Synthesis and antitubercular evaluation of new fluoroquinolone derivatives coupled with carbohydrates.
We describe in this work the synthesis of nine new fluoroquinolone derivatives based on modifications at the C-7 position of the known fluoroquinolones cipro-, gati-, and moxifloxacin, as well as their antitubercular evaluation. The synthesis of these new analogues was improved using microwave irradiation, providing several advantages such as better yields and shorter reaction times, in comparison with classical reaction conditions. Derivatives 4, 5, and 7 exhibited promising antitubercular activities.
Saraiva
Maurício F
MF
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, Brazil.
de Souza
Marcus V N
MV
Tran Huu Dau
Marie E
ME
Araújo
Débora P
DP
de Carvalho
Gustavo S G
GS
de Almeida
Mauro V
MV
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001372:Aza Compounds / Q000737:chemistry / Q000494:pharmacology; D002241:Carbohydrates / Q000737:chemistry*; D002939:Ciprofloxacin / Q000737:chemistry / Q000494:pharmacology; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077734:Gatifloxacin; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D000077266:Moxifloxacin; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology
D000995:Antitubercular Agents; D001372:Aza Compounds; D002241:Carbohydrates; D024841:Fluoroquinolones; D011804:Quinolines; D002939:Ciprofloxacin; D000077734:Gatifloxacin; D000077266:Moxifloxacin