Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria

…, SA Fraga-Spano, DJ Hlasta, SG Johnson…

Index: Macielag, Mark J.; Demers, James P.; Fraga-Spano, Stephanie A.; Hlasta, Dennis J.; Johnson, Sigmond G.; Kanojia, Ramesh M.; Russell, Ronald K.; Sui, Zhihua; Weidner-Wells, Michele A.; Werblood, Harvey; Foleno, Barbara D.; Goldschmidt, Raul M.; Loeloff, Michael J.; Webb, Glenda C.; Barrett, John F. Journal of Medicinal Chemistry, 1998 , vol. 41, # 16 p. 2939 - 2945

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Citation Number: 120

Abstract

A new class of inhibitors of the two-component regulatory systems (TCS) of bacteria was discovered based on the salicylanilide screening hits, closantel (1) and tetrachlorosalicylanilide (9). A systematic SAR study versus a model TCS, KinA/Spo0F, demonstrated the importance of electron-attracting substituents in the salicyloyl ring and hydrophobic groups in the anilide moiety for optimal activity. In addition, derivatives 8 and ...