Synthesis of Some 4,5-Dihydrothieno[3,2-e][1,2,4]Triazolo[4,3-a] Pyrimi-dine-2-Carboxamides as Anti-Inflammatory and Analgesic Agents | Zendy

Omaima G. Shaaban | Zendy; Ola H. Rizk | Zendy; Aida E. Bayad | Zendy; Ibrahim M. ElAshmawy | Zendy

Open Access

Synthesis of Some 4,5-Dihydrothieno[3,2-e][1,2,4]Triazolo[4,3-a] Pyrimi-dine-2-Carboxamides as Anti-Inflammatory and Analgesic Agents

Author(s) -

Omaima G. Shaaban,

Ola H. Rizk,

Aida E. Bayad,

Ibrahim M. ElAshmawy

Publication year - 2013

Publication title -

the open medicinal chemistry journal

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.294

H-Index - 18

ISSN - 1874-1045

DOI - 10.2174/1874104501307010049

Subject(s) - analgesic , pyrimidine , pharmacology , acute toxicity , anti inflammatory , chemistry , edema , diclofenac , analgesic agents , toxicity , medicine , stereochemistry , organic chemistry , surgery

A new series 4,5-dihydrothieno[ 3,2-e ][1,2,4]triazolo[ 4,3-a ]pyrimidine-2-carboxamide was synthesized. Twenty one newly synthesized compounds were investigated for their anti-inflammatory and analgesic activity using acute and subacute formalin-induced paw edema models and diclofenac Na as a reference. The acute toxicity (ALD50) and ulcerogenic effects of the active compounds were also determined. The thienotriazolopyrimidines 10a, 10c and 11c were found to exhibit remarkable anti-inflammatory activity at both models in addition to good analgesic activity with a delayed onset of action. Moreover, the active compounds showed high GI safety level and are well tolerated by experimental animals with high safety margin (ALD50 > 0.4 g/kg). Docking study using Molecular Operating Environment (MOE) version 2008.10 into COX-2 has been made for derivatives of highest anti-inflammatory activity.

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