Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK

…, KA Newlander, WJ Burgess, WE DeWolf…

Index: Seefeld, Mark A.; Miller, William H.; Newlander, Kenneth A.; Burgess, Walter J.; DeWolf Jr., Walter E.; Elkins, Patricia A.; Head, Martha S.; Jakas, Dalia R.; Janson, Cheryl A.; Keller, Paul M.; Manley, Peter J.; Moore, Terrance D.; Payne, David J.; Pearson, Stewart; Polizzi, Brian J.; Qiu, Xiayang; Rittenhouse, Stephen F.; Uzinskas, Irene N.; Wallis, Nicola G.; Huffman, William F. Journal of Medicinal Chemistry, 2003 , vol. 46, # 9 p. 1627 - 1635

Full Text: HTML

Citation Number: 126

Abstract

Bacterial enoyl-ACP reductase (FabI) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis and is an attractive target for the development of novel antibacterial agents. Previously we reported the development of FabI inhibitor 4 with narrow spectrum antimicrobial activity and in vivo efficacy against Staphylococcus aureus via intraperitoneal (ip) administration. Through iterative medicinal chemistry aided by X-ray crystal structure ...