270575-91-2Relevant articles and documents
Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives
Kuemmerle, Arthur E.,Raimundo, Juliana M.,Leal, Carla M.,da Silva, Givanildo S.,Balliano, Tatiane L.,Pereira, Mariano A.,de Simone, Carlos A.,Sudo, Roberto T.,Zapata-Sudo, Gisele,Fraga, Carlos A.M.,Barreiro, Eliezer J.
experimental part, p. 4004 - 4009 (2009/12/04)
In this report we disclose the synthesis, vasodilatory activity, and identification of bioactive conformation of new N-acylhydrazone and N-methyl-N-acylhydrazone derivatives, structurally designed by bioisosteric replacements of previously described cardioactive compounds LASSBio-294 and its N-methyl derivative LASSBio-785. Some of these novel derivatives presented improved vasorelaxant properties, being new cardiovascular drug candidates.
Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters, derived from natural safrole
Lima, Patricia C.,Lima, Lidia M.,Da Silva, Kelli Cristine M.,Leda, Paulo Henrique O.,De Miranda, Ana Luisa P.,Fraga, Carlos A. M.,Barreiro, Eliezer J.
, p. 187 - 203 (2007/10/03)
A new series of antinociceptive compounds belonging to the N- acylarylhydrazone (NAH) class were synthesized from natural safrole (7). The most analgesic derivative represented by 10f, [(4'-N,N- dimethylaminobenzylidene-3-(3',4'-methylenedioxyphenyl)propionylhydrazine], was more potent than dipyrone and indomethacin, used as standards. The NAH compounds described herein were structurally planned by molecular hybridization and classical bioisosterism strategies on previously reported analgesic NAH in order to identify the pharmacophoric contribution of the N- acylarylhydrazone moiety and investigate the structure-activity relationship (SAR) in these series. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
