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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
Authors:Ana Cristina Lima Leite  Renata Freitas Fisher Vieira  Diogo Rodrigo de M Moreira  Dalci Jose Brondani  Rajendra M Srivastava  Vernica Freitas da Silva  Marcos Antnio de Morais Júnior
Institution:Ana Cristina Lima Leite, Renata Freitas Fisher Vieira, Diogo Rodrigo de M. Moreira, Dalci Jose Brondani, Rajendra M. Srivastava, Verônica Freitas da Silva,Marcos Antônio de Morais Júnior,
Abstract:Compounds derived from 1,2,4-oxadiazole have being reported for their anti-inflamatory 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.
Keywords:Peptidomimetic  1  2  4-Oxadiazoles  Genotoxic activity
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