scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones

2009 ◽  
Vol 6 (4) ◽  
pp. 1055-1062 ◽  
Author(s):  
Manish Srivastav ◽  
MD. Salahuddin ◽  
S. M. Shantakumar
Keyword(s):  
Antibacterial Activity ◽  
Benzoic Acid ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Substituted 1 ◽  
Amino Benzoic Acid

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.

scholarly journals Synthesis, Characterization, and Anti-Inflammatory Activity of Newer Quinazolinone Analogs

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Chatrasal Singh Rajput ◽  
Shiwani Singhal
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Analgesic Activities

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.

scholarly journals Quinazoline-containing Hydrazydes of Dicarboxylic Acids and Products of Their Structural Modification: A Novel Class of Anti-inflammatory Agents

2021 ◽  
Vol 68 (2) ◽  
pp. 395-403
Author(s):  
Nataliia Krasovska ◽  
Viktor Stavytskyi ◽  
Inna Nosulenko ◽  
Oleksandr Karpenko ◽  
Oleksii Voskoboinik ◽  
...  
Keyword(s):  
Chemical Modification ◽  
Spectral Data ◽  
1H Nmr ◽  
Structural Modification ◽  
Dicarboxylic Acids ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Amide Fragment

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.

Synthesis, Characterization and Evaluation of Azetidinylquinolines and Thiazolidinylquinolines as Antibacterial Agents

2014 ◽  
Vol 7 (3) ◽  
pp. 2536-2543
Author(s):  
Shalabh Sharma ◽  
Kuldeep K Saxena
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Antibacterial Agents ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
New Compounds

Several molecules were synthesized like 8-ethoxy-4-methyl-2-amino-(3’-chloro-2’-oxo-4’-substitutedaryl-1’-azeti-dinyl)-quinolines 8-12 and 8-ethoxy-4-methyl-2-amino-(2’-substitutedaryl-4’-oxo-1’,3’-thiazolidin-3’-yl)quinolines 13-17 from 8-ethoxy-4-methyl-2-(substitutedarylidenylimino amino)-quinolines 3-7, and screened to evaluate their antibacterial activity against numerous strains of bacteria        in vitro. The structures of new compounds were established on the basis of their elemental analysis, IR, 1H-NMR and mass spectral data. The results showed that three compounds 10, 11 and 16 were found to exhibit promising antibacterial activity as compared to the standard drug amphicillin.   

scholarly journals SYNTHESIS OF SOME NEW PRODRUGS OF SULPHONAMIDES AND STUDIES ON THEIR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTION

2002 ◽  
Vol 70 (3) ◽  
pp. 277-286 ◽  
Author(s):  
Khan M.S.Y. ◽  
Husain A. ◽  
Hasan S.M. ◽  
Akhter M.
Keyword(s):  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Significant Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Inflammatory Action

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

Synthesis, spectral description, and lipophilicity parameters determination of phenylcarbamic acid derivatives with integrated N-phenylpiperazine moiety in the structure

2006 ◽  
Vol 60 (1) ◽  
Author(s):  
I. Malík ◽  
E. Sedlárová ◽  
J. Csöllei ◽  
F. Andriamainty ◽  
P. Kurfürst ◽  
...  
Keyword(s):  
Neural Network ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Computer Programs ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
The Neural Network ◽  
Lipophilicity Parameters

AbstractThe phenylcarbamic acid derivatives with N-phenylpiperazine moiety in the molecule have been prepared. The structure has been confirmed by elemental analysis, IR, 1H NMR, and mass spectral data. For the prepared set of the compounds the lipophilicity parameters have been determined. The experimentally obtained lipophilicity parameters have been correlated with theoretical entries obtained by different computer programs based on the neural network and fragmental methods.

scholarly journals Synthesis and Antimicrobial Activity of (2-Methoxy/2-Amino)-6-{4'-[(4'''-Chlorophenyl) (Phenyl) Methyl Amino] Phenyl}-4-Aryl Nicotinonitrile

2015 ◽  
Vol 49 ◽  
pp. 99-103
Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Layer Chromatography

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.

scholarly journals Synthesis, Anti-inflammatory Activity and in silico Studies of Some Novel Morpholine Based Carboxamides

2020 ◽  
Vol 32 (4) ◽  
pp. 901-906
Author(s):  
Premanand M. Honavar ◽  
Vasantha Kumar ◽  
P. Nikhil ◽  
Naveen Kumar ◽  
S. Sreenivasa ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Rat Paw Edema ◽  
Amide Derivatives ◽  
In Silico Studies ◽  
Anti Inflammatory ◽  
Docking Interaction ◽  
Rat Paw ◽  
Aromatic Heterocyclic

Two series of carboxamides were synthesized from 3-fluoro-4-morpholinoaniline and different substituted aromatic/heterocyclic carboxylic acids. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The newly synthesized amide derivatives were screened for anti-inflammatory activity by following carrageenan induced rat paw edema method. Among the compounds screened, compound 6e was found to be highly potent. Molecular docking interaction of active compounds revealed that effective binding was observed in the pocket of COX-I and COX-II proteins.

