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A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC50=2 muM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (IC50<20 nM). Additionally, physicochemical and pharmacokinetic properties were evaluated. It could be shown that compounds bearing a piperazine or phenyl substituted betaAla-Gly side chain exhibited the best overall profile. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Recommanded Product: 3-Piperazin-1-yl-pyridazine, you can also check out more blogs about51047-56-4
Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2223 – PubChem