Reaction of 4-aroyl-2(3H)-dihydrofuranones with hydroxylamine hydrochloride. Synthesis and pharmacological study of a series of 3-aryl-4,5-dihydro-4-isoxazoleacetic acids

1991 ◽  
Vol 56 (11) ◽  
pp. 2494-2499 ◽  
Author(s):  
Maria M. Curzu ◽  
Gérard A. Pinna ◽  
Giorgio Cignarella ◽  
Daniela Barlocco ◽  
Maria Piera Demontis
Keyword(s):  
Wistar Rats ◽  
Antiinflammatory Activity ◽  
Pharmacological Study ◽  
Hydroxylamine Hydrochloride ◽  
Reference Drug ◽  
Phenyl Derivative ◽  
Interesting Compound ◽  
Carrageenin Edema

We have synthesized and tested for their antiinflammatory activity a new series of 3-aryl-4,5-dihydro-4-isoxazoleacetic acids (IVa-IVg). Preliminary pharmacological results seem to indicate the 3-phenyl derivative IVa as the most interesting compound. In fact, when tested against carrageenin edema in Wistar rats, it shows antiinflammatory activity comparable to that of naproxene, taken as reference drug, though of shorter duration. All the substituted phenyl derivatives were less active (IVd-IVf) or inactive (IVb, IVc, IVg).

scholarly journals Histopathological Studies on the Effects of Chloroform and Methanolic Extracts of Ilex kudingcha in Trypanosoma brucei Infected Albino Wistar Rats

2018 ◽  
Vol 04 ◽  
pp. 50
Author(s):  
Olajoju. T. Soniran ◽  
Kalu. K. Ngele ◽  
Christopher. O. Alisa ◽  
Damilola. A. Omoboyowa ◽  
Nnabude. H. Agu ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Wistar Rats ◽  
Methanolic Extract ◽  
Phytochemical Analysis ◽  
Diminazene Aceturate ◽  
Leaf Extracts ◽  
Standard Drug ◽  
Phytochemical Study ◽  
Reference Drug ◽  
Histopathological Studies

Histopathological studies of the effects of chloroform and methanolic leaf extracts of Ilex kudingcha in Trypanosoma brucei infected albino wistar rats were investigated. The toxicity and phytochemical study were also carried out using standard protocol. T. brucei infected animals were administered orally with 200 and 400 mg/kg b.w. of the extracts and 3.5 mg/kg b.w. of the standard drug (diminazene aceturate). Results on acute toxicity studies (LD50) revealed no sign of lethality up to the dose of 5,000 mg/kg body weight but the liver and kidney histology of infected animals treated with 5,000 mg/kg b.w. of I. kudingcha extracts were observed to be hepatotoxic and nephrotoxic. The methanol extracts showed appreciably high in vivo anti-trypanosomal activities compared to the reference drug. Histological examination of the organs revealed serious pathological lesions in the liver of the infected animals without treatment (negative control). In the positive control animals (infected animals administered standard drug), mild multifocal aggregate of inflammatory leucocytes was observed. In the other experimental animals, no pathological lesion was observed in the liver, kidney, brain, and heart of infected animals treated with the methanolic extract and combined methanol and chloroform extracts. The effectiveness of the methanolic extract at reducing the lesions caused by the parasite is the same compared with the standard drug. Phytochemical analysis of the plant extracts showed that methanol extract contained appreciable high levels of alkaloids, saponin, tannins, phenol, and glycoside while flavonoid was not detected. Hence, the curative properties of methanolic extract of I. kudingcha as observed in the organs indicate its anti-trypanosomal properties but it should be consumed at minimal doses.

scholarly journals The Hypoglycaemic, Antihyperlipidemic and Antioxidative Effects of Anacardium Occidentale Methanolic Nut Extract in Streptozotocin-Induced Diabetic Male Wistar Rats

