Evaluation of the Analgesic and Anti-inflammatory Activities of Some Thiazolo[4,5-d]pyrimidines

Balkan, Ayla; Gören, Zafer; Urgun, Hüsne; Calis, Uensal; Çakar, Ayşe Nur; Atilla, Pergin; Uzbay, Tayfun

doi:10.1055/s-0031-1299915

Cited by 7 publications

(7 citation statements)

References 6 publications

(6 reference statements)

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“…Mounting of the specimen was done by using Distrene Phthalate Xylene (D.P.X.) and examined under microscope for photomicrographic analysis [75]. …”

Section: Methodsmentioning

confidence: 99%

Ameliorative Effects of a Polyphenolic Fraction of Cinnamomum zeylanicum L. bark in Animal Models of Inflammation and Arthritis

Rathi

2013

Sci. Pharm.

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Cinnamon bark (Cinnamomum zeylanicum Syn C. verum, family: Lauraceae) is one of the oldest traditional medicines for inflammatory- and pain-related disorders. The objective of the present study was to evaluate the efficacy of the polyphenol fraction from Cinnamomum zeylanicum bark (CPP) in animal models of inflammation and rheumatoid arthritis. Dose-response studies of CPP (50, 100, and 200 mg/kg) used in a separate set of in vivo experiments were conducted in acute (carrageenan-induced rat paw edema), subacute (cotton pellet-induced granuloma), and sub-chronic (AIA, adjuvant-induced established polyarthrtis) models of inflammation in rats and the acetic acid-induced writhing model of pain in mice. Effects of CPP on cytokine (IL-2, IL-4, and IFNγ) release from Concanavalin (ConA)-stimulated lymphocytes were also evaluated in vitro. CPP showed a strong and dose-dependent reduction in paw volume, weight loss reversal effects against carrageenan-induced paw edema, and cotton pellet-induced granuloma models in rats. CPP (200 mg/kg p.o. for 10 days) showed a significant reduction in elevated serum TNF-α concentration without causing gastric ulcerogenicity in the AIA model in rats. CPP also demonstrated mild analgesic effects during acute treatment as evidenced by the reduction in the writhing and paw withdrawal threshold of the inflamed rat paw during the acetic acid-induced writhing model and Randall-Selitto test. CPP was found to inhibit cytokine (IL-2, IL-4, and IFNγ) release from ConA-stimulated lymphocytes in vitro. In conclusion, CPP demonstrated prominent action in animal models of inflammation and arthritis and therefore can be considered as a potential anti-rheumatic agent with disease-modifying action.

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“…Mounting of the specimen was done by using Distrene Phthalate Xylene (D.P.X.) and examined under microscope for photomicrographic analysis [75]. …”

Section: Methodsmentioning

confidence: 99%

Ameliorative Effects of a Polyphenolic Fraction of Cinnamomum zeylanicum L. bark in Animal Models of Inflammation and Arthritis

Rathi

2013

Sci. Pharm.

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“…For the biological activity of thiazolo[4,5-d]pyrimidine derivatives, see: Balkan et al (2002); Bekhit et al (2003); Danel et al (1998); Fahmy et al (2003). For the synthesis of thiazolo [4,5-d]pyrimidines via tandem aza-Wittig and cyclization reactions of iminophosphorane and alkylamines, see: Liang et al (2007).…”

Section: Related Literaturementioning

confidence: 99%

6-(4-Fluorophenethyl)-7-imino-3-phenyl-2,3,6,7-tetrahydro-1,3-thiazolo[4,5-d]pyrimidine-2-thione

Liang

Yang

2009

Acta Cryst E

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“…The [4,5-d] isomer of thiazolopyrimidines can be considered as 7-thio analogues of guanine and adenine due to replacement of a nitrogen by a sulfur atom at position 7 of the purine ring. Thiazolo [4,5-d]pyrimidines were reported to possess a broad range of biological activitities, including anticancer [1,2,3], antibacterial [4,5,6], analgesic [7,8], antidepressant [9], and antiviral (human cytomegalovirus) [10] properties. In view of these facts, the aim of this study was to design and syn-thesize new derivatives of 3-phenylthiazolo [4,5-d]pyrimidine-2-thiones in the hope that the new compounds might show significant antitumor activity, may be more potent, possessing selective efficacy and lower toxicity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antitumor Screening of Novel 3-Phenylthiazolo [4,5-d]pyrimidin-2-thione Derivatives

Becan

Wagner

2011

Arzneimittelforschung

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A series of new derivatives of 3-phenylthiazolo[4,5-d]pyrimidine-2-thiones were synthesized by the cyclization of 4-amino-5-alkyl(aryl) carboxamido-2,3-dihydrothiazolo-2-thione with aromatic aldehydes. Amine moieties were substituted in position 7 of the obtained bicyclic compounds. The synthesized compounds were characterized by elemental analysis, IR, 1H-NMR, and 13C-NMR spectral data. Some of the newly synthesized compounds were selected by the U.S. National Cancer Institute for in vitro antitumor screening. The two compounds 3d 7-chloro-5-(4-fluorophenyl)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-d]pyrinimidine-2-thione and 4i 5-(2-chlorophenyl)-7-(4-fluorobenzylaxnlno)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-dipyrhflldlfle-2thione proved to be the most active in the present study and their antitumor activities against 60 human tumor cell lines were described.

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Evaluation of the Analgesic and Anti-inflammatory Activities of Some Thiazolo[4,5-d]pyrimidines

Cited by 7 publications

References 6 publications

Ameliorative Effects of a Polyphenolic Fraction of Cinnamomum zeylanicum L. bark in Animal Models of Inflammation and Arthritis

Ameliorative Effects of a Polyphenolic Fraction of Cinnamomum zeylanicum L. bark in Animal Models of Inflammation and Arthritis

6-(4-Fluorophenethyl)-7-imino-3-phenyl-2,3,6,7-tetrahydro-1,3-thiazolo[4,5-d]pyrimidine-2-thione

Synthesis and Antitumor Screening of Novel 3-Phenylthiazolo [4,5-d]pyrimidin-2-thione Derivatives

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