Il Farmaco

Towards new neuroprotective agents: design and synthesis of 4H-thieno [2, 3-c] isoquinolin-5-one derivatives as potent PARP-1 inhibitors

R Pellicciari, E Camaioni, G Costantino, M Marinozzi…

Index: Pellicciari, Roberto; Camaioni, Emidio; Costantino, Gabriele; Marinozzi, Maura; Macchiarulo, Antonio; Moroni, Flavio; Natalini, Benedetto Farmaco, 2003 , vol. 58, # 9 p. 851 - 858

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Citation Number: 28

Abstract

An excessive activation of poly (ADP-ribose) polymerase-1 (PARP-1), a nuclear enzyme able to catalyze the transfer of ADP-ribose from NAD to acceptor proteins, is involved in the progression of neuronal damage after brain insult. Potent and selective PARP-1 inhibitors have neuroprotective properties in experimental models of brain ischemia. As a follow up of our previous structure–activity relationship study and in search for novel potent PARP-1 ...