2021 ◽  
Author(s):  
Folasade O. AJAO ◽  
Michael A. Olamoyegun ◽  
Marcus O. Iyedupe
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Wistar Rats ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Anacardium Occidentale ◽  
Low Density ◽  
Reference Drug ◽  
Antioxidative Effects ◽  
Group 2

Abstract Background: This research work investigated the antidiabetic, anti-hyperlipidemic, and antioxidative effects of Anacardium occidentale methanolic nut extract in Streptozotocin (STZ)-induced diabetic Wistar rats. Methods: Forty (40) Wistar rats weighing 250±30g were randomly divided into five groups of 8 rats each. Group 1 served as the control; Group 2-5 were induced with diabetes with a single dose of 50mg/kg bw of streptozotocin intraperitoneally. After diabetes induction, Group 2 served as the STZ-only group, Groups 3 and 4 were administered 100mg/kg bw and 200mg/kg bw p.o Anacardium occidentale nut extract, respectively, while Group 5 was administered 2mg/kg bw of glimepiride as a reference drug for a period of 4 weeks. Food and water intake were monitored daily, body weight, and blood glucose levels weekly throughout the experiment. On day 29, the animals were sacrificed, and blood samples were collected through cardiac puncture for biochemical studies. Results: Administration of the nut extract significantly (p<0.05) increased the food intake and body weight of diabetic treated rats, fasting blood glucose level and oral glucose tolerance test (OGTT) decreased significantly (p<0.05) in treated rats. On lipid profile, administration of nut extract significantly decreased (p<0.05) triglyceride, low-density lipoprotein, total cholesterol, and very-low-density lipoprotein concentrations while it significantly increases (p<0.05) the high-density lipoprotein. Anacardium occidentale nut extract caused significantly (p<0.05) increases in SOD, GPx, GSH, and CAT levels with a decrease MDA level in diabetic treated rats. Markers of liver and kidney functions were also improved in diabetic treated rats.Conclusion: Treatment with Anacardium occidentale methanolic nut extract has hypoglycemic, hypolipidemic, and hepato-protective effects in diabetic rats. It also alleviates oxidative stress activity and restoration of markers of kidney function, and may be useful as alternative therapy in the management of diabetes and its related complications.

scholarly journals Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain

1999 ◽  
Vol 57 (4) ◽  
pp. 916-920 ◽  
Author(s):  
NILZA D. ALVES ◽  
CARLOS M. DE CASTRO-COSTA ◽  
ALBA M. DE CARVALHO ◽  
FRANKLIN J. C. SANTOS ◽  
DELANO G. SILVEIRA
Keyword(s):  
Neuropathic Pain ◽  
Analgesic Effect ◽  
Wistar Rats ◽  
Pharmacological Study ◽  
Thermal Stimulus ◽  
Chronic Neuropathic Pain ◽  
Pain Symptoms ◽  
The Right ◽  
Dose Dependent ◽  
Thermal Stimuli

Since anticonvulsants have been used for treating neuralgias, an interest has arisen to experimentally test vigabatrin for its gabaergic mechanism of action. For this, 41 Wistar rats were used, and in 25 of them a constrictive sciatic neuropathy was induced (Bennet & Xie model). For testing pain symptoms, spontaneous (scratching) and evoked behaviors to noxious (46o C) and non-noxious (40o C) thermal stimuli were quantified. Moreover, a comparative pharmacological study of vigabatrin with other analgesic anticonvulsant drugs was also performed. The results showed a possible dose-dependent analgesic effect of vigabatrin (gamma-vinyl-GABA) on experimental neuropathic pain, as shown by the significant (p<0.05) decreasing effect of vigabatrin on scratching and by its significant (p<0.05) increasing effect on the latency of the right hindpaw withdrawal of the animals to noxious thermal stimulus. This was corroborated by similar findings with analgesic anticonvulsants (carbamazepine, phenytoin and valproic acid). This possible and not yet described analgesic effect of vigabatrin seems not to be opioid mediated.

scholarly journals Synthesis, antimicrobial and anti-cancer activities of some new N-ethyl, N-benzyl and N-benzoyl-3-indolyl heterocycles

