Genotoxic activity of 3-[3-phenyl-1,2,4-oxadiazol-5-yl] propionic acid and its peptidyl derivatives determined by Ames and SOS response tests.
Compounds derived from 1,2,4-oxadiazole have being reported for their anti-inflammatory activity. However, those compounds should be devoid of any genotoxic side effect. In this work, the genotoxic activity of peptidomimetic moiety-containing 1,2,4-oxadiazoles derivatives was tested based on the Ames and SOS Chromotest. The results showed no mutagenic activity on the Ames test for 3-[3-phenyl-1,2,4-oxadiazol-5-yl] propionic acid (POPA) parental drug, but a weak SOS response induction on Chromotest. The chemical modifications reduced that response to a non-significative level, with l-phenylalanine peptidomimetic derivative being showing the lowest induction response. The results pointed out for the effectiveness of promoting chemical modifications of biological active compounds to increase its mode of action, showed in previous work, without increasing and even decreasing its DNA damage effect.
Leite
Ana Cristina Lima
AC
LABSINFA (Laboratório de Planejamento, Avaliação e Síntese de Fármacos) Centro de Ciências da Saúde, Recife, Brazil.
Vieira
Renata Freitas Fisher
RF
de M Moreira
Diogo Rodrigo
DR
Brondani
Dalci Jose
DJ
Srivastava
Rajendra M
RM
da Silva
Verônica Freitas
VF
de Morais Júnior
Marcos Antônio
MA
D000818:Animals; D004247:DNA / Q000187:drug effects; D004249:DNA Damage; D009152:Mutagenicity Tests / Q000379:methods; D009153:Mutagens / Q000737:chemistry* / Q000633:toxicity*; D010069:Oxadiazoles / Q000737:chemistry* / Q000633:toxicity*; D051381:Rats; D013014:SOS Response, Genetics / Q000187:drug effects*; D012486:Salmonella typhimurium / Q000187:drug effects
C092645:3-(3-phenyl-1,2,4-oxadiazol-5-yl)propionic acid; D009153:Mutagens; D010069:Oxadiazoles; D004247:DNA