ChemInform Abstract: Synthesis and Evaluation of N‐(α‐Benzamido cinnamoyl) Aryl Hydrazone Derivatives for Antiinflammatory and Antioxidant Activities.

Rajitha, Galla; Saideepa, N; Pallerla, Praneetha

doi:10.1002/chin.201136067

Cited by 24 publications

(29 citation statements)

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“…The deep yellow colour of oxazolone immediately changed to light yellow colour product, which was filtered, washed, used in next step [16] General procedure for the synthesis of 2-benzamido-N'-(substituted)-3-(thiophen-2yl)acrylohydrazide (4a-l): Equimolar ratios of α-benzamido-(4-nitro)-cinnamal-hydrazide and different benzaldehydes (0.01 mol) in absolute ethanol with a few drops of glacial acetic acid were transferred in to reaction flask and allowed to microwave irradiation at 160 watts with 15 s of interval for about 60-180 s. The reaction was monitored by TLC and the mixture was allowed to cool at room temperature, filter and purified by recrystallization from methanol. The physical data of all the title compounds were given below: in vivo Antiinflammatory activity: The in vivo antiinflammatory activity of all the title compounds was evaluated using carrageenan-induced hind paw edema test in male albino rats (150-180 g) of Wistar strain at 100 mg/kg body weight [17].…”

Section: Methodsmentioning

confidence: 99%

Microwave Assisted Synthesis, Characterization, Molecular Docking, Antiinflammatory and Analgesic Activity of Acylhydrazones Bearing Thiophene Moiety

Soujanya¹,

Rajitha²

2017

Asian J. Chem.

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NSAIDS are the first drug of choice in the treatment of inflammation has several side effects and still there is a need to introduce a new effective agent. In the present study, N-acylhydrazones bearing thiophene moiety were synthesized by applying bioisosterism drug design tool, characterized, screened for anti-inflammatory, analgesic activity and molecular docking using GLIDE. All the compounds viz., 2-benzamido-N'-(substituted)-3-(thiophen-2-yl)acrylohydrazides (4a-l) were synthesized by the microwave irradiation of compound 2-(benzamido)-3-(thiophen-2-yl)acrylohydrazide (3) with different aromatic/heteroaromatic aldehydes in acidic conditions by microwave irradiation and characterized by IR, 1 H & 13 C NMR, Mass spectra, followed by elemental analysis. Compound 4j showed slightly superior anti-inflammatory and analgesic activity (76 and 64 %) than standard (73 %, 62 %). The above results were supported by molecular docking studies done by using COX-2 protein revealed, compound (4j,4d) have -9.77, -9.58 as docking score which is higher than standard (-7.18). The present study concludes the potentiality of acylhydrazones to further developed as effective anti-inflammatory agents.

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Section: Methodsmentioning

confidence: 99%

Microwave Assisted Synthesis, Characterization, Molecular Docking, Antiinflammatory and Analgesic Activity of Acylhydrazones Bearing Thiophene Moiety

Soujanya¹,

Rajitha²

2017

Asian J. Chem.

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“…246°C [15][16]; IR KBr (cm 4-(1-(2-(3-methylquinoxalin-2-yl) 2-(1,3-dihydro-2H-inden-2-ylidene) (2-methylquinoxalin-3-yl)-2-((naphthalen-1-yl) …”

Section: Synthesis Of 3-methylquinoxaline-2(1h)-onementioning

confidence: 99%

“…Quinoxaline, or 1,4-benzo[pyrazine is an important structural unit among nitrogencontaining heterocyclic compounds. Quinoxalines are, in general, easy to prepare and numerous derivatives have been reported in the literature because of their biological activity, specifically as antimicrobial [2][3][4][5][6][7][8], antibacterial [9][10][11], anti-cancer [12], antiaminoceptive [13], anti-inflammatory [14,15] anti-viral [16][17][18], antimalaria [19] agents. They possess well known biological activities including AMPA/GlyN receptor antagonist [20], antihistaminic agents [21], anti-trypanosomal activity [22], anti-herps, trypanocida, antiplasmodial activity [23], Ca 2+ uptake/release inhibitor [24], and inhibitor of vascular smooth muscle cell proliferation.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Biological Evaluation of Some Novel 3-Methlyquinoxaline-2-Hydrazone Derivatives

