scholarly journals Microwave Mediated Organic Reaction: A Convenient Approach for Rapid and Efficient Synthesis of Biologically Active Substituted 1,3-Dihydro-2H-indol-2-one Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Jnyanaranjan Panda ◽  
Biswa Mohan Sahoo ◽  
Nikunja Kishor Mishra ◽  
Sai Krushna Padhi ◽  
Jitendriya Mishra
Keyword(s):  
Anthelmintic Activity ◽  
Mannich Bases ◽  
Biologically Active ◽  
Secondary Amines ◽  
Dependent Manner ◽  
Substituted Anilines ◽  
Standard Drug ◽  
Compound Libraries ◽  
Work First ◽  
Dose Dependent

A simple and efficient method has been developed for the synthesis of 1,3-dihydro-2H-indol-2-one derivatives using microwave irradiation technique. By taking advantage of the efficient source of energy of microwave, compound libraries for lead generation and optimization can be assembled in a fraction of time. In the present work, first the Schiff’s bases are synthesized by reaction of isatin with substituted anilines in the presence of acetic acid under microwave heating. Then the condensation of Schiff bases with different secondary amines in the presence of formaldehyde produces Mannich bases. The newly synthesized Mannich bases were characterized by means of spectral data and then evaluated for anthelmintic activity againstPheretima posthuma(Indian earthworm) and compared with standard albendazole. The compounds were evaluated at the concentrations of 10, 20, and 50 mg/mL. The effect of the standard drug albendazole at 10 mg/mL was also evaluated. The results of the present study indicate that some of the test compounds significantly demonstrated paralysis and also caused death of worms in a dose-dependent manner.

scholarly journals Antinociceptive and Anthelmintic Activities of Leaves of Leea aequata

2018 ◽  
Vol 17 (2) ◽  
pp. 251-255 ◽  
Author(s):  
Sushanta Halder ◽  
Nazmus Saqueeb ◽  
Nazmul Qais
Keyword(s):  
Crude Extract ◽  
Methanol Extract ◽  
Diclofenac Sodium ◽  
Anthelmintic Activity ◽  
Radiant Heat ◽  
Antinociceptive Activity ◽  
Dependent Manner ◽  
Standard Drug ◽  
Dose Dependent ◽  
Crude Methanol Extract

The objective of the study was to evaluate the antinociceptive and anthelmintic activities of the crude methanol extract of leaves of Leea aequata and its fractions. The crude extract and its fractions at 200- and 400-mg/kg bw were subjected to assay for their antinociceptive activity using acetic acid induced writhing and radiant heat tail flicking methods. The ethyl acetate soluble fraction at 400 mg/kg bw induced 40.97% inhibition of writhing in mice while the carbon tetrachloride and chloroform soluble fractions of crude extract at the same dose displayed activity with 40.28% inhibition of writhing as compared to standard diclofenac sodium. The crude extract elongated the reaction time by 57.04% after 30 minute of administration in radiant heat tail flicking method, which suggested the central antinociceptive activity as compared to morphine. The methanol extract of the leaves of L. aequata exhibited profound anthelmintic activity in a dose dependent manner with shortest time of paralysis and death at 100 mg/ml concentration. It caused paralysis of the earthworm Pheretima posthuma at 9.44 min and death at 12.9 min when compared to the standard drug albendazole, which at 10 mg/ml concentration revealed the same at 8.21 minutes and 11.18 minutes, respectively. Dhaka Univ. J. Pharm. Sci. 17(2): 251-255, 2018 (December)

Microwave-assisted synthesis of novel Mannich base and conazole derivatives containing biological avtive pharmacological groups

2020 ◽  
Vol 17 ◽  
Author(s):  
Yıldız Uygun Cebeci ◽  
Sule Ceylan ◽  
Neslihan Demirbas ◽  
Şengül Alpay Karaoğlu
Keyword(s):  
Antimicrobial Activity ◽  
Active Sites ◽  
Sodium Ethoxide ◽  
Mannich Bases ◽  
Biologically Active ◽  
Secondary Amines ◽  
Microwave Assisted Synthesis ◽  
Standard Drug ◽  
Triazole Derivatives ◽  
Microwave Assisted

