scholarly journals Synthesis and Anti-Inflammatory Activity of a Novel Series of Diphenyl-1,2,4-triazoles and Related Derivatives

2012 ◽  
Vol 9 (4) ◽  
pp. 2510-2515 ◽  
Author(s):  
Swapna Cherala ◽  
Harikiran Lingabathula ◽  
Rama Ganta ◽  
Srinivas Ampati ◽  
Sarangapani Manda
Keyword(s):  
Spectral Analysis ◽  
Rat Model ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Mass Spectral Analysis ◽  
Thiourea Derivatives ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory

In the present investigation we have synthesized a series of new 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]urea and 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]thiourea derivatives (4Ia - 4IId). The newly synthesised derivatives were characterized by using the data of IR,1H NMR and Mass Spectral analysis. Thus synthesised and characterized targetted compounds were further screened for their anti-inflammatory activity by using Carrageenan – induced paw edema rat model. Among all the newly synthesized derivatives, Compounds 4Ia-4Ic and Compounds 4IIa-4IId were reduced the inflammation very significantly (p<0.0001), thus these compounds showed promising anti-inflammatory activity and only one compound (4Id) showed moderate anti-inflammatory activity (p<0.05).

scholarly journals Preparation and Characterization of New 1,3,5-Trisubstituted-2-Pyrazolines Derivative for their Anti-Inflammatory Activity

2021 ◽  
pp. 992-1004
Author(s):  
Jitendra Kumar Chaudhary ◽  
Alok Pal Jain ◽  
O. P. Tiwari
Keyword(s):  
Inflammatory Activity ◽  
Paw Edema ◽  
Mass Spectral Analysis ◽  
Phenyl Hydrazine ◽  
Design Synthesis ◽  
Standard Drug ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Relevant Degree

The objective of the paper was to design, synthesis and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for anti-inflammatory potential. The 1,3,5-tri-substituted-2-pyrazolines derivatives has been synthesized by the reaction of chalcone     derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total Sixteen compounds has been synthesized and characterized by the IR, 1HNMR and mass spectral analysis. Proposed compounds have been evaluated for anti-inflammatory activity. Anti-inflammatory activity of the compounds carried out by two animal     model i.e. Carrageenan induced, paw edema in rats and Inhibition of formalin induced paw edema in rats. Anti-inflammatory activity of the compounds C7, C8 and C2 were shown 98.26,  92.77 and 96.24 percentages of inhibition and compounds D7, D8 and D2  were shown 81.50, 83.81 and 78.32 percentages of inhibition as compared to the standard drug Diclofenac at 10 mg/kg was inhibit the inflammation 99.42 % after 6h. These result is a evident that synthesized compounds show relevant degree of anti-inflammatory activity as compared to the standard drug. It is also concluded that the presence of SO2NH2 group, Cl, CH3, OCH3 and N(CH3)2 group may provide the active compounds when attached to the pyrazoline group. But the addition of OH, Br and no substitution in phenyl ring may diminish the activity. 

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.

Synthesis of novel pyridazinyl benzimidazole, benzothiazole and benzoxazole of Expected Anti-Inflammatory Activity

2009 ◽  
Vol 2009 (7) ◽  
pp. 448-451 ◽  
Author(s):  
Hanan M. Refaat ◽  
Omneya M. Khalil ◽  
Suzan M. Abuel-Maaty
Keyword(s):  
Butyric Acid ◽  
Elemental Analysis ◽  
Inflammatory Activity ◽  
Reference Standard ◽  
Paw Edema ◽  
H Nmr ◽  
Cyclic Anhydrides ◽  
Anti Inflammatory ◽  
New Compounds

In this study, a novel series of 6-oxopyridazinyl benzazoles and 3, 6-dioxopyridazinyl benzazoles were prepared from the starting compounds, 2-hydrazinobenzimidazole, 2-hydrazinobenzothiazole and 2-hydrazinobenzoxazole by reaction with butyric acid derivatives and cyclic anhydrides respectively. The structures of the new compounds were confirmed by elemental analysis as well as 1H NMR, IR and MS data. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity using carrageenan induced paw edema at dose 100 mg kg−1 using indomethacin as a reference standard and were found to be bioactive.

