| 摘要 |
THIS INVENTION PROVIDES A GUINOLONE DERIVATIVE WHICH EXERTS STRONG ANTIBACTERIAL ACTION UPON VARIOUS BACTERIA INCLUDING RESISTANT STRAINS AND HAS HIGH SAFETY. PARTICULARLY, IT RELATES TO A COMPOUND REPRESENTED BY THE FOLLOWING FORMULA (I), ITS SALTS AND HYDRATES THEREOF:(FORMULA I)WHEREIN R 1 AND R2 EACH INDEPENDENTLY REPRESENTS A HYDROGEN ATOM OR AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, IN WHICH THE ALKYL GROUP MAY HAVE ONE OR MORE SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF HYDROXYL GROUP, A HALOGEN ATOM, AN ALKYLTHIO GROUP HAVING 1 TO 6 CARBON ATOMS AND AN ALKYLOXY GROUP; N IS AN INTEGER OF 1 TO 4; AND QIS A PARTIAL STRUCTURE REPRESENTED BY THE FOLLOWING FORMULA (D):(FORMULA D)WHEREIN R3 REPRESENTS AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, AN ALKENYL GROUP HAVING 2 TO 6 CARBON ATOMS, A HALOGENOALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, A CYCLIC ALKYL GROUP HAVING 3 TO 6 CARBON ATOMS WHICH MAY HAVE A SUBSTITUENT, WITH THE PROVISO THAT WHEN R3 IS A CYCLOPROPYL GROUP IT IS SUBSTITUTED BY A HALOGEN COMPOUND AN ARYLGROUP WHICH MAY HAVE A SUBSTITUENT, A HETEROARYL GROUP WHICH MAY HAVE A SUBSTITUENT, AN ALKOXYL GROUP HAVING 1 TO 6 CARBON ATOMS OR AN ALKYLAMINO GROUP HAVING 1 TO 6 CARBON ATOMS;R4 REPRESENTS A HYDROGEN ATOM OR AN ALKYLTHIO GROUP HAVING 1 TO 6 CARBON ATOMS;R4 AND R3 MAY FORM TOGETHER WITH A PART OF THE MOTHER SKELETON A RING STRUCTURE OPTIONALLY CONTAINING A SULFUR ATOM AS A RING CONSTITUTING ATOM THEREOF AND OPTIONALLY HAVING AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS AS A SUBSTITUENT;R5 REPRESENTS A HYDROGEN ATOM, AN AMINO GROUP, A HYDROXYL GROUP, A THIOL GROUP, A HALOGENOMETHYL GROUP, AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, AN ALKENYL GROUP HAVING 2 TO 6 CARBON ATOMS, AN ALKYNYL GROUP HAVING 2 TO 6 CARBON ATOMS OR AN ALKOXYL GROUP HAVING 1 TO 6 CARBON ATOMS, IN WHICH THE AMINO GROUP MAY HAVE ONE OR MORE SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF A FORMYL GROUP, AN ALKY GROUP HAVING 1 TO 6 CARBON ATOMS AND AN ACYL GROUP HAVING 2 TO 5 CARBON ATOMS;X1 REPRESENTS A HALOGEN ATOM OR A HYDROGEN ATOM;A1 REPRESENTS A NITROGEN ATOM OR A PARTIAL STRUCTURE REPRESENTED BY FORMULA (II):(FORMULA II)WHEREIN X2 REPRESENTS A HYDROGEN ATOM, AN AMINO GROUP, A HALOGEN ATOM, A CYANO GROUP, A HALOGENOMETHYL GROUP, A HALOGENAMETHOXYL GROUP, AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, AN ALKENYL GROUP HAVING 2 TO 6 CARBON ATOMS, AN ALKYNYL GROUP HAVING 2 TO 6 CARBON ATOMS OR AN ALKOXYL GROUP HAVING 1 TO 6 CARBON ATOMS, IN WHICH THE AMINO GROUP MAY HAVE ONE OR MORE SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF A FORMYLGROUP, AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS AND AN ACYL GROUP HAVING 2 TO 5 CARBON ATOMS; ANDX2 AND R3 MAY FORM TOGETHER WITH A PART OF THE MOTHER SKELETON A RING STRUCTURE OPTIONALLY CONTAINING AN OXYGEN ATOM, A NITROGEN ATOM OR SULFUR ATOM AS A RING CONSTITUTING ATOM THEREOF AND OPTIONALLY HAVING AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS AS A SUBSTITUENT; ANDY REPRESENTS A HYDROGEN ATOM, A PHENYL GROUP, AN ACETOXYMETHYL GROUP, APIVALOYLOXYMETHYL GROUP, AN ETHOXYCARBONYL GROUP, A CHOLINE GROUP, ADIMETHYLAMINOETHYL GROUP, A 5-INDANYL GROUP, A PHTHALIDINYL GROUP, A 5-ALKYL-2-OXO-1 ,3-DIOXOL-4-YLMETHYL GROUP, A 3-ACETOXY-2-OXOBUTYL GROUP, AN ALKYL GROUP HAVING 1 TO 6 CARBON ATOMS, AN ALKOXYMETHYL GROUP HAVING 2 TO 7 CARBON ATOMS OR A PHENYLALKYL GROUP COMPOSED OF AN ALKYLENE GROUP HAVING 1 TO 6 CARBON ATOMS AND A PHENYL GROUP. |
