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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit

Texto completo
Autor(es):
Ferreira de Melo, Thais Regina [1] ; Chelucci, Rafael Consolin [1] ; Lopes Pires, Maria Elisa [1] ; Dutra, Luiz Antonio [1] ; Barbieri, Karina Pereira [1] ; Bosquesi, Priscila Longhin [1] ; Goulart Trossini, Gustavo Henrique [2] ; Chung, Man Chin [1] ; dos Santos, Jean Leandro [1]
Número total de Autores: 9
Afiliação do(s) autor(es):
[1] State Univ Sao Paulo UNESP, Sch Pharmaceut Sci, BR-14801902 Sao Paulo - Brazil
[2] Univ Sao Paulo, Fac Pharmaceut Sci, BR-05508900 Sao Paulo - Brazil
Número total de Afiliações: 2
Tipo de documento: Artigo Científico
Fonte: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES; v. 15, n. 4, p. 5821-5837, APR 2014.
Citações Web of Science: 11
Resumo

A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a-e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a-e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a-e are less gastrotoxic than the respective parent drug. Compounds 4b-e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a-b and 4d-e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a-e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non- steroidal anti-inflammatory drugs. (AU)

Processo FAPESP: 12/50359-2 - Planejamento, síntese e avaliação farmacológica de novas moléculas híbridas úteis ao tratamento de desordens hematológicas
Beneficiário:Jean Leandro dos Santos
Linha de fomento: Auxílio à Pesquisa - Parceria para Inovação Tecnológica - PITE
Processo FAPESP: 11/15204-5 - Síntese e avaliação farmacológica de novos compostos híbridos úteis para tratamento dos sintomas de anemia falciforme
Beneficiário:Thaís Regina Ferreira de Melo
Linha de fomento: Bolsas no Brasil - Mestrado