2012 ◽  
Vol 62 (2) ◽  
pp. 157-179 ◽  
Author(s):  
Eslam El-Sawy ◽  
Adel Mandour ◽  
Khaled Mahmoud ◽  
Inas Islam ◽  
Heba Abo-Salem
Keyword(s):  
Hydrazine Hydrate ◽  
Hydroxylamine Hydrochloride ◽  
Reference Drug ◽  
Highly Active ◽  
Anti Cancer ◽  
Hct 116 ◽  
New Compounds ◽  
Substituted 1 ◽  
Isoxazole Derivatives

Synthesis, antimicrobial and anti-cancer activities of some newN-ethyl,N-benzyl andN-benzoyl-3-indolyl heterocyclesA series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2-ene-1-ones (2a, b-4a, b) were prepared and allowed to react with urea, thiourea or guanidine to give pyrimidine derivatives5a, b-13a, b. Reaction of2a, b-4a, bwith ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives14a, b-16a, b. Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives17a, b-19a, b. On the other hand, reaction of2a, b-4a, bwith some hydrazine derivatives, namely hydrazine hydrate, acetyl hydrazine, phenylhydrazine and benzylhydrazine hydrochloride, led to the formation of pyrazole derivatives20a, b-31a, b. Moreover, reaction of2a, b-4a, bwith hydroxylamine hydrochloride gave isoxazole derivatives32a, b-34a, b. The newly synthesized compounds were tested for their antimicrobial activity and showed that 4-(N-ethyl-1H-indol-3-yl)-6-(p-chlorophenyl)-pyrimidine-2-amine (11b) was the most active of all the test compounds towardsCandida albicanscompared to the reference drug cycloheximide. Eighteen new compounds, namely pyrimidin-2(1H)-ones5a, b-7a, b, pyrimidin-2(1H)-thiones8a, b-10a, band pyrimidin-2-amines11a, b-13a, bderivatives, were tested for theirin vitroantiproliferative activity against HEPG2, MCF7 and HCT-116 cancer cell lines. 4-(N-ethyl-1H-indol-3-yl)-6-(p-methoxyphenyl)-pyrimidin-2-amine (11a)was found to be highly active withIC50of 0.7 μmol L-1.

scholarly journals HYPOGLYCEMIC EFFECT OF ANDROGRAPHIS ECHIOIDES ON STREPTOZOTOCIN INDUCED EXPERIMENTAL RATS

2015 ◽  
Vol 7 ◽  
pp. 55
Author(s):  
Mani Rupeshkumar ◽  
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Wistar Rats ◽  
Methanol Extract ◽  
Fasting Blood Glucose ◽  
Hypoglycemic Effect ◽  
Reference Drug ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
Single Intraperitoneal Injection

The present study aims to study the hypoglycemic effect of methanol extract of Andrographisechioides (MEAE) in streptozotocin (STZ)-induced diabetic Wistar rats. Hyperglycemia was induced in rats by single intraperitoneal injection of STZ (55 mg/kg bodyweight). Three days after STZ induction, the hyperglycemic rats were treated with MEAE orally at the doses of 200, 500, and 800 mg/kg body weight daily for 21 days. Glibenclamide (1 mg/kg, orally) was used as reference drug. The fasting blood glucose levels were measured on each 7th day during the 21 days of treatment.

scholarly journals Antiinflammatory activity of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates on carrageenan model of inflammation

2019 ◽  
pp. 82-87
Author(s):  
B. V. Pristupa ◽  
I. O. Shyshkin ◽  
Ya. V. Rozhkovsky ◽  
V. O. Gelmboldt
Keyword(s):  
Antiinflammatory Activity ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Male Rats ◽  
Control Group ◽  
Paw Edema ◽  
Commercial Preparation ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Inflammatory Effect

