Structure-activity relationships among DNA gyrase inhibitors. Synthesis and biological evaluation of 1, 2-dihydro-4, 4-dimethyl-1-oxo-2-naphthalenecarboxylic acids …

T Hogberg, I Khanna, SD Drake…

Index: Hoegberg, Thomas; Khanna, Ish; Drake, Steven D.; Mitscher, Lester A.; Shen, Linus L. Journal of Medicinal Chemistry, 1984 , vol. 27, # 3 p. 306 - 310

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Citation Number: 32

Abstract

A series of oxolinic acid analogues was synthesized in an attempt to evaluate the role, if any, played by the N-1 atom in putative modes of action of antimicrobial DNA gyrase inhibitors. Carba analogues were prepared because these have no possibility of an internal resonance contribution of the nitrogen atom and yet could otherwise satisfy electronic requirements of putative modes of action. Successful routes were developed involving Friedel-Craft's ...