Synthesis of symmetrical and unsymmetrical subphthalocyanine dimers containing a hydroquinone bridge

2013 ◽  
Vol 17 (12) ◽  
pp. 1167-1172 ◽  
Author(s):  
Lakshmi C. Kasi Viswanath ◽  
Laura D. Shirtcliff ◽  
K. Darrell Berlin
Keyword(s):  
Spectral Analysis ◽  
Chlorine Atom ◽  
Pressure Vessel ◽  
Molar Ratio ◽  
Mass Spectral Analysis ◽  
New Approach ◽  
Mass Spectral ◽  
H Nmr ◽  
C Nmr

Three novel hydroquinone-based symmetrically and unsymmetrically substituted subphthalocyanine (SubPc) dimers have been synthesized through the axial substitution of the macrocycle. The mono SubPc hydroquinone derivative (Hq-SubPc) first prepared acts as a nucleophile which replaces the chlorine atom of the second SubPc molecule to form the dimer. The dimers were obtained by reacting hydroquinone and the respective SubPcs in a 1:1 molar ratio in toluene at 180 °C in a pressure vessel. This new approach allowed stoichiometric quantities of reactants to be utilized. All dimers were characterized by 1 H NMR, 13 C NMR, UV-vis, fluorescence and mass spectral analysis.

scholarly journals Inhibition of Formalin Induced Paw Edema in Rats by Various Fractions/Extracts of Bryophyllum pinnatum

2019 ◽  
Vol 7 (2) ◽  
pp. 63-66
Author(s):  
R. K. Gupta ◽  
M. Lohani ◽  
R. Vishwakarma
Keyword(s):  
Rat Model ◽  
Leaf Extract ◽  
Marked Decrease ◽  
Inflammatory Diseases ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Inflammatory Drug ◽  
Anti Inflammatory ◽  
Bryophyllum Pinnatum

Traditionally, Bryophyllum pinnatum is used in the management of arthritis and inflammatory diseases. However, B. pinnatum has not been analysed previously for anti-inflammatory activity. Hence, this study is designed to determine the anti-inflammatory effects of various fractions of B. pinnatum leaf extract using rat model of formalin-induced paw edema. Treatment with various fractions showed marked decrease in formalin-induced paw volume and edema in rats. The results of BPAAF treatment were comparable to standard drug, diclofenac. These results indicate that B. pinnatum could be developed as ant-inflammatory drug after further studies.

scholarly journals Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents

2008 ◽  
Vol 58 (4) ◽  
pp. 467-477 ◽  
Author(s):  
Mohammad Amir ◽  
Sadique Javed ◽  
Harish Kumar
Keyword(s):  
Lipid Peroxidation ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Test Results ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents Twelve new 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones (7-18) have been synthesized by reacting 1-aryl-3-(1H-indol-3-yl)-2-propen-1-one with urea and thiourea in ethanolic potassium hydroxide. Their structures have been confirmed by IR, 1H NMR and mass spectral data. The compounds were tested for their anti-inflammatory activity. Test results revealed that compounds showed 49.5 to 70.7% anti-inflammatory activity where-as the standard drug ibuprofen showed 86.4% activity at the same oral dose. Four compounds, 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-one (8), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-one (10), 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (14), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (16), that showed significant anti-inflammatory activity were selected to study their ulcerogenic and lipid peroxidation activities. All tested compounds showed significant reduction in the ulcerogenic potential and lipid peroxidation compared to the standard drug ibuprofen.

scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel 2,4-Diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine Derivatives

2009 ◽  
Vol 6 (2) ◽  
pp. 495-503 ◽  
Author(s):  
P. Venkatesh ◽  
S. N. Pandeya
Keyword(s):  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Second Step ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Methoxy Groups ◽  
Anti Inflammatory ◽  
Sar Study ◽  
New Compounds