Taiwo¹,

Em²,

Ij³

et al. 2017

Organic Chem Curr Res

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Alzheimer's disease is a chronic and progressive neurodegenerative disease which occurs due to lower levels of acetylcholine neurotransmitters, and results in a gradual decline in memory and other cognitive processes. Acetylcholinesterase and butyrylcholinesterase have been reported to be the primary regulators of the acetylcholine levels in the brain. Evidence shows that acetylcholinesterase activity decreases in Alzheimer's disease, while activity of butyrylcholinesterase elevate in advanced Alzheimer's disease, which suggests a key involvement of butyrylcholinesterase in acetylcholine hydrolysis during Alzheimer's disease symptoms. In order to sustain the level of remaining acetylcholine, acetylcholinesterase and butyrylcholinesterase inhibitors may be used. Therefore, inhibiting the activity of butyrylcholinesterase may be an effective way to control Alzheimer's disease associated disorders. In this study, eleven 3-methylquinoxaline-2-hdrazones were synthesized from the reactions of 3-methylquinoxaline-2-hydrazine with different substituted aromatic ketones and aromatic aldehyde. All the newly synthesized compounds have been characterized on the basis of IR, 1 H-NMR and 13 H-NMR spectral data as well as physical data. All the synthesized compounds were biologically evaluated against cholinesterases (acetylcholinesterase and butyrylcholinesterase). Compounds 2-12 were found to be a good selective inhibitor for acetycholinesterase and butyrylcholinesterase. Among the series, compounds 6 (IC 50 =170 ± 30 µg/mL) and 10 (IC 50 =180 ± 10 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 2 (IC 50 =780 ± 10 µg/mL), 5 (IC 50 =550 ± 10 µg/mL) and 6 (IC 50 =790 ± 10 µg/mL), were found to be most active inhibitor against butyrylcholinesterase. The IC 50 values for all the synthesized compounds were lower than standard, eserine (IC 50 =70 ± 20 µg/mL). Their considerable acetylcholinesterase and butyrylcholinesterase inhibitory activities makes them a good candidate for the development of selective acetycholinesterase and butyrylcholinesterase inhibitors.

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“…[124], [125] were showed Analgesic and antiinflammatory activity (Hernandez et al, 2012). The antiinflammatory activity exhibited by some aryl hydrazones [126] ( Rajitha et al 2011). Various hydrazone derivatives [127] have promising in-vivo anti-inflammatory activity (Moldovan et al, 2011).…”

Section: Leishmanicidal Activitymentioning

confidence: 99%

Pharmacologically potentials of hydrazonone containing compounds: a promising scaffold

Asif

2014

International Journal of Advanced Chemistry

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ChemInform Abstract: Synthesis and Evaluation of N‐(α‐Benzamido cinnamoyl) Aryl Hydrazone Derivatives for Antiinflammatory and Antioxidant Activities.

Cited by 24 publications

References 0 publications

Microwave Assisted Synthesis, Characterization, Molecular Docking, Antiinflammatory and Analgesic Activity of Acylhydrazones Bearing Thiophene Moiety

Microwave Assisted Synthesis, Characterization, Molecular Docking, Antiinflammatory and Analgesic Activity of Acylhydrazones Bearing Thiophene Moiety

Design, Synthesis and Biological Evaluation of Some Novel 3-Methlyquinoxaline-2-Hydrazone Derivatives

Pharmacologically potentials of hydrazonone containing compounds: a promising scaffold

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