Homo-Tris-Nitrones Derived from ?-Phenyl-N-tert-butylnitrone: Synthesis, Neuroprotection and Antioxidant Properties.
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ABSTRACT: Herein we report the synthesis, antioxidant and neuroprotective power of homo-tris-nitrones (HTN) 1-3, designed on the hypothesis that the incorporation of a third nitrone motif into our previously identified homo-bis-nitrone 6 (HBN6) would result in an improved and stronger neuroprotection. The neuroprotection of HTNs1-3, measured against oligomycin A/rotenone, showed that HTN2 was the best neuroprotective agent at a lower dose (EC50 = 51.63 ± 4.32 ?M), being similar in EC50 and maximal activity to ?-phenyl-N-tert-butylnitrone (PBN) and less potent than any of HBNs 4-6. The results of neuroprotection in an in vitro oxygen glucose deprivation model showed that HTN2 was the most powerful (EC50 = 87.57 ± 3.87 ?M), at lower dose, but 50-fold higher than its analogous HBN5, and ?1.7-fold less potent than PBN. HTN3 had a very good antinecrotic (IC50 = 3.47 ± 0.57 ?M), antiapoptotic, and antioxidant (EC50 = 6.77 ± 1.35 ?M) profile, very similar to that of its analogous HBN6. In spite of these results, and still being attractive neuroprotective agents, HTNs 2 and 3 do not have better neuroprotective properties than HBN6, but clearly exceed that of PBN.
SUBMITTER: Diez-Iriepa D
PROVIDER: S-EPMC7663103 | biostudies-literature | 2020 Oct
REPOSITORIES: biostudies-literature
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