Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives
AbstractThe 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. View Full-Text
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Silva, T.F.D.; Bispo Júnior, W.; Alexandre-Moreira, M.S.; Costa, F.N.; Monteiro, C.E.S.; Furlan Ferreira, F.; Barroso, R.C.R.; Noël, F.; Sudo, R.T.; Zapata-Sudo, G.; Lima, L.M.; Barreiro, E.J. Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives. Molecules 2015, 20, 3067-3088.
Silva TFD, Bispo Júnior W, Alexandre-Moreira MS, Costa FN, Monteiro CES, Furlan Ferreira F, Barroso RCR, Noël F, Sudo RT, Zapata-Sudo G, Lima LM, Barreiro EJ. Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives. Molecules. 2015; 20(2):3067-3088.Chicago/Turabian Style
Silva, Tiago Fernandes D.; Bispo Júnior, Walfrido; Alexandre-Moreira, Magna Suzana; Costa, Fanny Nascimento; Monteiro, Carlos E.S.; Furlan Ferreira, Fabio; Barroso, Regina Cely Rodrigues; Noël, François; Sudo, Roberto Takashi; Zapata-Sudo, Gisele; Lima, Lídia Moreira; Barreiro, Eliezer J. 2015. "Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives." Molecules 20, no. 2: 3067-3088.