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- Title
HETEROCYCLES 46. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF THIAZOLO[3,2-b][1,2,4]TRIAZOLES BEARING BENZENESULFONAMIDE MOIETY.
- Authors
CRIST, ANAMARIA; LEONTE, DENISA; VLASE, LAURIAN; BENCZE, LÁSZLÓ CSABA; IMRE, SILVIA; APAN, BOGDAN; MOGOŞAN, CRISTINA; ZAHARIA, VALENTIN
- Abstract
In order to synthesize novel anti-inflammatory and analgesic compounds with reduced ulcerogenic risk, a series of thiazolo[3,2-b][1,2,4]triazoles (6a-6d) and their corresponding acyclic intermediates (5a-5d) bearing benzenesulfonamide moiety were obtained and characterized by spectral analysis (1 NMR, 13C NMR, IR and MS). All synthesized compounds were evaluated in vivo for their anti-inflammatory and antinociceptive activities in a rat model of acute inflammation induced by λ-carrageenan. The compounds 5b, 5c and 6d showed significant anti-inflammatory activity when compared to negative control group, but they did not show superior anti-inflammatory activity when compared to diclofenac, as reference drug. The compounds were also screened for antinociceptive activity in a model of inflammatory hyperalgesia and compounds 5a, 5b, 5c, 6a, 6d presented a significant increase of nociceptive threshold in the inflamed paw. Moreover, compounds 5c, 6a, 6b, 6c and 6d did not show any significant ulcerogenic activity.
- Subjects
HETEROCYCLIC compounds; TRIAZOLES synthesis; BENZENESULFONAMIDES; NONSTEROIDAL anti-inflammatory agents; NUCLEAR magnetic resonance
- Publication
Farmacia, 2018, Vol 66, Issue 5, p883
- ISSN
0014-8237
- Publication type
Article
- DOI
10.31925/farmacia.2018.5.20