SYNTHESIS, DOCKING STUDY AND ANTI-INFLAMMATORY STUDIES OF SOME FLAVANONES

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 54-60
Author(s):  
Ishwar K. Bhat ◽  
Keyword(s):  
Diclofenac Sodium ◽  
Docking Study ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Ligand Interaction ◽  
Standard Drug ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory ◽  
Phosphoinositide 3 Kinase

In this work, a series of flavanones (P1-P9) was synthesized by cyclization of substituted (hydroxyphenyl)- 3-(phenyl) prop-2-en-1-ones (S1-S9). The structures of the synthesized compounds were characterized by IR, 1 H NMR and mass spectral data. These derivatives were evaluated for anti-inflammatory activity. Compounds P1, P3, P6 and P7 showed excellent anti-inflammatory activity as compared to standard drug diclofenac sodium. Molecular docking of these flavanones (P1-P9) was also performed with receptor phosphoinositide-3-kinase PI3Kδ (PDB code: 5ITD). All the flavanones (P1-P9) were docked into same groove of the binding site of native co-crystallized (5-{4-[3-(4-acetylpiperazine-1-carbonyl) phenyl] quinazolin-6-yl}-2-methoxypyridine carbonitrile) ligand for activity explanation and exhibited good ligand interaction and binding affinity were of range -4.57 to -8.79kcal/mol.

scholarly journals Synthesis New of Nucleoside of 1,3-bis-(2,3,5-tri-O-Benzoyl-β-D-Ribofuranosyl)-8-(Trifluoromethyl)-2-Methyl-4-Quinazolinone

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 57
Author(s):  
Laila Mohammed Break ◽  
Wafa Saad Al-harthi
Keyword(s):  
Benzoic Acid ◽  
Spectral Data ◽  
Chemical Stability ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Sodium Metal ◽  
Fluorine Compounds ◽  
Fluorinated Nucleosides

Fluorinated nucleosides are very important for increased biological and chemical stability of organ fluorine compounds. Synthesis of (1H)-8-trifluloromethyl-2-methyl-4-quinazolinone 3 from 2-amino-3-(trifluoromethyl) benzoic acid 1 was performed. Ribosylation of compound 4 with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-d-ribofuranose 5 using the silylation method created the benzoylated nucleoside derivative 6. Debenzoylation of the protected nucleoside 6 via reaction with sodium metal in dry methanol to create the corresponding free nucleoside 1,3-bis-(2,3,5-tri-O-benzoyl-β-d-ribofuranosyl)-8-(trifluoromethyl)-2-methyl-4-quinazolinone 7. The structures of the newly synthesis compounds have been confirmed on the basis of IR, 1HNMR, 13CNMR, and mass spectral data.

Partially oxidized porphyrazines

2006 ◽  
Vol 10 (07) ◽  
pp. 996-1002 ◽  
Author(s):  
Ayhan Nazli ◽  
Ergün Gonca ◽  
Ahmet Gül
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Trifluoroacetic Acid ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Ft Ir ◽  
New Compounds

Magnesium porphyrazinate substituted with eight (1-naphthyl) groups on the peripheral positions has been synthesized by cyclotetramerization of 3,4-(1-naphthyl)pyrroline-2,5-diimine, 4-(1-naphthyl)pyrroline-2,5-diimine in the presence of magnesium butanolate. Its demetalation by treatment with trifluoroacetic acid, resulted in a partially oxidized product, namely, octakis(1-naphthyl)-2-seco-porphyrazine-2,3-dione. Further reaction of this product with copper(II) acetate, zinc(II) acetate and cobalt(II) acetate led to the metallo derivatives, [octakis(1-naphthyl)-2-seco-2,3-dioxoporphyrazinato]M(II) ( M = Cu , Zn or Co ). These new compounds have been characterized by elemental analysis, together with FT-IR, 1 H NMR, UV-vis and mass spectral data.

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