title: Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.
abstract: 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.
authors.affiliation: Laboratório de Avaliação e Síntese de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, RJ 21941-902, Brazil.
authors.forename: Arthur E
authors.initials: AE
authors.lastname: Kümmerle
authors.forename: Juliana M
authors.initials: JM
authors.lastname: Raimundo
authors.forename: Carla M
authors.initials: CM
authors.lastname: Leal
authors.forename: Givanildo S
authors.initials: GS
authors.lastname: da Silva
authors.forename: Tatiane L
authors.initials: TL
authors.lastname: Balliano
authors.forename: Mariano A
authors.initials: MA
authors.lastname: Pereira
authors.forename: Carlos A
authors.initials: CA
authors.lastname: de Simone
authors.forename: Roberto T
authors.initials: RT
authors.lastname: Sudo
authors.forename: Gisele
authors.initials: G
authors.lastname: Zapata-Sudo
authors.forename: Carlos A M
authors.initials: CA
authors.lastname: Fraga
authors.forename: Eliezer J
authors.initials: EJ
authors.lastname: Barreiro
mesh_terms: D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D018360:Crystallography, X-Ray; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008297:Male; D008958:Models, Molecular; D051381:Rats; D017208:Rats, Wistar; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D006835:Hydrazones; C439284:LASSBio 294; C503362:LASSBio-785; D013876:Thiophenes; D014665:Vasodilator Agents