Background: The aim of this study is to synthesize new Mannich bases and conazol derivatives with biological activity by the microwave-assisted method. Introduction: 1,2,4-Triazole-3-one (3) acquired from tryptamine was transformed to the corresponding carbox(thio)amides (6a-c) via several steps. Compounds, 6a-c, were refluxed with sodium hydroxide to yield 1,2,4-triazole derivatives (7a-c). Compounds 3 and 7a-c on treatment with different heterocyclic secondary amines in an ambiance with formaldehyde afforded the Mannich bases 8-15 having diverse pharmacophore units with biologically active sites. The reaction of compound 3 and 2-bromo-1-(4-chlorophenyl) ethanone in the presence of sodium ethoxide gave the corresponding product yielded the corresponding 2-substituted-1,2,4-triazole-3-one, 16, which was reduced to 1,2,4-triazoles (17). Synthesis of compounds 18, 19, and 20 were carried out starting from compounds 17 with 4-chlorobenzyl chloride (for 18), 2,4- dichlorobenzyl chloride (for 19), and 2,6-dichlorobenzyl chloride (for 20). Method: The conventional technique was utilized for the synthesis of compounds, 3-7, and microwave-assisted technique for the compounds, 8-20. That is, green chemistry techniques were applied during these reactions. The structures molecules were elucidated on the foundation of 1H NMR, 13C NMR, FT-IR, EI-MS methods, and elemental analysis. Novel synthesized molecules were investigated for their antimicrobial activity using MIC (minimum inhibitory concentration) method. Results and Discussion: Aminoalkylation of triazole derivatives 3 and 7a–c with fluoroquinolones such as ciprofloxacin and norfloxacin provided an enhancement to the bioactivity of Mannich bases 8-11 against the tested microorganisms. The MIC values ranged between <0.24 and 3.9 μg/mL”. Moreover, molecules 10 and 11 have more effective on M. smegmatis than the other compounds by the MIC values of <1 μg/mL. They have shown very good antituberculosis activity. Conclusion: Most of the synthesized structures were observed to have excellent antimicrobial activity against most microorganisms taken into account. These molecules have activity better than the standard drug ampicillin and streptomycin.

scholarly journals IN VITRO EVALUATION OF ANTHELMINTIC ACTIVITY OF ETHANOLIC EXTRACT OF CENTELLA ASIATICA LINN. IN INDIAN ADULT EARTHWORMS

2021 ◽  
pp. 39-41
Author(s):  
SWAGATA DATTA ◽  
GEETANJALI NINGTHOUJAM ◽  
CHRISTINA ZOSANGPUII ◽  
PAONAM SHYAMASAKHI ◽  
NAMEIRAKPAM MEENA
Keyword(s):  
Anthelmintic Activity ◽  
Ethanolic Extract ◽  
Centella Asiatica ◽  
Dependent Manner ◽  
Standard Drug ◽  
Gum Acacia ◽  
Significant Difference ◽  
Dose Dependent ◽  
Higher Doses

Objective: Helminthiasis is one of the most prevalent parasitic infestations worldwide posing a major threat to public health. The control of these nematodes has relied largely on the use of a limited number of anthelmintics. However, emerging resistance and side effects to the currently available anthelmintic drugs is a major concern and discovery of newer anthelmintics with a novel mode of action is the need of the hour. The present study is aimed to evaluate the anthelmintic activity of ethanolic extract of Centella asiatica Linn. (EECA) on Indian earthworms (Pheretima posthuma). Methods: The earthworms were divided into 4 groups with 6 worms in each group. The anthelmintic activity of EECA at two different concentrations (25 mg/ml and 50 mg/ml) was evaluated by assessing the time of paralysis and time of death of the worms. Albendazole was used as standard and 2% gum acacia as control. Results: Albendazole at 25 mg/ml showed the highest anthelmintic activity and had significant difference (p<0.001) with EECA at both 25 mg/ml and 50 mg/ml. Conclusion: Both doses of the test drug showed anthelmintic activity but the extract at either dose was found to be less effective than the standard drug. Further studies with higher doses of the extract should be done to evaluate the anthelmintic activity in a dose-dependent manner.

