Crohn's Disease is a chronic transmural inflammatory condition of the gastrointestinal mucosa that can affect any portion of the gastrointestinal tract. Although antibiotics are utilized in the management of Crohn's disease, there have been few controlled trials to support their efficacy. Metronidazole is the only antibiotic that has been shown to provide clinical benefits for patients with ileocolonic and perianal Crohn's disease. It's been suggested that ciprofloxacin in combination with metronidazole may be more effective than metronidazole alone in treatment of Crohn's disease.        Amino acids have been used as carriers of drugs because of their ability to transplant into mammalian tissue. Our long standing involvement in benzotriazole mediated peptide chemistry inspired us to design a new, effective and flexible methodology for synthesis of metronidazole bis conjugates.  Herein we report the synthesis of metronidazole bis conjugates with quinolone antibiotics and amino acids which show high potential as antibiotics against Crohn's disease.

Metronidazole bis-conjugates with antibiotics and amino acids

245th National Meeting (2013)

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