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

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.

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Phytochemical and pharmacological evaluation of Tragia cannabina for anti-inflammatory activity

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i8.10857 ◽

2012 ◽

Vol 1 (8) ◽

pp. 213 ◽

Cited By ~ 1

Author(s):

Raju Venkategowda Hosahally ◽

Ganapaty Seru ◽

Prasanna Shankarrao Sutar ◽

Vijaya Gopalachar Joshi ◽

Kishori Prasanna Sutar ◽

...

Keyword(s):

Body Weight ◽

Methanolic Extract ◽

Pharmaceutical Journal ◽

Inflammatory Activity ◽

Reference Standard ◽

Paw Edema ◽

Pharmacological Evaluation ◽

Whole Plant ◽

Soxhlet Apparatus ◽

Anti Inflammatory

The present study investigates the anti-inflammatory activity of methanolic and chloroform extracts of Tragia cannabina. The whole plant of Tragia cannabina was extracted with methanol and chloroform by using soxhlet apparatus. The effect of both extracts of Tragia cannabina was studied on carrageenan induced paw edema. The methanolic extract decreased the edema induced in hind paw. The percentage inhibition of paw edema was maximum with methanolic and chloroform extracts of Tragia cannabina at 300mg/kg body weight and has showed significant anti-inflammatory activity. It has been concluded that both the methanolic and chloroform extracts of Tragia cannabina showed significant anti-inflammatory activity comparable to that of reference standard Ibuprofen.DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.10857">http://dx.doi.org/10.3329/icpj.v1i8.10857</a> International Current Pharmaceutical Journal 2012, 1(8): 213-216

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Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: Synthesis and their biological evaluation

Journal of the Serbian Chemical Society ◽

10.2298/jsc101104092g ◽

2011 ◽

Vol 76 (8) ◽

pp. 1057-1067 ◽

Cited By ~ 6

Author(s):

Sadaf Gilani ◽

Suroor Khan ◽

Ozair Alam ◽

Vijender Singh ◽

Alka Arora

Keyword(s):

Lipid Peroxidation ◽

Acid Hydrazide ◽

Inflammatory Activity ◽

Paw Edema ◽

Rat Paw Edema ◽

Anti Inflammatory ◽

Rat Paw ◽

New Compounds ◽

Derivatives Of ◽

Ulcerogenic Action

A series of thiazolidin-4-one (2a-h, 3a-h), azetidin-2-one (4a- h) and 1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new compounds, out of 32, showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from the results that their protective effects may be related to inhibition of lipid peroxidation in the gastric mucosa.

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In Vivo Evaluation of Anti-inflammatory Activity of 2-[3-Acetyl- 5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanylbutyric Acid

Folia Medica ◽

10.1515/folmed-2017-0095 ◽

2018 ◽

Vol 60 (2) ◽

pp. 270-274

Author(s):

Hristina Zlatanova ◽

Stanislava Vladimirova ◽

Ilia Kostadinov ◽

Atanas T. Bijev

Keyword(s):

Chronic Inflammation ◽

Butyric Acid ◽

Inflammatory Activity ◽

Control Group ◽

Paw Edema ◽

In Vivo Evaluation ◽

Continuous Administration ◽

Inflammation Model ◽

Anti Inflammatory ◽

Acid Compound

Abstract Background: Persisting inflammatory stimuli cause chronic inflammation recognized as the major factor contributing to the development of a number of diseases. One group of drugs used in the treatment of chronic inflammation is the group of non-steroidal anti-inflammatory drugs and, more specifically, the selective COX-2 inhibitors (coxibs). However, most of the coxibs were withdrawn from the market in view of their safety profile. In the present study, 2-[3-Acetyl-5-(4-chlorophenyl)- 2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e), an Npyrrolylcarboxylic acid derivative structurally related to celecoxib, is evaluated for anti-inflammatory activity after single and multiple (14 days) administration using an animal inflammation model. Aim: To evaluate the anti-inflammatory properties of 2-[3-Acetyl-5-(4-chlorophenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e) after single and multiple (14 days) administration using an animal inflammation model. Materials and methods: Forty Wistar rats were allocated into 5 groups (n=8) treated with saline (controls), diclofenac (25 mg/kg b.w.), compound 3e (10, 20 and 40 mg/kg b.w.) intraperitoneally. The volume of the right hind paw of the animals of all groups is measured prior to treatment and two, three and four hours after administration of carrageenan using a plethysmometer (Ugo Basile, Italy). The percentage of paw edema is calculated using the Trinus formula. Results: In a single administration, compound 3e in doses of 10 and 20 mg/kg b.w. did not inhibit paw edema, while a dose of 40 mg/kg b.w. significantly inhibited carrageenan-induced paw edema at 2 hours in comparison with the control group. After continuous administration, compound 3e in doses of 10, 20 and 40 mg/kg b.w. significantly reduced paw edema at 2, 3, and 4 hours compared to animals treated with saline. Conclusions: Compound 3e shows anti-inflammatory properties similar to those of diclofenac after continuous administration.

