Synthesis and structural optimization of 7-(3,3-disubstituted-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids as antibacterial agents
摘要:
A series of the titled compounds were synthesized and tested for antibacterial activities in comparison with typical fluoroquinolones. (S)-3-Aminomethyl-3-fluoromethyl derivative (Y-688) was confirmed to be optimal because ofbeing most active especially against Gram-positive bacteria including fluoroquinolone-resistant strains and showing high photostability. (C) 1997 Elsevier Science Ltd.
Compounds of formula (I): ##STR1## (in which R.sup.1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.