Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.
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.
Kümmerle
Arthur E
AE
Laboratório de Avaliação e Síntese de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, RJ 21941-902, Brazil.
Raimundo
Juliana M
JM
Leal
Carla M
CM
da Silva
Givanildo S
GS
Balliano
Tatiane L
TL
Pereira
Mariano A
MA
de Simone
Carlos A
CA
Sudo
Roberto T
RT
Zapata-Sudo
Gisele
G
Fraga
Carlos A M
CA
Barreiro
Eliezer J
EJ
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*
D006835:Hydrazones; C439284:LASSBio 294; C503362:LASSBio-785; D013876:Thiophenes; D014665:Vasodilator Agents