scholarly journals In-vitro Screening for Anthelmintic Potential of Crotalaria retusa on Pheretima posthuma

2019 ◽  
Vol 9 (4-A) ◽  
pp. 340-343
Author(s):  
Rakesh Tirkey
Keyword(s):  
Leaf Extract ◽  
Anthelmintic Activity ◽  
Dependent Manner ◽  
In Vitro Screening ◽  
Standard Drug ◽  
Death Time ◽  
Soxhlet Method ◽  
Dose Dependent

Objective: Aim of the present study is to evaluate the anthelmintic potential of Crotalaria retusa leaf extract on Pheretima posthuma. Methods: Extracts of Crotalaria retusa leaves prepared by Soxhlet method. The extracts were screened for phytochemicals such as alkaloid, flavonoid, tannin, steroids, etc. aqueous (AECR) and ethanolic (EECR) extracts were tested for anthelmintic activity using Indian adult earthworm (Pheretima posthuma). Results: The observation showed that EECR gave shorter paralysis and death time at 100 mg/mL as compared to AECR. Mean±SEM values were calculated for both extract and standard. EECR showed anthelmintic activity in a dose-dependent manner taking the shortest time for paralysis. Conclusion: The result demonstrated that both the investigational extracts showed significant anthelmintic activity (P<0.05) for the time taken for paralysis and death when compared to standard drug mebendazole. Keywords: Crotalaria retusa, Anthelmintic, Pheretima posthuma, phytochemical.

Ecological and physiological as well as biochemical properties of representatives of the Genus sedum L.

2014 ◽  
Vol 25 (3-4) ◽  
pp. 24-33
Author(s):  
O. I. Dzjuba ◽  
M. V. Yatsenko
Keyword(s):  
Nitric Oxide ◽  
Cell Line ◽  
Methanol Extract ◽  
Hepatoma Cell ◽  
Ethanol Extract ◽  
Biochemical Properties ◽  
Biologically Active ◽  
Hepatoma Cell Line ◽  
Dependent Manner ◽  
Dose Dependent

