Synthesis, selective anti-Helicobacter pylori activity, and cytotoxicity of novel N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides.
N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones. Some of them possessed the best activity against H. pylori metronidazole resistant strains with MIC values lower than the drug reference (metronidazole). Furthermore, anti-inflammatory activity through the inhibition of the IL-8 production was investigated.
Chimenti
Franco
F
Dipartimento di Chimica e Tecnologie del Farmaco, Università 'La Sapienza', P.le A. Moro 5, 00185 Rome, Italy.
Bizzarri
Bruna
B
Bolasco
Adriana
A
Secci
Daniela
D
Chimenti
Paola
P
Granese
Arianna
A
Carradori
Simone
S
Rivanera
Daniela
D
Zicari
Alessandra
A
Scaltrito
M Maddalena
MM
Sisto
Francesca
F
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D024881:Drug Resistance, Bacterial; D016480:Helicobacter pylori / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D016209:Interleukin-8 / Q000378:metabolism; D008795:Metronidazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D003374:Coumarins; D016209:Interleukin-8; D008795:Metronidazole; C030123:coumarin