Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: Orally effective anti-inflammatory drug candidates
| Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
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| Data(s) |
20/10/2012
20/10/2012
2009
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| Resumo |
We described herein the molecular design of novel in vivo anti-inflammatory 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives (1) planned by applying the molecular hybridization approach. This work also points out to the discovery of LASSBio-930 (1c) as a novel anti-inflammatory and anti-hyperalgesic prototype, which was able to reduce carrageenan-induced rat paw edema with an ED(50) of 97.8 mu mol/kg, acting mainly as a non-selective COX inhibitor. (C) 2009 Elsevier Ltd. All rights reserved. CAPES (BR) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) CNPq (BR) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) FAPERJ (BR) Fundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) PRONEX (BR) IMINOFAR[420.015/05-1] IMINOFAR |
| Identificador |
BIOORGANIC & MEDICINAL CHEMISTRY, v.17, n.3, p.1125-1131, 2009 0968-0896 http://producao.usp.br/handle/BDPI/29969 10.1016/j.bmc.2008.12.045 |
| Idioma(s) |
eng |
| Publicador |
PERGAMON-ELSEVIER SCIENCE LTD |
| Relação |
Bioorganic & Medicinal Chemistry |
| Direitos |
restrictedAccess Copyright PERGAMON-ELSEVIER SCIENCE LTD |
| Palavras-Chave | #N-Acylhydrazone derivatives #Anti-inflammatory #Anti-hyperalgesic #COX-1 inhibitor #Safrole #1,3-Benzodioxole #NATURAL SAFROLE #PHARMACOLOGICAL EVALUATION #ANTITHROMBOTIC DRUGS #MEDICINAL CHEMISTRY #N-ACYLHYDRAZONES #LEAD-COMPOUNDS #DERIVATIVES #INFLAMMATION #CYCLOOXYGENASE-2 #DESIGN #Biochemistry & Molecular Biology #Chemistry, Medicinal #Chemistry, Organic |
| Tipo |
article original article publishedVersion |
