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- Title
Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives.
- Authors
Fernandes da Silva, Tiago; Bispo Júnior, Walfrido; Alexandre-Moreira, Magna Suzana; Nascimento Costa, Fanny; da Silva Monteiro, Carlos Eduardo; Ferreira, Fabio Furlan; Rodrigues Barroso, Regina Cely; Noël, François; Takashi Sudo, Roberto; Zapata-Sudo, Gisele; Moreira Lima, Lídia; Barreiro, Eliezer J.
- Abstract
The N-acylhydrazone (NAH) moiety is considered a privileged structure, being present in many compounds with diverse pharmacological activities. Among the activities attributed to NAH derivatives anti-inflammatory and analgesic ones are recurrent. As part of a research program aiming at the design of new analgesic and anti-inflammatory lead-candidates, a series of cyclohexyl-N-acylhydrazones 10-26 were structurally designed from molecular modification on the prototype LASSBio-294, representing a new class of cycloalkyl analogues. Compounds 10-26 and their conformationally restricted analogue 9 were synthetized and evaluated as analgesic and anti-inflammatory agents in classical pharmacologic protocols. The cyclohexyl-N-acylhydrazones 10-26 and the cyclohexenyl analogue 9 showed great anti-inflammatory and/or analgesic activities, but compound 13 stood out as a new prototype to treat acute and chronic painful states due to its important analgesic activity in a neuropathic pain model.
- Subjects
ANALGESICS; ANTI-inflammatory agents; CHEMICAL derivatives; CYCLOALKYL group; PHARMACOLOGY
- Publication
Molecules, 2015, Vol 20, Issue 2, p3067
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules20023067