Time filter

Source Type

Gupta S.K.,Hygia Institute of Pharmaceutical Education and Research
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry | Year: 2016

Background: Non-steroidal anti-inflammatory drugs (NSAIDS) are clinically used as anti-inflammatory, analgesic and antipyretic agents but they have the drawbacks such as gastric irritation and gastric ulceration. Recently, quinoline derivatives have shown significant anti-inflammatory and less ulcerogenic activity. The present study deals with the synthesis and pharmacological assessment of a series of novel quinoline derivatives bearing azetidinones scaffolds as anti-inflammatory and analgesic agents. Methods: A series of newer 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4- yl)azetidin-2-one derivatives (6a-l) was synthesized starting with acetanilide (1). Initially, acetanilide (1) was allowed to react with Vilsmeier-Haack reagent (DMF + POCl3) to form 2- chloro-3-formyl quinoline (2). The 2-chloro-3-formyl quinoline (2) was further treated with p-toluenesulphonic acid and sodium azide which yielded Tetrazolo [1,5-1] quinoline-4- carbaldehyde (3). The reaction of formyl group with various substituted amines (4a-l) formed corresponding Schiff base intermediates (5a-l), which were further allowed to react with chloroacetyl chloride to produce 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4-yl) azetidin-2-one derivatives (6a-l). The structure of the final analogues (6a-l) has been confirmed on the basis of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra. All the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities by using carrageenan induced rat paw model and Eddy’s hot plate method respectively. Results: All the values of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra were found to be prominent. The anti-inflammatory activity test revealed that 3-chloro-1-(4-methoxyphenyl)- 4-(tetrazolo[1,5-a] quinolin-4-yl)azetidin-2-one (6b), 3-chloro-1-(2-methoxyphenyl)- 4-(tetrazolo[1,5-a]quinolin-4-yl)azetidin-2-one (6a) exhibited significant anti-inflammatory and analgesic activity as compared to control group. Conclusion: The results of the current study indicate that substitution at quinoline derivatives bearing azetidinones scaffolds showed potent analgesic and anti-inflammatory activities. © 2016 Bentham Science Publishers.


Singh M.,Maharshi Dayanand Saraswati University | Pareek P.K.,Maharshi Dayanand Saraswati University | Chippa H.,Maharshi Dayanand Saraswati University | Ravikant,Hygia Institute of Pharmaceutical Education and Research | Ojha K.G.,Maharshi Dayanand Saraswati University
Collection of Czechoslovak Chemical Communications | Year: 2010

2,3,5,6-Tetrasubstituted-4-aryl-1-(6-ethoxybenzothiazol-2-yl)-1, 4-dihydropyridines were synthesized by the reaction of 2-amino-6- ethoxybenzothiazole, an aromatic aldehyde and an active methylene compound in methanol by conventional or microwave irradiation method (solvent-free or with solid support). All compounds were tested for antibacterial and antifungal activities and the results were compared with standard drugs. Their acaricidal and antifeedant activities were also tested. © 2010 Institute of Organic Chemistry and Biochemistry.


Jawaid T.,Hygia Institute of Pharmaceutical Education and Research | Shakya A.K.,Al-Ahliyya Amman University | Siddiqui H.H.,Integral University | Kamal M.,Integral University
Zeitschrift fur Naturforschung - Section C Journal of Biosciences | Year: 2014

Cucurbita maxima (CM) seed oil is commonly used in Indian folk medicine to treat various ailments. We have investigated the effect of CM seed oil on memory impairment induced by scopolamine in rats. Male adult Wistar rats were administered scopolamine 1 mg=kg body weight, i.p. or 1:25 mg=kg body weight, s.c. to induce memory impairment. The nootropic agent piracetam 100 mg=kg body weight, i.p. and CM seed oil 100 and 200 mg=kg body weight, p.o. were administered daily for five consecutive days. The memory function was evaluated in the Morris water maze (MWM) test, the social recognition test (SRT), the elevated plus maze (EPM) test, and the pole climbing test (PCT). Acetylcholinesterase (AChE) activity and oxidative stress parameters were estimated in the cortex, hippocampus, and cerebellum of the brains after completion of the behavioural studies. The effects of scopolamine on the levels of the tumour necrosis factor alpha (TNF-a) transcript were also investigated. Scopolamine caused memory impairment in all the behavioural paradigms along with a significant increase in the AChE activity and oxidative stress in the brain. Scopolamine also caused a significant increase in the expression of TNF-α in the hippocampus. CM seed oil exhibited antiamnesic activity as indicated by a significant reduction in the latency time in the MWM test and decreased social interaction during trial 2 in the SRT. Further, treatment with CM seed oil significantly decreased the AChE activity and malondialdehyde levels and increased the glutathione level in brain regions. CM seed oil also significantly decreased the expression of TNF-α in the hippocampus. The effect of CM seed oil on behavioural and biochemical parameters was comparable to that observed in rats treated with piracetam. These results indicate that CM seed oil may exert antiamnesic activity which may be attributed to the inhibition of AChE and inflammation as well as its antioxidant activity in the brain. © 2014 Verlag der Zeitschrift für Naturforschung, Tübingen.