A series of some novel 2,4-diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine derivatives were synthesized and evaluated for anti-inflammatory activity. In the SAR study, the phenyl ring on 3 and 4 position of 1,2,4-thiadiazolidine ring substituted with chloro, nitro and methoxy groups showed better activity. The title compounds were synthesized from two steps; the first step involved the synthesis of diaryl substituted thioureas then, it was cyclised to give the 1,2,4-thiadiazole system in the presence of oxidizing agent (hydrogen peroxide and concentrated hydrochloric acid) in the second step. The purity of the synthesized compounds were judged by their C, H and N analysis and the structure was analyzed on the basis of IR, H1NMR, C13NMR and Mass spectral data. The anti-inflammatory activity of new compounds was determined by λ-Carrageenan induced mice paw edema method using diclofenac sodium as a standard. Among the compounds tested four compounds, B2 (2,4-diphenyl-3,5-bis(3-nitrophenylimino)-1,2,4-thiadiazolidine), B4 (2,4-diphenyl-3,5-bis(3-chlorophenylimino)-1,2,4-thiadiazolidine), B6 (2,4-diphenyl-3,5-bis(4-methoxyphenylimino)-1,2,4-thiadiazolidine) and B7 (2,4-diphenyl-3,5-bis (2-methoxyphenylimino)-1,2,4-thiadiazolidine) were the most active compounds in these series.

scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel Pyrazole Derivatives of Gallic Acid

2009 ◽  
Vol 6 (s1) ◽  
pp. S123-S128 ◽  
Author(s):  
S. Arunkumar ◽  
K. Ilango ◽  
R. S. Manikandan ◽  
N. Ramalakshmi
Keyword(s):  
Sodium Hydroxide Solution ◽  
Aromatic Aldehydes ◽  
Inflammatory Activity ◽  
Pyrazole Derivatives ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Derivatives Of

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.

Thiazole-Based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 21 ◽  
Author(s):  
Michelyn Haroun ◽  
Christopher Tratrat ◽  
Evangelia Tsolaki ◽  
Anthi Petrou ◽  
Antonis Gavalas ◽  
...  
Keyword(s):  
Aromatic Aldehyde ◽  
Molecular Modelling ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Chalcone Derivatives ◽  
Treat Ment ◽  
Anti Inflammatory

Background.: Inflammation is a multifactorial process reflecting response of the organismto various stimuli and is associated to a number of disorders such as arthritis, asthma and psoriasis, which require long-lasting or repeated treat-ment. Objective.: The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chal-cone derivatives. Method.: Chalcones were synthesized via Cliazen-Schmidt condensation1-(4-methyl-2-alkylamino)thiazol-5-yl) ethanone with corresponding aromatic aldehyde. For the evaluation of possible anti-inflammatory activity carrageneen mouse paw edema was used. Results.: Eight out of thirteen tested chalcones showed anti-inflammatory activity in range of 51-55%. Prediction of toxicity revealed that these compounds are not toxic. Conclusion.: In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.

scholarly journals SYNTHESIS, CHARACTERIZATION, AND ANTHELMINTIC ACTIVITY OF NOVEL BENZOTHIAZOLE DERIVATIVES CONTAINING INDOLE MOIETIES

2019 ◽  
pp. 321-325
Author(s):  
ALETI RAJAREDDY ◽  
SRINIVAS MURTHY M
Keyword(s):  
Spectral Analysis ◽  
Fourier Transform ◽  
Infrared Spectroscopy ◽  
Magnetic Resonance ◽  
Fourier Transform Infrared Spectroscopy ◽  
Anthelmintic Activity ◽  
Mass Spectral Analysis ◽  
Standard Drug ◽  
Mass Spectral ◽  
Benzothiazole Derivatives

Objective: The objective of this study was to synthesize and evaluate the anthelmintic activity (AA) of novel benzothiazole derivatives containing indole moieties (BDIM). Methods: The present works which involve the substituted isatin Schiff bases undergo acetylating and reacting with 2-aminobenzothiazole to give novel BDIM. Results: All the newly synthesized molecules (5a-5o) were characterized by Fourier-transform infrared spectroscopy, H_nuclear magnetic resonance, and mass spectral analysis along with physical data. The biological potentials of the newly synthesized compounds are evaluated for their AA using an Indian earthworm (Pheretima posthuma), and albendazole was used as standard drug. Conclusion: The synthesized compound 5f, 5n, and 5o showed good AA, whereas others exhibited significant activities.

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