Ciprofloxacin analogues

Scheme 4.24 Synthesis of ciprofloxacin (A) and general structure of ciprofloxacin analogues (B).

Schwalbe T., Kadzimirsz D., las G. Synthesis of a library of ciprofloxacin analogues by means of sequential organic synthesis in microreactors. QSAR Comb. Sci. 2005 24(6) 758-768. 

Surprisingly, in the light of the results of studies such as those described above, the 1-t-butyl analogues (36) exhibit excellent antibacterial properties [83], The results for the in vitro evaluation of these agents relative to ciprofloxacin are shown in Table 6.14. Compound (36a), the 1-/-butyl analogue of... 

In a study aimed at examining both the electronic influence of attaching a phenyl ring to the cyclopropyl ring of ciprofloxacin and the tolerance to this added steric bulk, the enantiomeric fraiu-disubstituted cyclopropane analogues (60) and (61) were prepared [94]. In general, the (1 S,2R)-enantiomer (61) is... 

The 3-formyl analogues of norfloxacin, pefloxacin and ciprofloxacin, (82a-c) have also been shown to function as prodrugs of their respective parent... 

Small-scale combinatorial chemistry for library and analogue generation is easily automated with microreactors, using similar technology to that used for automated hplc, where sequential syntheses can be carried out on the same chip , for example in the preparation of analogues of ciprofloxacin. ... 

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