Gupta S.,Biotech Park | Misra G.,Hygia Institute of Pharmaceutical Education and Research | Pant M.C.,University of Lucknow | Seth P.K.,Biotech Park
Protein and Peptide Letters | Year: 2012

Head and neck squamous cell carcinoma (HNSCC) is a major cause of cancer related death. The epidermal growth factor receptor (EGFR) pathway is over expressed in HNSCC. EGFR regulates the HNSCC by inducing signalling events responsible for regulating key tumorigenic processes such as proliferation, inhibition of apoptosis, cell adhesion/motility, growth and survival. Present study evaluates the potential of N-(3-Ethynylphenyl)-6, 7-bis (2-methoxyethoxy) quinolin-4-amine as a new inhibitor for EGFR. We have explored the binding and inhibitory potential of the compound using molecular docking, structural interactions fingerprinting and molecular dynamics studies. The inhibitor exhibits extensive interactions with the EGFR catalytic site in the form of hydrogen bonds, pi-pi bond and salt bridges. It shows high specificity and binding affinity towards the protein. The compound can further be explored for its potential to serve in the diagnosis and treatment of HNSCC. The quantitative prediction provides a scope for future experimental testing, facilitating the understanding of the crosstalks between signalling pathways. © 2012 Bentham Science Publishers.


Jawaid T.,Hygia Institute of Pharmaceutical Education and Research | Rai A.,Hygia Institute of Pharmaceutical Education and Research | Kamal M.,Integral University
Asian Journal of Pharmaceutical and Clinical Research | Year: 2015

Objective: The aim of the present study was a comparative study of neuroprotective effect of telmisartan and donepezil against lipopolysaccharide (LPS)-induced neuroinflammation in mice. Methods: In this study, we investigated the comparative effect of telmisartan (5 mg/kg, p.o.) and donepezil (5 mg/kg, p.o.) in systemic inflammation induced by LPS, ibuprofen (40 mg/kg, p.o.) was used as standard. Mice were treated with a single i.c. injection of LPS (5 μg/5 μl/kg), after 7 days the animal behavior was evaluated by testing specific cognitive functions, on Morris water maze and Pole climbing test. Biochemical estimation for glutathione (GSH), malondialdehyde (MDA) and tumor necrosis factor alpha (TNF-α) was done by enzyme-linked immunosorbent assay plate reader. Results: The neuroprotective effect of telmisartan (5 mg/kg) and donepezil (5 mg/kg) in LPS induced neuroinflammation in mice was compared. Oral administration of telmisartan (5 mg/kg) for 7 days shows a better result in Morris water maze and pole climbing test, in comparison of donepezil. It also increases the level of GSH and decreases the level of MDA and TNF-α in mice brain. Conclusion: The present study demonstrates that telmisartan and donepezil reduces LPS-induced microglial activation, beta-amyloid generation, central nervous system cytokine production, and behavioral symptoms of sickness. In comparative study of telmisartan and donepezil, telmisartan shows significant decrease in escape latency time and transfer latency time in comparison of donepezil. Therefore, telmisartan is more effective as the comparative of donepezil. © 2015, Asian Journal of Pharmaceutical and Clinical Research. All Rights Reserved.