The article deals with the history of the study and the current state of research of physiological and biochemical properties of the plant genus Sedum that are useful for human and has been used in folk medicine for many years. It was noticed that antioxidant properties of extracts from plants S. sarmentosum, S. sempervivoides, S. takesimense were caused by the presence of phenolic compounds. Methanol extract of plants S. takesimense exhibited strong scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals as well as significant inhibitory effects on lipid peroxidation and low density lipoprotein (LDL) oxidation induced by a metal ion Cu2+. Various immunomodulatory activities of various fractions of plants extracts (S. dendroideum, S. kamtschaticum, S. sarmentosum, S. telephium) are observed. It was shown that the ethanol extract of S. sarmentosum and it’s fractions suppressed specific antibody and cellular responses to ovalbumin in mice. The methanol extract of plants S. sarmentosum reduced the levels of anti-inflammatory markers, such as volume of exudates, number of polymorphonuclear leukocytes, suppressed nitric oxide synthesis in activated macrophages via suppressed induction of inducible nitric oxide synthase (iNOS). Polysaccharides fractions from plants S. telephium inducing productions of tumor necrosis factor alpha (TNF-α), increasing the intensity of phagocytosis in vitro and in vivo. Methanol extract from the whole part of S. kamtschaticum strongly inhibit PGE2 production from lipopolysaccharide-induced RAW 264.7 cells, a mouse macrophage cell line via modulating activity in gene expression of the enzyme cyclooxygenase-2 (COX-2). The methanol extract of plants S. sarmentosum and the major kaempferol glycosides from S. dendroideum have antinociceptive activity. It was noticed that anti-adipogenic activity of extracts from plants S. kamtschaticum were caused by inhibition of peroxisome-proliferator-activated receptor γ (PPARγ) expression and it’s dependent target genes, such as genes encoding adipocyte protein 2 (аР2), lipoprotein lipase (LPL), adiponectin and CD36. Polysaccharides fractions from S. telephium cause inhibition of cell adhesion of human fibroblast (MRC5) to laminin and fibronectin via interfere with integrin-mediated cell behaviour and they contributed to the role of polysaccharides in cell-matrix interaction. The methanol extract of plants S. sarmentosum exhibited a significant inhibitory activity in the chick embryo chorioallantoic membrane angiogenesis in a dose-dependent manner. The crude alkaloid fraction of S. sarmentosum caused a dose-dependent inhibition of cell proliferation on murine hepatoma cell line BNL CL.2 and human hepatoma cell line HepG2 without necrosis or apoptosis. Alkaloids from plants S. sarmentosum may improve survival of hepatoma patients via the inhibition of excessive growth of tumor cells. Plant’s juices have antiviral activity (S. sarmentosum, S. spurium, S. stahlii). Crude ethanol extract S. praealtum have spermicidal activity of the in mice and a relevant inhibitory effect of aqueous extract on human spermatozoa motility as well as an anti-fertilizing activity in rats. Hepatoprotective triterpenes, e.g., δ-amyrone, 3-epi-δ-amyrin, δ-amyrin and sarmentolin were isolated from S. sarmentosum. 2- and 2,6-substituted piperidine alkaloids (e.g., norsedamine, allosedridine, sedamine, allosedamine) are observed in plants S. acre, which in the presence of data on the use of pyridine and piperidine derivatives for treating neurodegenerative diseases (e.g., Alzheimer's disease), points on the promising research in this area. Taking into account that biologically active compounds are accumulated in the aboveground vegetative organs of plants of Sedum, the prospects of further study of the use of Sedum for the purposes of biotechnology and in the pharmaceutical industry becomes apparent. This work extends the existing views regarding the use of plants Sedum.

scholarly journals Hepatoprotective effects of Sapium sebiferum in paracetamol-induced liver injury

2015 ◽  
Vol 10 (2) ◽  
pp. 393 ◽  
Author(s):  
Liaqat Hussain ◽  
Muhammad Sajid Hamid Akash ◽  
Madeha Tahir ◽  
Kanwal Rehman
Keyword(s):  
Liver Injury ◽  
Serum Levels ◽  
Therapeutic Effects ◽  
Sapium Sebiferum ◽  
Dependent Manner ◽  
Protective Effects ◽  
Drug Induced ◽  
Standard Drug ◽  
Hepatoprotective Effects ◽  
Dose Dependent

<span><em>Sapium sebiferum</em> leaves were used to determine its hepatoprotective effects against paracetamol-induced hepatotoxicity in mice. A dose dependent study was conducted using two different doses (200 mg/kg and 400 mg/kg) of the extract of </span><em>S. sebiferum</em><span> against toxic effects of paracetamol (500 mg/kg) in experimental animal model. Silymarin (50 mg/kg) was used as standard drug to compare therapeutic effects of </span><em>S. sebiferum</em><span> with control and paracetamol-treated groups. Paracetamol significantly increased the serum levels of liver enzyme markers like alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total bilirubin, and direct bilirubin. The extract showed protective effects by normalizing the liver enzymes markers in a dose dependent manner. Histopathological results confirmed the hepatoprotective effects of leaves of </span><em>S. sebiferum</em><span>. We conclude that leaves of </span><em>S. sebiferum</em><span> have strong hepatoprotective effects against paracetamol-induced liver injury and can be used in liver injuries caused by drug-induced toxicity.</span>

Evaluation of Hepatoprotective activity of Methanol extract of Persicaria hydropiper: An in vivo screening