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

E-Journal of Chemistry ◽

10.1155/2012/278695 ◽

2012 ◽

Vol 9 (4) ◽

pp. 2510-2515 ◽

Cited By ~ 1

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).

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

E-Journal of Chemistry ◽

10.1155/2009/645131 ◽

2009 ◽

Vol 6 (2) ◽

pp. 495-503 ◽

Cited By ~ 3

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.

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Anti-inflammatory properties of some novel thiazolo[4,5-b]pyridin-2-ones

Pharmacia ◽

10.3897/pharmacia.67.e38969 ◽

2020 ◽

Vol 67 (3) ◽

pp. 121-127

Author(s):

Taras Chaban ◽

Vasyl Matiychuk ◽

Olexandra Komarytsya ◽

Iryna Myrko ◽

Ihor Chaban ◽

...

Keyword(s):

Nmr Spectroscopy ◽

Elemental Analysis ◽

Paw Edema ◽

H Nmr ◽

Rat Paw Edema ◽

Anti Inflammatory ◽

Alkylation Reactions ◽

Rat Paw ◽

Inflammatory Action

Synthesis of novel N3 and C5 substituted thiazolo[4,5-b]pyridin-2-ones was carried out on the basis of [3+3]-cyclocodensation, acylation and alkylation reactions. The structures of the obtained compounds were confirmed by 1H NMR spectroscopy, and elemental analysis. The anti-inflammatory action of novel thiazolo[4,5-b]pyridine-2-one derivatives was evaluated in vivo employing the carrageenan-induced rat paw edema method. When compared with Ibuprofen, some our compounds were found to be more potent. Graphical abstract

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Phytochemical and pharmacological evaluation of Tragia cannabina for anti-inflammatory activity

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i8.11253 ◽

2012 ◽

Vol 1 (8) ◽

pp. 213-216 ◽

Cited By ~ 1

Author(s):

Raju Venkategowda Hosahally ◽

Ganapaty Seru ◽

Prasanna Shankarrao Sutar ◽

Vijaya Gopalachar Joshi ◽

Kishori Prasanna Sutar ◽

...

Keyword(s):

Body Weight ◽

Methanolic Extract ◽

Pharmaceutical Journal ◽

Inflammatory Activity ◽

Reference Standard ◽

Paw Edema ◽

Pharmacological Evaluation ◽

Whole Plant ◽

Soxhlet Apparatus ◽

Anti Inflammatory

The present study investigates the anti-inflammatory activity of methanolic and chloroform extracts of Tragia cannabina. The whole plant of Tragia cannabina was extracted with methanol and chloroform by using soxhlet apparatus. The effect of both extracts of Tragia cannabina was studied on carrageenan induced paw edema. The methanolic extract decreased the edema induced in hind paw. The percentage inhibition of paw edema was maximum with methanolic and chloroform extracts of Tragia cannabina at 300mg/kg body weight and has showed significant anti-inflammatory activity. It has been concluded that both the methanolic and chloroform extracts of Tragia cannabina showed significant anti-inflammatory activity comparable to that of reference standard Ibuprofen.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11253 International Current Pharmaceutical Journal 2012, 1(8): 213-216

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

Current Topics in Medicinal Chemistry ◽

10.2174/1568026621999201214232458 ◽

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.

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ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽

10.53879/id.58.01.11950 ◽

2021 ◽

Vol 58 (01) ◽

pp. 41-46

Author(s):

Deeksha Singh ◽

◽

Amit Nayak ◽

Rakesh Yadav ◽

Uttam Singh Baghel ◽

...

Keyword(s):

Phenolic Compounds ◽

Stem Bark ◽

Inflammatory Activity ◽

Antiulcer Activity ◽

Paw Edema ◽

Ulcer Index ◽

Pylorus Ligation ◽

Anti Inflammatory ◽

Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

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