ◽  
Hasan S.M. ◽  
Akhter M.

Various amide-based prodrugs of sulphonamides have been synthesised by condensing appropriate sulphonamide moiety with different β-aroyl propionic acids. All the compounds have been evaluated for their antimicrobial and anti-inflammatory activities. Their structures were established on the basis of elemental analysis, 1H NMR and Mass spectral data. Some of these compounds were found to have significant activity


2020 ◽  
Vol 32 (3) ◽  
pp. 607-611
Author(s):  
H. Hayun ◽  
R.N. Fauzan ◽  
N.T. Wibowo ◽  
A. Asrianingtiyas ◽  
N. Afriliana ◽  
...  

Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazole compounds, namely 2-methoxy-4-(1-phenyl-3-methyl-1H-pyrazol-5-yl)phenol (1) and its aminomethyl derivatives (2a-e) were evaluated for their anti-inflammatory potentiality. The structures of the synthesized compounds were elucidated using FTIR, NMR (1H & 13C) and mass spectral data. The study found that the activity of aminomethyl derivatives (2a-e) was higher than that of parent compound 1. In this series, aminomethyl derivatives bearing dimethylamino-methyl, diethylaminomethyl and pyrrolidinomethyl moieties (2a, 2c and 2e, respectively) were more active than diclofenac sodium, which was used as a standard. A study on the structure-activity relationship (SAR) suggested that the activity of aminomethyl moiety of the compound was influenced by its pKa value. Thus, novel compounds act as potential anti-inflammatory agents.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Chatrasal Singh Rajput ◽  
Shiwani Singhal

A series of 3-[2′-(Substitutedbenzylideneamino)phenyl]-2-methyl-6-substituted quinazolin-4-ones (5–10), 3-[2′-(3″-chloro-2″-oxo-4″-substitutedphenylazetidin-1″-yl)phenyl]-2-methyl-6-substitutedquinazolin-4-ones (11–16), and 3-[2′-(2″-substitutedphenyl-4″-oxo-1″,3″-thiazolidin-3″-yl)phentl]-2-methyl-6-substitutedquinazolin-4-ones (17–22) have been synthesized in the present study. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, H1 NMR, and mass spectral data. All the newly synthesized compounds were screened for anti-inflammatory and analgesic activities.


1978 ◽  
Vol 33 (4) ◽  
pp. 425-428 ◽  
Author(s):  
M. I. Ali ◽  
M. M. S. El-Morsy ◽  
N. M. Hassan ◽  
M. Sharaf

AbstractThe structure of some naphthoylacetanilides (1) obtained from a new route of synthesis is elucidated via inspection of IR, NMR, and mass spectral data. Napthoylacetanilides condensed with one or two moles of aromatic aldehyde to give 2-(naphthoyl)-cinnamanili-des (2) or 3-aryl-2,2′-dinaphthoyl-glutaric acid dianilides (3). Compound 2b added phenylmercaptan to give 3-phenyl 3-phenylthio-2-naphthoyl-propananilide (4). Reduction of 2b gave 2-benzyl 2-(2-naphthoyl)acetanilide (5). 1 is coupled with aryldiazonium salt to give 2-oxo naphthoylacetanilides-2-arylhydrazones (6). The mechanism of the reactions is discussed.


2009 ◽  
Vol 6 (s1) ◽  
pp. S123-S128 ◽  
Author(s):  
S. Arunkumar ◽  
K. Ilango ◽  
R. S. Manikandan ◽  
N. Ramalakshmi

In the present study, a new series of [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) have been synthesized. 3, 4, 5-Trihydroxy benzohydrazide (1) was synthesized from propyl gallate and hydrazine hydrate in presence of ethanol. Chalcones (2a-j) were synthesized from acetanilide and various aromatic aldehydes in presence of ethanol and sodium hydroxide solution. By refluxing the compound (1) and compounds (2a-j) in presence of ethanol yielded [5-substituted-3-(phenylamino)-4.5-dihydropyrazol-1yl] (3,4,5-trihydroxy phenyl)-methanone (3a-j). The final compounds [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) were synthesized by treating compounds (3a-j) with bromine water. The synthesized compounds have been characterized by IR,1HNMR and Mass spectral data. The compounds were evaluated forin vivoanti-inflammatory activity by carrageenan induced paw edema test. In general all compounds were found to exhibit good anti-inflammatory activity.


2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.


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