2021 ◽  
pp. 5819-5824
Author(s):  
Pooja Kamra ◽  
Mahaveer Singh ◽  
Hardarshan Singh Lamba ◽  
Birendra Srivastava
Keyword(s):  
Carbon Tetrachloride ◽  
Intraperitoneal Administration ◽  
Hepatoprotective Activity ◽  
Dependent Manner ◽  
Standard Drug ◽  
Whole Plant ◽  
Dose Dependent ◽  
Histopathological Investigation ◽  
Different Doses

The present study aimed to evaluate the hepatoprotective potential of methanolic whole plant extract of Persicaria hydropiper in carbon tetrachloride (CCl4) induced hepatotoxicity model. Hepatotoxicity was induced in rats by intraperitoneal administration of carbon tetrachloride (CCl4) for seven days. The extract was thereafter administered at two different doses of 200 mg/kg and 400 mg/kg body weight for next seven days. Silymarin was used as a reference standard. The extract revealed hepatoprotective activity in dose dependent manner. The dose of 400 mg/kg exhibited maximum hepatoprotective ability as apparent from several evaluation parameters including liver function profile, bilirubin, antioxidant enzymes as well as histopathological investigation which was comparable to the standard drug Silymarin respectively. These findings sustenance the use of the extract as an adjuvant with existing therapy for treatment of liver ailments.

scholarly journals PRELIMINARY PHYTOCHEMICAL SCREENING AND EVALUATION OF ANALGESIC AND MUSCLE RELAXANT ACTIVITY OF THE ETHANOLIC EXTRACT OF THE LEAVES OF MIRABILIS JALAPA

2017 ◽  
pp. 81-84
Author(s):  
Deepsikha Bharali ◽  
Dipankar Saha
Keyword(s):  
Muscle Relaxant ◽  
Diclofenac Sodium ◽  
Ethanolic Extract ◽  
Dependent Manner ◽  
Phytochemical Screening ◽  
Standard Drug ◽  
Standard Procedures ◽  
Mirabilis Jalapa ◽  
Muscle Relaxant Activity ◽  
Dose Dependent

Objective: The aim and objectives of the present work is to determine pharmacological activity upon ethnopharmacological survey. The present study deals with phytochemical screening and analgesic as well as muscle relaxant activity of leaves of Mirabilis jalapa.Methods: The present study is aimed at phytochemical screening and evaluating the analgesic and muscle relaxant activities of ethanolic leaf extract of Mirabilis jalapa by using hot plate method and rota rod method respectively [1, 2]. The Phytochemical screening of the extract was done according to the standard procedures to reveal the presence of the active constituents like Alkaloids, flavonoids, phenols, glycosides, tannins, saponins, steroids, carbohydrates etc [3-5].Results: The analgesic and muscle relaxant activity study were dose dependent. The EEMJ extracts (100 mg/kg, 200 mg/kg, 500 mg/kg) and the standard drug Diclofenac sodium (25 mg/kg) shows significant increase in the reaction time when compared with control at 30 min, 60 min, 90 min and 120 min and the effect of standard was found to be highest during the study. Another study was designed to evaluate the skeletal muscle relaxant properties of ethanolic extract of leaves of Mirabilis jalapa. Linn by taking the EEMJ extracts (100 mg/kg, 200 mg/kg, 500 mg/kg) and standard drug Lorzepam (10 mg/kg). Both the extracts and standard drug show decrease in the fall of time in a dose dependent manner when compared with control at 15 min, 30 min, 45 min respectively. Conclusion: Therefore, from the above study it is revealed that Mirabilis jalapa showing better pharmacological activities (Analgesic and Muscle relaxant) in dose dependent manner.

scholarly journals Comparative Evaluation of Analgesic, Anti-inflammatory and Antipyretic Effects of Synthetic Derivatives of Organoantimony (?) Ferocenyl Benzoate with Piroxicam

2016 ◽  
Vol 19 (1) ◽  
pp. 15-24
Author(s):  
Muhammad Shoaib Akhtar ◽  
Zulfiqar Khan ◽  
Muhammad Naveed Mushtaq ◽  
Muhammad Salman Akhtar
Keyword(s):  
Pharmaceutical Journal ◽  
Significant Inhibition ◽  
Diffusion Method ◽  
Dependent Manner ◽  
Standard Drug ◽  
Compound A ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Synthetic Derivatives ◽  
Dose Dependent