In the last decade, high cariesprophylactic efficacy of ammonium hexafluorosilicates, including salts with substituted biologically active ammonium cations, has been demonstrated. Among the promising anti-caries agents are recently synthesized 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates, for whose cations anti-inflammatory activity is expected. The aim of the work is to assess the presence of anti-inflammatory activity in the series of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates in the experiment. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed technique, carrageenan is a commercial preparation, reference drug is a indomethacin. Experiments on the anti-inflammatory activity of hexafluorosilicates were performed on 77 white Wistar male rats weighing 174–190 g using the carrageenan model of inflammation. The inflammatory reaction was reproduced by subplantary administration of 0.1 ml of a 0.2% solution of carrageenan, the studied compounds were administered orally in doses 1/10, 1/20, 1/50 from LD50 for the compound III. It was established that after administration of carrageenan, animals of the control group showed marked paw edema, which gradually increased and was maximal after 24 hours of observation. According to the data obtained, the indices for compounds I-III practically do not differ from those of the control group. This indicates that, despite the results of the PASS forecast and the presence of acetic acid residue, an anti-inflammatory pharmacofor, in compounds I-III, the compounds under study do not have an anti-inflammatory effect in the carrageenan model. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates do not show the expected anti-inflammatory activity in the carrageenan model of inflammation.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

scholarly journals Synthesis, Analgesic and Antimicrobial Activities of Some Novel Isoxazole Derivatives

1970 ◽  
Vol 7 (2) ◽  
pp. 113-118 ◽  
Author(s):  
SK Sahu ◽  
M Banerjee ◽  
D Sahu ◽  
CC Behera ◽  
GC Pradhan ◽  
...  
Keyword(s):  
Hydroxylamine Hydrochloride ◽  
Analysis Data ◽  
Antimicrobial Activities ◽  
Elemental Analysis Data ◽  
Antibacterial And Antifungal Activity ◽  
Reference Drug ◽  
Microbial Screening ◽  
Antibacterial And Antifungal ◽  
Isoxazole Derivatives

Substituted aryl-N-chalconyl aminophenols 1a-f were synthesized by base catalysed condensation of equimolar mixture of N-(4-hydroxyphenyl)-acetamide and appropriate araldehydes. Treatment of compounds 1a-f with hydroxylamine hydrochloride in ethanol afforded a series of novel 4-(5′-substituted-aryl-4′,5′-dihydro-isoxazole-3′-yl-amino) phenols have been synthesized by treating substituted aryl-N-chalconyl aminophenol with hydroxylamine hydrochloride. Structures of newly synthesized compounds 2a-f were confirmed by IR, 1H-NMR and elemental analysis data. The synthesized compounds were investigated for their analgesic and antimicrobial activities. Compounds 2e and 2f exhibited significant analgesic activity in comparison to the reference drug paracetamol. In in vitro anti-microbial screening, compounds 2c and 2f showed higher antibacterial and antifungal activity in comparison to the reference standard ciprofloxacin and clotrimazole, respectively. Compound 2f bearing 4-Cl phenyl substitution at 5 position of Ioxazoline ring was found to be the most potent compound of the series. Key words: Isoxazole, Analgesic, Antibacterial activity. doi: 10.3329/dujps.v7i2.2165 Dhaka Univ. J. Pharm. Sci. 7(2): 113-118, 2008 (December)

scholarly journals EFFECT OF LYOPHILIZED JUICE OF PUNICA GRANATUM L. IN ANTINOCICEPTIVE AND INFLAMMATORY PAIN

2021 ◽  
pp. 17-19
Author(s):  
JOSE ANTONIO GUERRERO-SOLANO ◽  
MIRANDELI BAUTISTA ◽  
NELLY DEL SOCORRO CRUZ-CANSINO ◽  
ALEJANDRO CHEHUE-ROMERO ◽  
OSMAR ANTONIO JARAMILLO-MORALES
Keyword(s):  
Body Weight ◽  
Acetylsalicylic Acid ◽  
Inflammatory Pain ◽  
Wistar Rats ◽  
Formalin Test ◽  
Antinociceptive Effect ◽  
Punica Granatum ◽  
Reference Drug ◽  
Male Wistar Rats ◽  
Punica Granatum L

