| 摘要 |
Esters of nitroxoline with mono- or poly-carboxylic or sulphonic acids, esp. of formula (I), are new cpds. (where X is CO or SO2; R is =17C opt. unsatd., (branched) hydrocarbyl, aryl or aralkyl in which each phenyl ring can be substd. by >=1.1-4C alkyl, F, Cl, Br, NO2 or CN, a gp.-AXOY, or adamantyl; A is 2-20C opt. unsatd. hydrocarbyl; Y is H, 1-4C alkyl or 5-nitroquinolin-8-yl). (I) are prepd. by reacting nitroxoline (II) with the appropriate acid or its deriv. (I) are useful antibacterials and antifungals at least as effective as (II) but with a longer-lasting effect and better oil solubility. Toxicity is low e.g. the LDo=>=1.1g/kg orally in rats. Specific cpd. is 5-nitroquinolin-8-yl undecylinate. |
