Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases
| Autor: | Vittorio A. Sauro, Chetan Pandit, Yong Kang Zhang, Kirk R. Maples, Stephen J. Baker, Rajeshwar Singh, Stephen J. Benkovic, Jacob J. Plattner, Ving J. Lee, Tsutomu Akama, Maureen Kully, Jehangir Khan |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Boron Compounds
Pyridines medicine.drug_class Gram-positive bacteria Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science Borane Skin Diseases Biochemistry Anti-inflammatory Structure-Activity Relationship chemistry.chemical_compound Minimum inhibitory concentration Drug Discovery Leukocytes medicine Humans Structure–activity relationship Boranes Molecular Biology Borinic acid Boron Antibacterial agent Molecular Structure biology Organic Chemistry Esters biology.organism_classification Anti-Bacterial Agents chemistry Cytokines Molecular Medicine Antibacterial activity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 16:5963-5967 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2006.08.130 |
| Popis: | A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studies, we identified 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (2g, AN0128) as having the best combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions. |
| Databáze: | OpenAIRE |
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