Design and synthesis of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1, 3, 4, 5-tetrahydro-benzo [c][1, 6]-and [c][1, 7]-naphthyridin- …

D Ferraris, RP Ficco, T Pahutski, S Lautar…

Index: Ferraris, Dana; Ficco, Rica Pargas; Pahutski, Thomas; Lautar, Susan; Huang, Shirley; Zhang, Jie; Kalish, Vincent Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 15 p. 2513 - 2518

Full Text: HTML

Citation Number: 25

Abstract

The 1, 3, 4, 5-tetrahydro-benzo [c][1, 6]-and [c][1, 7]-napthyridin-6-ones are presented as a potent class of PARP-1 inhibitors. Derivatives of these partially saturated aza-5 [H]- phenanthridin-6-ones were designed and synthesized with tertiary amines for salt formation, thus enhancing aqueous solubility, iv formulation and their potential use in acute ischemic injuries (ie, myocardial ischemia and stroke). We found that partial saturation of the C-ring ...