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.

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 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

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 Green Synthetic Protocol for (E)-1-Aryl-3-(2-morpholinoquinolin- 3-yl)prop-2-en-1-ones and Their Antimicrobial Activity

2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
13C Nmr ◽  
Mass Spectral Data ◽  
In Vitro Antimicrobial Activity ◽  
Mass Spectral ◽  
Fungal Organisms

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.

scholarly journals Binuclear Rhenium and Manganese Carbonyl Compounds Containing Hetero-Mercaptanes

2012 ◽  
Vol 25 (1) ◽  
pp. 62-70 ◽  
Author(s):  
Md Anwarul Hoque ◽  
Md Arzu Miah ◽  
Md Nurul Abser ◽  
Abul K Azad ◽  
Kamrun N Khan ◽  
...  
Keyword(s):  
Ambient Temperature ◽  
Spectral Data ◽  
1H Nmr ◽  
Metal Atom ◽  
Carbonyl Compounds ◽  
Chemical Society ◽  
Mass Spectral Data ◽  
Heterocyclic Ligands ◽  
Mass Spectral ◽  
Manganese Carbonyl

Treatment of 2-Mercaptothiazoline, 2-Mercaptobenzimidazole, 2-Mercapto-1- methylimidazole with [M2(CO)10] (M = Re and Mn) at ambient temperature in presence of decarbonylating reagent Me3NO give the complexes [Mn2(?-?2-C3H4NS2)2(CO)6] (1), [Re2(?-?2-C3H4NS2)2(CO)6] (2), [Mn2(?-?2-C7H5SN2)2(CO)6] (3), [Re2(?-?2- C7H5SN2)2(CO)6] (4), [Re2(?-?2-C4H5N2S)2(CO)6] (5) and [Re2(?1-C4H5N2SH)(CO)9] (6) respectively. All the compounds have been characterized by IR, 1H NMR and mass spectral data. The heterocyclic ligands are expected to be coordinated to two or single metal atom through the nitrogen and sulfur atoms or via only sulfur atom.DOI: http://dx.doi.org/10.3329/jbcs.v25i1.11775 Journal of Bangladesh Chemical Society, Vol. 25(1), 62-70, 2012> 

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, 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 N-[2-(1H-Indol-3-yl)ethyl]-2-(4-isobutylphenyl)propanamide

Molbank ◽  
10.3390/m1031 ◽  
2018 ◽  
Vol 2018 (4) ◽  
pp. M1031
Author(s):  
Stanimir Manolov ◽  
Iliyan Ivanov ◽  
Yulian Voynikov
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Magnetic Resonance ◽  
Spectral Data ◽  
1H Nmr ◽  
13C Nmr ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Nuclear Magnetic

The compound in the title was prepared by reaction between tryptamine and ibuprofen using N,N′-dicyclohexylcarbodiimide as a “dehydrating” reagent. The structure of the newly synthesized compound was determined by nuclear magnetic resonance (NMR) (1H-NMR and 13C-NMR), UV, IR, and mass spectral data.

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