| 摘要 |
Naphthalene derivatives (or mono- or polyaza analogs) (I), having a side-chain containing a cycloalkylene, heterocycloalkylene, arylene or heteroarylene group in the 1-position, are new. Naphthalene or mono- or polyaza-naphthalene derivatives of formula (I) and their salts, solvates and hydrates are new; [Image] A : O, S, NH, alkylene, alkenylene, alkynylene or heteroalkylene; X 1>-X 5>N, CH or CR 4>; Cy : cycloalkylene, heterocycloalkylene, arylene or heteroarylene; R 1>H, halo, OH, NH 2, SH, alkyl, heteroalkyl, alkoxy, heteroalkoxy, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, cycloalkoxy, alkylcycloalkoxy, heterocycloalkoxy or heteroalkylcycloalkoxy; R 2>halo, OH, NH 2, SH, alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; or two R 2>groups together form part of an aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aralkyl or heteroaralkyl ring; R 3>alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; R 4>halo, OH, alkyl, alkenyl, alkynyl or heteroaralkyl; and m, n : 0-2. ACTIVITY : Antibacterial. MECHANISM OF ACTION : DNA Gyrase Inhibitor; Topoisomerase IV Inhibitor. |
