title: Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives.
abstract: This paper describes the synthesis of new cyclic imides obtained by reaction with N-antipyrine-3,4-dichloromaleimides and different aromatic amines. The analgesic activity of the synthesized compounds was initially investigated against the writhing test in mice, followed by analysis of the most promising compounds in this model and in the formalin-induced model. The results indicate that the compounds containing the electron-withdrawing substituents in the para position of the substitute ring exerted more potent analgesic activity in mice, being much more potent than the prototype N-antipyrine-3,4-dichloromaleimide and some reference drugs. Some compounds exhibited activity against human opportunistic and pathogenic fungi, with MIC values of between 40 and 100 μg/mL (91.74 and 236.96 μM), and it was verified that only a few compounds presented potential for cytotoxic activity.
authors: Núcleo de Investigações Químico-Farmacêuticas/CCS, Universidade do Vale do Itajaí, Caixa Postal 360, CEP 88302-202, Itajaí, Santa Catarina, Brazil.
authors: Fernanda
authors: F
authors: Mahle
authors: Tatiana da Rosa
authors: Tda R
authors: Guimarães
authors: Aleandra Vergilina
authors: AV
authors: Meira
authors: Rogério
authors: R
authors: Corrêa
authors: Rosana Cé
authors: RC
authors: Bella Cruz
authors: Alexandre
authors: A
authors: Bella Cruz
authors: Ricardo José
authors: RJ
authors: Nunes
authors: Valdir
authors: V
authors: Cechinel-Filho
authors: Fátima
authors: F
authors: de Campos-Buzzi
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000983:Antipyrine / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D008301:Maleimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D008301:Maleimides; D000983:Antipyrine