Jawaid T.,Hygia Institute of Pharmaceutical Education and Research | Argal S.,Hygia Institute of Pharmaceutical Education and Research | Kamal M.,Integral University
Asian Journal of Pharmaceutical and Clinical Research | Year: 2015

Objective: The investigate the antidiabetic and antihyperlipidemic effect of ethanolic extract of Alocasia indica (EEAI) rhizomes in high-fat diet/streptozotocin (HFD/STZ) and STZ/nicotinamide-induced Type 2 diabetic rats. Methods: Diabetes was induced in male Wistar rats by the administration of a HFD for 15 days/STZ (35 mg/kg b.w., i.p.) and STZ (60 mg/kg b.w., i.p.)/nicotinamide (110 mg/kg b.w., i.p.). EEAI (100 and 200 mg/kg b.w., p.o.) was administered to diabetic rats for 28 days in HFD/STZ-induced Type 2 diabetic rats and for 15 days in STZ/nicotinamide-induced Type 2 diabetic rats. The effect of EEAI on blood glucose and body weight was studied in Type 2 diabetic rats. All these effects were compared with glibenclamide (5 mg/kg b.w., p.o.) as a reference antidiabetic drug. Results: The administration of the EEAI (100 and 200 mg/kg b.w., p.o.) resulted in a significant decrease in blood glucose level and significant increase in body weight in the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetic rats. Further EEAI showed antihyperlipidemic activity as evidenced by significant decrease in serum total cholesterol, triglycerides, low-density lipoprotein cholesterol (LDL-C), very LDL-C levels coupled together with elevation of high-density lipoprotein cholesterol level in diabetic rats in the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetic rats. Conclusion: The results suggest that the EEAI rhizomes possess a promising effect on the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetes. © 2014, Asian Journal of Pharmaceutical and Clinical Research. All Rights Reserved.


Gupta A.,CSIR - Central Electrochemical Research Institute | Pant G.,CSIR - Central Electrochemical Research Institute | Mitra K.,CSIR - Central Electrochemical Research Institute | Madan J.,Hygia Institute of Pharmaceutical Education and Research | And 2 more authors.
Molecular Pharmaceutics | Year: 2014

We investigated whether particles suitable for delivery to alveolar macrophages may provide a means of targeting rapamycin, an inducer of autophagy, to alveolar macrophages as a host-directed antituberculosis agent. Inhalable particles were prepared by spray-drying and characterized using laser scattering and electron microscopy. Their aerodynamic diameter was calculated from bulk and tapped densities. In vitro drug release was studied in PBS containing 1% SDS. In vitro uptake of particles by THP-1 derived macrophages was studied by flow cytometry. Cytotoxicity of the particles toward macrophages and their efficacy against intracellular Mycobacterium tuberculosis were studied using a methyltetrazolium assay and counting bacterial colonies obtained when cell lysates were plated on agar. The encapsulation efficiency was 88.8 ± 1.13% and drug content 22 ± 4% w/w. The particles had a median diameter of 2.88 ± 0.8 μm and appeared as collapsed spheres. Their calculated aerodynamic diameter was about 1 μm. In vitro drug release from the particles was first-order and extended beyond 10 days. Flow cytometry indicated that the particles were taken up by macrophages within 3 h. Macrophages exposed to the particles or rapamycin in solution at a concentration of 100 μg/mL over a 24 h period maintained 79.37 ± 0.72% and 58.33 ± 1.39% viability, respectively. Efficacy studies concluded that particles were more effective in clearing intracellular mycobacteria than rapamycin in solution. It was concluded that the preparation was suitable for formulating as a dry powder inhalation to test efficacy of inhaled, macrophage-targeted rapamycin against TB. © 2014 American Chemical Society.


PubMed | Hygia Institute of Pharmaceutical Education and Research
Type: Journal Article | Journal: Anti-inflammatory & anti-allergy agents in medicinal chemistry | Year: 2016