The current study was planned to evaluate comparative anti-inflammatory, analgesic and anti-pyretic activities of two newly synthesized organo-antimony (v) ferrocenyl benzoate derivatives with piroxicam. Anti-microbial activity of these compounds was also screened against two microorganisms. Analgesic effect of test compounds was evaluated by formalin-induced paw licking test in mice. The test compounds at 50 and 100 mg/kg b.w. doses exhibited significant (p<0.001) reduction of paw licking in treated mice comparable with standard drug piroxicam. Anti-inflammatory activity was assessed against carrageenan-induced paw oedema. The compound A produced anti-inflammatory effects comparable with standard piroxicam in dose dependent manner whereas compound B showed better effects than piroxicam at dose of 100 mg/kg body weight. To investigate anti-pyretic activity, fever was induced by administration of Brewer’s yeast in mice. Compound A showed highly significant inhibition of pyrexia (p<0.001) comparable to piroxicam after 3 hours while compound B (50 and 100 mg/kg) produced relatively lower anti-pyretic effect than standard drug. Antibacterial activity determined by disc diffusion method showed that compound B was relatively more effective than compound A against Staphylococcus aureus and Klebsiella pneumoniae. It is conceivable that both the tested compounds possessed anti-inflammatory, analgesic, anti-pyretic and anti-microbial effects even after the structural modification of parent compound.Bangladesh Pharmaceutical Journal 19(1): 15-24, 2016

scholarly journals Evaluation of analgesic, neuropharmacological and cytotoxic activity of Trigonella foenum-graecum Linn.

1970 ◽  
Vol 1 (1) ◽  
pp. 6-11
Author(s):  
Moli Akter ◽  
Mirola Afroze ◽  
Ambia Khatun
Keyword(s):  
Acetic Acid ◽  
Brine Shrimp ◽  
Dependent Manner ◽  
Immersion Method ◽  
Standard Drug ◽  
Writhing Test ◽  
Trigonella Foenum Graecum ◽  
Vincristine Sulphate ◽  
Tail Immersion ◽  
Dose Dependent

The present study was carried out to investigate the possible analgesic, neuropharmacological and cytotoxic activities of the methanolic extract of Trigonella foenum-graecum Linn. leaves. The analgesic and neuropharmacological activities of Trigonella foenum-graecum Linn. were investigated at the doses of 100mg/kg, 200mg/kg and 400mg/kg of body weight in mice. Analgesic potential of the extract was evaluated for centrally acting analgesic property using tail immersion method and peripheral analgesic actions using acetic acid-induced writhing test. In acetic acid-induced writhing test, extract produced a significant (p < 0.001) inhibition of writhing response in a dose dependent manner but maximum inhibition (93.46%) of writhing was found at 400mg/kg dose. In tail immersion method, extract caused a significant (p < 0.001) increase in latency time and the results were comparable to the standard drug Diclofenac- Sodium. In addition, neuropharmacological property of crude extract was carried out by Hole cross and Open field test. The extract significantly (p < 0.05-0.001) displayed a dose dependent suppression of motor activity, exploratory behaviour. Furthermore, the extract was subjected to Brine Shrimp lethality bioassay for primary evaluation of cytotoxicity, where the extract was found to be highly toxic to Brine Shrimp nauplii, having LC50 values of 10μg/ml while the LC50 of the reference anticancer drug vincristine sulphate was 0.66μg/ml. The results of this present study suggest that the extract possesses analgesic, cytotoxic and CNS depressant activities. Key Words: Trigonella foenum-graecum Linn.; cytotoxicity; neuropharmacological; analgesic activity. DOI: http://dx.doi.org/10.3329/icpj.v1i1.9218 International Current Pharmaceutical Journal 2011, 1(1): 6-11

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