New 1,3,4-thiadiazole derivatives endowed with analgesic and anti-inflammatory activities

New 2,4-disubstituted 1,3,4-thiadiazole derivatives 3a– t were synthesized and tested for pharmacological actions. Compounds showed interesting analgesic and anti-inflammatory activity in vivo; ulcerogenic action was also reported. Two series of N-[5-oxo-4-(arylsulfonyl)-4,5-dihydro-1,3,4-thiadiazol...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2006-03, Vol.14 (6), p.1698-1705
Main Authors: Schenone, Silvia, Brullo, Chiara, Bruno, Olga, Bondavalli, Francesco, Ranise, Angelo, Filippelli, Walter, Rinaldi, Barbara, Capuano, Annalisa, Falcone, Giuseppe
Format: Article
Language:English
Subjects:
1,3,4-Thiadiazoles
Amides - chemical synthesis
Amides - chemistry
Analgesic activity
Analgesics
Analgesics - chemical synthesis
Analgesics - chemistry
Analgesics - pharmacology
Animals
Anti-inflammatory activity
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - chemistry
Anti-Inflammatory Agents - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Drug Evaluation, Preclinical
Female
Indomethacin - pharmacology
Intestinal Mucosa - drug effects
Male
Medical sciences
Mice
Neuropharmacology
Pharmacology. Drug treatments
Rats
Stomach Ulcer - complications
Thiadiazoles - chemical synthesis
Thiadiazoles - chemistry
Thiadiazoles - pharmacology
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Summary:New 2,4-disubstituted 1,3,4-thiadiazole derivatives 3a– t were synthesized and tested for pharmacological actions. Compounds showed interesting analgesic and anti-inflammatory activity in vivo; ulcerogenic action was also reported. Two series of N-[5-oxo-4-(arylsulfonyl)-4,5-dihydro-1,3,4-thiadiazol-2-yl]-amides were synthesized and tested in vivo for their analgesic and anti-inflammatory activities. All the new compounds possess good antalgic action in the acetic acid writhing test and some terms of the series showed also fair anti-inflammatory activity in the carrageenan rat paw edema test. Ulcerogenic and irritative action on the gastrointestinal mucose, in comparison with indomethacin is low.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2005.10.064