Non-steroidal anti-inflammatory drugs (NSAIDS) are clinically used as anti-inflammatory, analgesic and antipyretic agents but they have the drawbacks such as gastric irritation and gastric ulceration. Recently, quinoline derivatives have shown significant anti-inflammatory and less ulcerogenic activity. The present study deals with the synthesis and pharmacological assessment of a series of novel quinoline derivatives bearing azetidinones scaffolds as anti-inflammatory and analgesic agents.A series of newer 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4- yl)azetidin-2-one derivatives (6a-l) was synthesized starting with acetanilide (1). Initially, acetanilide (1) was allowed to react with Vilsmeier-Haack reagent (DMF + POCl3) to form 2- chloro-3-formyl quinoline (2). The 2-chloro-3-formyl quinoline (2) was further treated with p-toluenesulphonic acid and sodium azide which yielded Tetrazolo [1,5-1] quinoline-4- carbaldehyde (3). The reaction of formyl group with various substituted amines (4a-l) formed corresponding Schiff base intermediates (5a-l), which were further allowed to react with chloroacetyl chloride to produce 3-chloro-1-(substituted)-4-(tetrazolo [1,5-a]quinolin-4-yl) azetidin-2-one derivatives (6a-l). The structure of the final analogues (6a-l) has been confirmed on the basis of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra. All the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities by using carrageenan induced rat paw model and Eddys hot plate method respectively.All the values of elemental analysis, IR, 1H NMR, 13C NMR and mass spectra were found to be prominent. The anti-inflammatory activity test revealed that 3-chloro-1-(4-methoxyphenyl)- 4-(tetrazolo[1,5-a] quinolin-4-yl)azetidin-2-one (6b), 3-chloro-1-(2-methoxyphenyl)- 4-(tetrazolo[1,5-a]quinolin-4-yl)azetidin-2-one (6a) exhibited significant anti-inflammatory and analgesic activity as compared to control group.The results of the current study indicate that substitution at quinoline derivatives bearing azetidinones scaffolds showed potent analgesic and anti-inflammatory activities.


PubMed | Integral University and Hygia Institute of Pharmaceutical Education and Research
Type: Journal Article | Journal: Journal of advanced pharmaceutical technology & research | Year: 2015

The comparative study of neuroprotective effect of angiotensin converting enzyme inhibitors against scopolamine-induced neuroinflammation in albino Wistar rats was studied. Male albino rats were administered with scopolamine to induce memory impairment. The standard nootropic agent, piracetam (200 mg/kg b.w., [i.p.]), perindopril (0.1 mg/kg b.w., [i.p.]), enalapril (0.1 mg/kg b.w., [i.p.]), and ramipril (0.1 mg/kg b.w., [i.p.]) were administered in different group of animals for 5 days. On 5(th) day, scopolamine (1 mg/kg b.w., i.p.) was administered after 60 min of the last dose of test drug. Memory function was evaluated in Morris water maze (MWM) test and pole climbing test (PCT). Biochemical estimations like glutathione (GSH), malondialdehyde (MDA), and acetylcholinesterase activity in the brain were estimated after completion of behavior study. All three test groups shows improvement in learning and memory in comparison to control group. Perindopril treated group showed a more effective significant decrease in escape latency time and transfer latency time compared to enalapril and ramipril treated group on day 4 in MWM test and PCT, respectively. Perindopril shows a significant reduction in MDA level and acetylcholinesterase activity and a significant rise in GSH level compared to enalapril and ramipril. The finding of this study indicates that Perindopril is more effective in memory retention compared to enalapril and ramipril.


PubMed | Integral University and Hygia Institute of Pharmaceutical Education and Research
Type: Journal Article | Journal: Journal of advanced pharmaceutical technology & research | Year: 2015

To study the estrogenic activity of the hydro-alcoholic extract of Bambusa arundinaceae leaves (HEBA) in female Wistar rats. The dried powdered leaves were extracted with hydroalcoholic mixture (60%), and the resultant extract was subjected for phytochemical analyses to identify different phytoconstituents. HEBA were administered to ovariectomized rats for 7 days at three different doses (viz., 200, 300, 400 mg/kg body weight, p.o.) and their estrogenic activity were compared with each of daily treatment with 0.2 mg/kg body weight, i.p. conjugated equine estrogen as a positive control or olive oil as a negative control. Estrogenic activity was evaluated by doing uterotropic assay, vaginal cytology and measurement of vaginal opening in female Wistar rats. Oral administration of HEBA in ovariectomized immature and mature female Wistar rats in a dose of 400 mg/kg b.w. resulted in significant increase in the uterine wet weight (in mg) (224.82 7.01) and (912.25 27.22) when compared with ovariectomized control rats (111.52 3.17) and (506.67 21.39). HEBA (400 mg/kg b.w., p.o.) treated rats, showing only cornified epithelial cells which was an indication of the presence of the estrogen and also showed 100% vaginal opening. It was observed that HEBA possess significant estrogenic activity at 400 mg/kg b.w., p.o. which was evident by uterotropic assay, measurement of vaginal opening, and histopathological changes.

Loading Hygia Institute of Pharmaceutical Education and Research collaborators
Loading Hygia Institute of Pharmaceutical Education and Research collaborators