New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk

…, JM Domagala, RD Gogliotti, SE Hagen…

Index: Sanchez; Bridges; Bucsh; Domagala; Gogliotti; Hagen; Heifetz; Joannides; Sesnie; Shapiro; Szotek Journal of Medicinal Chemistry, 1992 ,  vol. 35,  # 2  p. 361 - 367

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Citation Number: 27

Abstract

(Figure 1). Our efforts in this area have resulted in the production of several diverse series of compounds, each of which has produced potential clinical candidates." One of these highly potent chemical entities, a 6, 8-difluoroquinolone, has shown a high degree of phototoxicity in several models, including man. The initial introduction of the 8-fluor0 substituent increased both in vitro activity and in vivo efficacy and provided the first examples of ...