Published January 1, 2013
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Synthesis and Pharmacological Evaluation of Some Novel Thebaine Derivatives: N-(Tetrazol-1H-5-yl)-6,14-endoethenotetrahydrothebaine Incorporating the 1,3,4-Oxadiazole or the 1,3,4-Thiadiazole Moiety
Creators
- 1. Gazi Univ, Fac Sci, Dept Chem, TR-06500 Ankara, Turkey
- 2. Gazi Univ, Fac Med, Dept Anesthesiol & Reanimat, TR-06500 Ankara, Turkey
- 3. Diskapi Yildirim Bayezit Res & Educ Hosp, Dept Pathol, Ankara, Turkey
- 4. Gazi Univ, Fac Med, Dept Clin Biochem, TR-06500 Ankara, Turkey
- 5. Gazi Univ, Fac Pharm, Dept Pharmacol, TR-06500 Ankara, Turkey
Description
In this study, we synthesized some novel N-(tetrazol-1H-5-yl)-6,14-endoethenotetrahydrothebaine 7-substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives as potential analgesic agents. The structures of the compounds were established on the basis of their IR, 1H NMR, 13C NMR, 2D NMR, and high-resolution mass spectral data. The analgesic activity was evaluated by a rat-hot plate test model and a rat tail-flick model. Compound 12 showed analgesic activity higher than that of morphine. In addition to a histopathological and biochemical evaluation, the LD50 dose for the most active compound 12 was determined.
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