Objective: The aim of this study was to explore the analgesic activity of lyophilized juice of Punica granatum L., obtained from Hidalgo, Mexico, in theformalin test.Methods: We extracted the juice manually, filtered it and then dried down in a lyophilizer machine. We evaluated the antinociceptive effect oflyophilized juice from pomegranate in the formalin test (2%) in male Wistar rats (180–200 g body weight). Thirty minutes before the test, a dose of316 mg/kg (lyophilized juice) and acetylsalicylic acid as reference drug (100 mg/kg) both were administered intragastrically (i.g.).Results: The oral administration of lyophilized juice of pomegranate showed a significant decrease in the number of flinches in the temporal courseand a significant antinociceptive effect in nociceptive and inflammatory pain compared with the vehicle. In the same way, this effect appeared with thedrug of reference (acetylsalicylic acid 100 mg/kg i.g). Furthermore, it was shown that juice had a 34% of antinociception on overall effect versus vehicle.Conclusion: The results suggest that lyophilized juice of pomegranate has antinociceptive effect in nociceptive and inflammatory pain. Therefore, thisstudy supports the possible use of this lyophilized juice of pomegranate in the treatment of pain.

scholarly journals Evaluation of the curative role, Anti-inflammatory and anti-oxidative activity of some dietary spices on carrageenan induced paw edema in albino Wistar rats

2020 ◽  
Vol 10 (5-s) ◽  
pp. 90-96
Author(s):  
Khaoula Bouaoud ◽  
Noreddine Menadi ◽  
Mohammed Zairi ◽  
Sofiane Bouazza ◽  
Hadjer Bekhadda ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Wistar Rats ◽  
Red Pepper ◽  
Total Phenolic ◽  
Control Group ◽  
Paw Edema ◽  
Standard Drug ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Dietary Spices

Background: Inflammation is a major burning problem worldwide and billions of individuals are affected. Some of the spices used daily in Algerian cuisine have been known to possess major anti-inflammatory effects. Turmeric, red pepper, ginger, cinnamon and cumin  etc. are a few of the wide spectrum of spices used in Algeria. The aim of the study was to investigate the antiinflammatory effect  and anti actvity of some dietary spices in carrageenan induced models of inflammation on Wistar  rats. Methods: Albino wistar rats were divided into four groups. Inflammation was induced on the animal by injecting the right hand paw with carrageenan (0.1 ml of 1%). Group 1  was fed with food and water and  treated with carrageenan (control) whereas group 2 and  3 treated with different doses (100 and 200 mg/kg/bw) of aqueous extract of some dietary spices with carrageenan, respectively. Group 4  treated with standard drug diclofenac sodium (10 mg/kg b.w., reference drug for inflammation), once for 24 hrs. Results: The content of total phenolic was 137.2±21.6 mg/g and flavonoids 122.3±5.8 mg/g. After 60, 120, 180, 240 and 300 min, the data indicate that  some dietary spices 100 and 200 mg/kg was significantly effective reducing paw edema volumes induced by carrageenan compared to control (p <0.01). The levels of serum pro-inflammatory white blood cells, neutrophile, lymphocyte, monocyte,  eosinophile, total protein and protein c reactive and total cephalin KADIN  and platelts in the control group were significantly increased by carrageenan injection compared with the normal group. The rats pretreated with some spices 100 and 200 mg/kg had significantly lower levels of pro-inflammatory to compare control group. The paw edema in carrageenan-induced rats was considerably reduced by treating with 100 and 200  mg/kg aqueous extract of some dietary spices when compared to the untreated  rats (p<0.001). Conclusion : The present results clearly demonstarted that carrageenan significantly increased paw edema whereas some dietary treated rats significantly decreased the paw edema. The study underlines the importance of some of the frequently used spices (Turmeric, red pepper, ginger, cinnamon and cumin)  in the treatment of inflammation.

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